- acetylcholine binding protein
- muscarinic acetylcholine receptor
- neuronal acetylcholine receptor
- nicotinic acetylcholine receptor
- soluble acetylcholine receptor
- acetylcholine receptor subunit alpha/neuronal acetylcholine receptor subunit beta-2
- acetylcholine receptor subunit alpha/neuronal acetylcholine receptor subunit beta-4
- acetylcholine receptor subunit alpha
- acetylcholine receptor subunit delta
- muscarinic acetylcholine receptor m1
- muscarinic acetylcholine receptor m2
- muscarinic acetylcholine receptor m3
- muscarinic acetylcholine receptor m4
- muscarinic acetylcholine receptor m5
- neuronal nicotinic acetylcholine receptor
- acetylcholine receptor protein alpha chain
- acetylcholine receptor protein delta chain
- acetylcholine receptor protein epsilon chain
- acetylcholine-binding protein (ls-achbp)
- muscarinic acetylcholine receptor m2 and m4
- muscarinic acetylcholine receptor m2 and m5
- neuronal acetylcholine receptor (alpha4beta2 nachr)
- neuronal acetylcholine receptor alpha4/beta2
- neuronal acetylcholine receptor; alpha2/beta2
- neuronal acetylcholine receptor; alpha2/beta4
- neuronal acetylcholine receptor; alpha4/beta4
- nicotinic acetylcholine receptor alpha1 subunit
- nicotinic acetylcholine receptor alpha9/alpha10
- acetylcholine receptor subunit beta-like 2
- acetylcholine receptor; alpha1/beta1/delta/gamma
- neuronal acetylcholine receptor subunit alpha-10
- neuronal acetylcholine receptor subunit alpha-2
- neuronal acetylcholine receptor subunit alpha-3
- neuronal acetylcholine receptor subunit alpha-4
- neuronal acetylcholine receptor subunit alpha-5
- neuronal acetylcholine receptor subunit alpha-6
- neuronal acetylcholine receptor subunit alpha-7
- neuronal acetylcholine receptor subunit alpha-9
- neuronal acetylcholine receptor subunit beta-2
- neuronal acetylcholine receptor subunit beta-4
- nicotinic acetylcholine receptor alpha3/beta2/alpha5
- nicotinic acetylcholine receptor alpha3/beta4/alpha5
- nicotinic acetylcholine receptor alpha4/beta2/alpha5
- nicotinic acetylcholine receptor alpha6/alpha3/beta4
- nicotinic acetylcholine receptor subunit alpha-9
- acetylcholine receptor subunit alpha/beta/delta/epsilon
- acetylcholine receptor subunit alpha/beta/delta/gamma
- neuronal acetylcholine receptor alpha-2/beta-2
- neuronal acetylcholine receptor alpha-2/beta-4
- neuronal acetylcholine receptor protein alpha-6 subunit
- neuronal acetylcholine receptor protein alpha-7 subunit
- neuronal acetylcholine receptor subunit alpha-7 (nachr)
- neuronal acetylcholine receptor; alpha3/alpha6/beta2/beta3
- nicotinic acetylcholine receptor alpha-1/beta-1
- nicotinic acetylcholine receptor alpha1/beta1/epsilon/delta
- nicotinic acetylcholine receptor alpha1/beta1/gamma/delta
- nicotinic acetylcholine receptor alpha6/alpha3/beta2/beta3
- isoform alpha-4-2 of neuronal acetylcholine receptor subunit alpha-4 (alpha-4-2)/neuronal acetylcholine receptor subunit beta-2
- acetylcholine receptor protein alpha/beta/delta/gamma chain
- neuronal acetylcholine receptor subunit alpha 4 beta 2
- neuronal acetylcholine receptor subunit alpha-10/alpha-9
- neuronal acetylcholine receptor subunit alpha-3/beta-4
- neuronal acetylcholine receptor subunit alpha-4/beta-2
- neuronal acetylcholine receptor subunit alpha-6/beta-2
- neuronal acetylcholine receptor subunit alpha-6/beta-3
- neuronal acetylcholine receptor subunit alpha-6/beta-4
- neuronal acetylcholine receptor subunit beta-2/beta-4
- neuronal acetylcholine receptor protein alpha-10/alpha-9 subunit
- neuronal acetylcholine receptor protein alpha-2/beta-2 subunit
- neuronal acetylcholine receptor protein alpha-3/beta-2 subunit
- neuronal acetylcholine receptor protein alpha-4/beta-2 subunit
- nicotinic acetylcholine receptor alpha-1/beta-1/delta/epsilon
- nicotinic acetylcholine receptor alpha-3/beta-4/alpha-5
- neuronal acetylcholine receptor protein alpha-2 subunit/subunit beta-4
- neuronal acetylcholine receptor protein beta-2 subunit/subunit alpha-3
- neuronal acetylcholine receptor subunit alpha-3/alpha-5/beta-4
- neuronal acetylcholine receptor subunit alpha-3/alpha-6/beta-3
- neuronal acetylcholine receptor subunit alpha-3/alpha-6/beta-4
- neuronal acetylcholine receptor subunit alpha-3/alpha-6/beta-2/beta-3
- isoform alpha-4-2 of neuronal acetylcholine receptor subunit alpha-4 (alpha-4-2)
- muscarinic acetylcholine receptor m3 [1-273,470-589,n6q,n15q,n41q,n48q,n52q,f550c]
- muscarinic acetylcholine receptor m3 [1-273,470-589,n6q,n15q,n41q,n48q,n52q,f554c]
- muscarinic acetylcholine receptor m3 [1-273,470-589,n6q,n15q,n41q,n48q,n52q,r551c]
- muscarinic acetylcholine receptor m3 [1-273,470-589,n6q,n15q,n41q,n48q,n52q,t556c]
BDBM29405 acetylcholine chloride
BDBM10759 2-acetoxyethyl(trimethyl)ammonium;bromide 2-acetoxyethyl(trimethyl)ammonium;perchlorate CHEMBL667 US10667515, Compound ACh [2-(acetyloxy)ethyl]trimethylazanium acetylcholine acetylcholine chloride cid_6060
- Nemecz, Akos; Taylor, Palmer Creating an a7 Nicotinic Acetylcholine Recognition Domain from the Acetylcholine-binding Protein Taylor Research Group (2014)
- Hansen, CP; Jensen, AA; Christensen, JK; Balle, T; Liljefors, T; Frølund, B Novel acetylcholine and carbamoylcholine analogues: development of a functionally selective alpha4beta2 nicotinic acetylcholine receptor agonist. J Med Chem 51: 7380-95 (2009)
- Lindsley, CW; Conn, PJ; Engers, DW; Bender, AM; Engers, JL Antagonists of the muscarinic acetylcholine receptor M4 US Patent US11149022 (2021)
- Slavov, SH; Radzvilovits, M; LeFrancois, S; Stoyanova-Slavova, IB; Soti, F; Kem, WR; Katritzky, AR A computational study of the binding of 3-(arylidene) anabaseines to two major brain nicotinic acetylcholine receptors and to the acetylcholine binding protein. Eur J Med Chem 45: 2433-46 (2010)
- Kargbo, RB Allosteric Modulators of the M4 Muscarinic Acetylcholine Receptor. ACS Med Chem Lett 9: 783-784 (2018)
- Faghih, R; Gopalakrishnan, M; Briggs, CA Allosteric modulators of the alpha7 nicotinic acetylcholine receptor. J Med Chem 51: 701-12 (2008)
- Rosse, G Anabaseine analogues as modulators of nicotinic acetylcholine receptor. ACS Med Chem Lett 4: 902-3 (2013)
- Ragab, HM; Kim, JS; Dukat, M; Navarro, H; Glennon, RA Aryloxyethylamines: binding at alpha7 nicotinic acetylcholine receptors. Bioorg Med Chem Lett 16: 4283-6 (2006)
- Efange, SM; Khare, A; Parsons, SM; Bau, R; Metzenthin, T Nonsymmetrical bipiperidyls as inhibitors of vesicular acetylcholine storage. J Med Chem 36: 985-9 (1993)
- Rosse, G Positive allosteric modulators of nicotinic acetylcholine receptor. ACS Med Chem Lett 4: 319-20 (2013)
- Acharya, R; Burnett, DA; Bursavich, MG; Cook, AS; Harrison, BA; McRiner, AJ Aminobenzisoxazole compounds as agonists of α7-nicotinic acetylcholine receptors US Patent US10370370 (2019)
- Bolchi, C; Valoti, E; Binda, M; Fasoli, F; Ferrara, R; Fumagalli, L; Gotti, C; Matucci, R; Vistoli, G; Pallavicini, M Design, synthesis and binding affinity of acetylcholine carbamoyl analogues. Bioorg Med Chem Lett 23: 6481-5 (2013)
- Mazurov, AA; Speake, JD; Yohannes, D Discovery and development ofa7 nicotinic acetylcholine receptor modulators. J Med Chem 54: 7943-61 (2011)
- Abin-Carriquiry, JA; Zunini, MP; Cassels, BK; Wonnacott, S; Dajas, F In silico characterization of cytisinoids docked into an acetylcholine binding protein. Bioorg Med Chem Lett 20: 3683-7 (2010)
- Lee, NR; Zhang, X; Darna, M; Dwoskin, LP; Zheng, G Muscarinic acetylcholine receptor binding affinities of pethidine analogs. Bioorg Med Chem Lett 25: 5032-5 (2015)
- Holladay, MW; Dart, MJ; Lynch, JK Neuronal nicotinic acetylcholine receptors as targets for drug discovery. J Med Chem 40: 4169-94 (1998)
- Lindsley, CW; Conn, PJ; Engers, DW; Bollinger, S; Tarr, JC; Spearing, P; Engers, JL; Long, M; Bridges, TM Positive allosteric modulators of the muscarinic acetylcholine receptor M4 US Patent US10239887 (2019)
- Tu, Z; Luo, Z; Liu, H; Jin, H; Parsons, SM Sulfur-containing compounds targeting vesicular acetylcholine transporter US Patent US10421722 (2019)
- Kombo, DC; Mazurov, A; Tallapragada, K; Hammond, PS; Chewning, J; Hauser, TA; Vasquez-Valdivieso, M; Yohannes, D; Talley, TT; Taylor, P; Caldwell, WS Docking studies of benzylidene anabaseine interactions witha7 nicotinic acetylcholine receptor (nAChR) and acetylcholine binding proteins (AChBPs): application to the design of relateda7 selective ligands. Eur J Med Chem 46: 5625-35 (2011)
- Ding, YS; Kil, KE; Lin, KS; Ma, W; Yokota, Y; Carroll, IF A novel nicotinic acetylcholine receptor antagonist radioligand for PET studies. Bioorg Med Chem Lett 16: 1049-53 (2006)
- Iturriaga-Vásquez, P; Pérez, EG; Slater, EY; Bermúdez, I; Cassels, BK Aporphine metho salts as neuronal nicotinic acetylcholine receptor blockers. Bioorg Med Chem 15: 3368-72 (2007)
- McDonald, IM; Mate, RA; Zusi, FC; Huang, H; Post-Munson, DJ; Ferrante, MA; Gallagher, L; Bertekap, RL; Knox, RJ; Robertson, BJ; Harden, DG; Morgan, DG; Lodge, NJ; Dworetzky, SI; Olson, RE; Macor, JE Discovery of a novel series of quinolonea7 nicotinic acetylcholine receptor agonists. Bioorg Med Chem Lett 23: 1684-8 (2013)
- Jin, J; Wang, Y; Shi, D; Wang, F; Davis, RS; Jin, Q; Fu, W; Foley, JJ; Webb, EF; Dehaas, CJ; Berlanga, M; Burman, M; Sarau, HM; Morrow, DM; Rao, P; Kallal, LA; Moore, ML; Rivero, RA; Palovich, M; Salmon, M; Belmonte, KE; Busch-Petersen, J Discovery of novel and long acting muscarinic acetylcholine receptor antagonists. J Med Chem 51: 4866-9 (2008)
- Cheng, K; Khurana, S; Chen, Y; Kennedy, RH; Zimniak, P; Raufman, JP Lithocholylcholine, a bile acid/acetylcholine hybrid, is a muscarinic receptor antagonist. J Pharmacol Exp Ther 303: 29-35 (2002)
- Jin, J; Wang, Y; Shi, D; Wang, F; Fu, W; Davis, RS; Jin, Q; Foley, JJ; Sarau, HM; Morrow, DM; Moore, ML; Rivero, RA; Palovich, M; Salmon, M; Belmonte, KE; Busch-Petersen, J Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas. Bioorg Med Chem Lett 18: 5481-6 (2008)
- Faundez-Parraguez, M; Farias-Rabelo, N; Gonzalez-Gutierrez, JP; Etcheverry-Berrios, A; Alzate-Morales, J; Adasme-Carreño, F; Varas, R; Bermudez, I; Iturriaga-Vasquez, P Neonicotinic analogues: selective antagonists fora4ß2 nicotinic acetylcholine receptors. Bioorg Med Chem 21: 2687-94 (2013)
- Mazurov, A; Miao, L; Xiao, Y Nicotinic acetylcholine receptor sub-type selective amides of diazabicycloalkanes US Patent US8921410 (2014)
- Lynagh, T; Kiontke, S; Meyhoff-Madsen, M; Gless, BH; Johannesen, J; Kattelmann, S; Christiansen, A; Dufva, M; Laustsen, AH; Devkota, K; Olsen, CA; K?mmel, D; Pless, SA; Lohse, B Peptide Inhibitors of the ?-Cobratoxin-Nicotinic Acetylcholine Receptor Interaction. J Med Chem 63: 13709-13718 (2020)
- Leonik, FM; Papke, RL; Horenstein, NA Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors. Bioorg Med Chem Lett 17: 1520-2 (2007)
- Chen, X; Kl?ckner, J; Holze, J; Zimmermann, C; Seemann, WK; Schrage, R; Bock, A; Mohr, K; Tr?nkle, C; Holzgrabe, U; Decker, M Rational design of partial agonists for the muscarinic m1 acetylcholine receptor. J Med Chem 58: 560-76 (2015)
- Miller, DK; Wong, EH; Chesnut, MD; Dwoskin, LP Reboxetine: functional inhibition of monoamine transporters and nicotinic acetylcholine receptors. J Pharmacol Exp Ther 302: 687-95 (2002)
- Yu, LF; Zhang, HK; Caldarone, BJ; Eaton, JB; Lukas, RJ; Kozikowski, AP Recent developments in novel antidepressants targetinga4ß2-nicotinic acetylcholine receptors. J Med Chem 57: 8204-23 (2014)
- Christopoulos, A; Grant, MK; Ayoubzadeh, N; Kim, ON; Sauerberg, P; Jeppesen, L; El-Fakahany, EE Synthesis and pharmacological evaluation of dimeric muscarinic acetylcholine receptor agonists. J Pharmacol Exp Ther 298: 1260-8 (2001)
- Tomassoli, I; G?ndisch, D The twin drug approach for novel nicotinic acetylcholine receptor ligands. Bioorg Med Chem 23: 4375-89 (2015)
- Blass, BE Allosteric Modulators of Nicotinic Acetylcholine Receptors Useful for the Treatment of Cognitive Impairment. ACS Med Chem Lett 9: 163-164 (2018)
- Fleβner, T; Böβ, F; Erb, C; Hafner, F; Schnizler, K; Lang, D; Luithle, J; Van Kampen, M; Van Der Staay, F Azabicyclic carbamates and their use as alpha-7 nicotinic acetylcholine receptor agonists US Patent US9714242 (2017)
- Jensen, AA; Mikkelsen, I; Frølund, B; Bräuner-Osborne, H; Falch, E; Krogsgaard-Larsen, P Carbamoylcholine homologs: novel and potent agonists at neuronal nicotinic acetylcholine receptors. Mol Pharmacol 64: 865-75 (2003)
- Bonner, TI; Young, AC; Brann, MR; Buckley, NJ Cloning and expression of the human and rat m5 muscarinic acetylcholine receptor genes. Neuron 1: 403-10 (1988)
- Brissonnet, Y; Araoz, R; Sousa, R; Percevault, L; Brument, S; Deniaud, D; Servent, D; Le Questel, JY; Lebreton, J; Gouin, SG Di- and heptavalent nicotinic analogues to interfere with ?7 nicotinic acetylcholine receptors. Bioorg Med Chem 27: 700-707 (2019)
- Strachan, JP; Farias, JJ; Zhang, J; Caldwell, WS; Bhatti, BS Diazaspirocyclic compounds as selective ligands for thea4ß2 nicotinic acetylcholine receptor. Bioorg Med Chem Lett 22: 5089-92 (2012)
- Ziegler, N; Bätz, J; Zabel, U; Lohse, MJ; Hoffmann, C FRET-based sensors for the human M1-, M3-, and M5-acetylcholine receptors. Bioorg Med Chem 19: 1048-54 (2011)
- Li, J; Zhang, X; Zhang, Z; Padakanti, PK; Jin, H; Cui, J; Li, A; Zeng, D; Rath, NP; Flores, H; Perlmutter, JS; Parsons, SM; Tu, Z Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter. J Med Chem 56: 6216-33 (2013)
- Ferretti, G; Dukat, M; Giannella, M; Piergentili, A; Pigini, M; Quaglia, W; Damaj, MI; Martin, BR; Glennon, RA Homoazanicotine: a structure-affinity study for nicotinic acetylcholine (nACh) receptor binding. J Med Chem 45: 4724-31 (2002)
- Efange, SM; Khare, AB; Mach, RH; Parsons, SM Hydroxylated decahydroquinolines as ligands for the vesicular acetylcholine transporter: synthesis and biological evaluation. J Med Chem 42: 2862-9 (1999)
- Honda, H; Tomizawa, M; Casida, JE Insect muscarinic acetylcholine receptor: pharmacological and toxicological profiles of antagonists and agonists. J Agric Food Chem 55: 2276-81 (2007)
- Jacyno, JM; Harwood, JS; Lin, NH; Campbell, JE; Sullivan, JP; Holladay, MW Lycaconitine revisited: partial synthesis and neuronal nicotinic acetylcholine receptor affinities. J Nat Prod 59: 707-9 (1996)
- Schmitt, JD; Sharples, CG; Caldwell, WS Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions. J Med Chem 42: 3066-74 (1999)
- Chojnacka, K; Papke, RL; Horenstein, NA Synthesis and evaluation of a conditionally-silent agonist for thea7 nicotinic acetylcholine receptor. Bioorg Med Chem Lett 23: 4145-9 (2013)
- Mullen, G; Napier, J; Balestra, M; DeCory, T; Hale, G; Macor, J; Mack, R; Loch, J; Wu, E; Kover, A; Verhoest, P; Sampognaro, A; Phillips, E; Zhu, Y; Murray, R; Griffith, R; Blosser, J; Gurley, D; Machulskis, A; Zongrone, J; Rosen, A; Gordon, J (-)-Spiro[1-azabicyclo[2.2.2]octane-3,5'-oxazolidin-2'-one], a conformationally restricted analogue of acetylcholine, is a highly selective full agonist at the alpha 7 nicotinic acetylcholine receptor. J Med Chem 43: 4045-50 (2000)
- Elliott, RL; Kopecka, H; Gunn, DE; Lin, NH; Garvey, DS; Ryther, KB; Holladay, MW; Anderson, DJ; Campbell, JE; Sullivan, JP; Buckley, MJ; Gunther, KL; O'Neill, AB; Decker, MW; Arnerić, SP 2-(Aryloxymethyl) azacyclic analogues as novel nicotinic acetylcholine receptor (nAChR) ligands Bioorg Med Chem Lett 6: 2283-2288 (1996)
- Mukhin, AG; Gündisch, D; Horti, AG; Koren, AO; Tamagnan, G; Kimes, AS; Chambers, J; Vaupel, DB; King, SL; Picciotto, MR; Innis, RB; London, ED 5-Iodo-A-85380, an alpha4beta2 subtype-selective ligand for nicotinic acetylcholine receptors. Mol Pharmacol 57: 642-9 (2000)
- Hobbs, SH; Johnson, SJ; Kesten, SR; Pavia, MR; Davis, RE; Schwarz, RD; Coughenour, LL; Myers, SL; Dudley, DT; Moss, WH Cholinergic agents: 2-oxazolidinone analogues of the acetylcholine-receptor muscarinic agonist pilocarpine Bioorg Med Chem Lett 1: 147-150 (1991)
- German, N; Kim, JS; Jain, A; Dukat, M; Pandya, A; Ma, Y; Weltzin, M; Schulte, MK; Glennon, RA Deconstruction of thea4ß2 nicotinic acetylcholine receptor positive allosteric modulator desformylflustrabromine. J Med Chem 54: 7259-67 (2011)
- Gao, Y; Kellar, KJ; Yasuda, RP; Tran, T; Xiao, Y; Dannals, RF; Horti, AG Derivatives of dibenzothiophene for positron emission tomography imaging ofa7-nicotinic acetylcholine receptors. J Med Chem 56: 7574-89 (2013)
- Lainé, DI; Wan, Z; Yan, H; Zhu, C; Xie, H; Fu, W; Busch-Petersen, J; Neipp, C; Davis, R; Widdowson, KL; Blaney, FE; Foley, J; Bacon, AM; Webb, EF; Luttmann, MA; Burman, M; Sarau, HM; Salmon, M; Palovich, MR; Belmonte, K Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists. J Med Chem 52: 5241-52 (2010)
- Yu, R; Kompella, SN; Adams, DJ; Craik, DJ; Kaas, Q Determination of the ?-conotoxin Vc1.1 binding site on the ?9?10 nicotinic acetylcholine receptor. J Med Chem 56: 3557-67 (2013)
- Yang, Q; Lachapelle, EA; Kablaoui, NM; Webb, D; Popiolek, M; Grimwood, S; Kozak, R; O'Connor, RE; Lazzaro, JT; Butler, CR; Zhang, L Discovery of Selective M4 Muscarinic Acetylcholine Receptor Agonists with Novel Carbamate Isosteres. ACS Med Chem Lett 10: 941-948 (2019)
- Jin, J; Budzik, B; Wang, Y; Shi, D; Wang, F; Xie, H; Wan, Z; Zhu, C; Foley, JJ; Webb, EF; Berlanga, M; Burman, M; Sarau, HM; Morrow, DM; Moore, ML; Rivero, RA; Palovich, M; Salmon, M; Belmonte, KE; Lainé, DI Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists. J Med Chem 51: 5915-8 (2008)
- Lainé, DI; McCleland, B; Thomas, S; Neipp, C; Underwood, B; Dufour, J; Widdowson, KL; Palovich, MR; Blaney, FE; Foley, JJ; Webb, EF; Luttmann, MA; Burman, M; Belmonte, K; Salmon, M Discovery of novel 1-azoniabicyclo[2.2.2]octane muscarinic acetylcholine receptor antagonists. J Med Chem 52: 2493-505 (2009)
- Geitmann, M; Retra, K; de Kloe, GE; Homan, E; Smit, AB; de Esch, IJ; Danielson, UH Interaction kinetic and structural dynamic analysis of ligand binding to acetylcholine-binding protein. Biochemistry 49: 8143-54 (2010)
- Alptüzün, V; Prinz, M; Hörr, V; Scheiber, J; Radacki, K; Fallarero, A; Vuorela, P; Engels, B; Braunschweig, H; Erciyas, E; Holzgrabe, U Interaction of (benzylidene-hydrazono)-1,4-dihydropyridines with beta-amyloid, acetylcholine, and butyrylcholine esterases. Bioorg Med Chem 18: 2049-59 (2010)
- Hojahmat, M; Horton, DB; Norrholm, SD; Miller, DK; Grinevich, VP; Deaciuc, AG; Dwoskin, LP; Crooks, PA Lobeline esters as novel ligands for neuronal nicotinic acetylcholine receptors and neurotransmitter transporters. Bioorg Med Chem 18: 640-9 (2010)
- Budzik, B; Wang, Y; Shi, D; Wang, F; Xie, H; Wan, Z; Zhu, C; Foley, JJ; Nuthulaganti, P; Kallal, LA; Sarau, HM; Morrow, DM; Moore, ML; Rivero, RA; Palovich, M; Salmon, M; Belmonte, KE; Laine, DI; Jin, J M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines. Bioorg Med Chem Lett 19: 1686-90 (2009)
- Xu, R; Dwoskin, LP; Grinevich, VP; Deaciuc, G; Crooks, PA Neuronal nicotinic acetylcholine receptor binding affinities of boron-containing nicotine analogues. Bioorg Med Chem Lett 11: 1245-8 (2001)
- Jensen, AA; Frølund, B; Liljefors, T; Krogsgaard-Larsen, P Neuronal nicotinic acetylcholine receptors: structural revelations, target identifications, and therapeutic inspirations. J Med Chem 48: 4705-45 (2005)
- Gallagher, R; Qudah, T; Balle, T; Chebib, M; McLeod, MD Novel methyllycaconitine analogues selective for the ?4?2 over ?7 nicotinic acetylcholine receptors. Bioorg Med Chem 51: (2021)
- Kachel, HS; Franzyk, H; Mellor, IR Philanthotoxin Analogues That Selectively Inhibit Ganglionic Nicotinic Acetylcholine Receptors with Exceptional Potency. J Med Chem 62: 6214-6222 (2019)
- She, X; Pegoli, A; Gruber, CG; Wifling, D; Carpenter, J; H?bner, H; Chen, M; Wan, J; Bernhardt, G; Gmeiner, P; Holliday, ND; Keller, M Red-Emitting Dibenzodiazepinone Derivatives as Fluorescent Dualsteric Probes for the Muscarinic Acetylcholine M J Med Chem 63: 4133-4154 (2020)
- Mortell, KH; Schrimpf, MR; Bunnelle, WH; Anderson, DJ; Gronlien, JH; Hagene, KT; Gopalakrishnan, M Structure-activity relationships of N-substituted ligands for the alpha7 nicotinic acetylcholine receptor. Bioorg Med Chem Lett 20: 104-7 (2010)
- Crowley, BM; Bell, IM; Harvey, AJ; Campbell, BT; Greshock, TJ; Rada, VL Substituted 6-membered aryl or heteroaryl allosteric modulators of nicotinic acetylcholine receptors US Patent US11026958 (2021)
- Jepsen, TH; Jensen, AA; Lund, MH; Glibstrup, E; Kristensen, JL Synthesis and Pharmacological Evaluation of DH?E Analogues as Neuronal Nicotinic Acetylcholine Receptor Antagonists. ACS Med Chem Lett 5: 766-70 (2014)
- Wei, ZL; Xiao, Y; Kellar, KJ; Kozikowski, AP Synthesis and pharmacological characterization of bivalent ligands of epibatidine at neuronal nicotinic acetylcholine receptors. Bioorg Med Chem Lett 14: 1855-8 (2004)
- Lee, J; Davis, CB; Rivero, RA; Reitz, AB; Shank, RP Synthesis and structure-activity relationship of novel pyridyl ethers for the nicotinic acetylcholine receptor. Bioorg Med Chem Lett 10: 1063-6 (2000)
- Ivy Carroll, F; Ma, W; Navarro, HA; Abraham, P; Wolckenhauer, SA; Damaj, MI; Martin, BR Synthesis, nicotinic acetylcholine receptor binding, antinociceptive and seizure properties of methyllycaconitine analogs. Bioorg Med Chem 15: 678-85 (2006)
- Ussing, CA; Hansen, CP; Petersen, JG; Jensen, AA; Rohde, LA; Ahring, PK; Nielsen, E?; Kastrup, JS; Gajhede, M; Frølund, B; Balle, T Synthesis, pharmacology, and biostructural characterization of novela4ß2 nicotinic acetylcholine receptor agonists. J Med Chem 56: 940-51 (2013)
- Jin, Q; Davis, RS; Bullion, AM; Jin, J; Wang, Y; Widdowson, KL; Palovich, MR; Foley, JJ; Schmidt, DB; Buckley, PT; Webb, EF; Salmon, M; Belmonte, KE; Sarau, HM; Busch-Petersen, J Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups. Bioorg Med Chem Lett 22: 7087-91 (2012)
- de Kloe, GE; Retra, K; Geitmann, M; Källblad, P; Nahar, T; van Elk, R; Smit, AB; van Muijlwijk-Koezen, JE; Leurs, R; Irth, H; Danielson, UH; de Esch, IJ Surface plasmon resonance biosensor based fragment screening using acetylcholine binding protein identifies ligand efficiency hot spots (LE hot spots) by deconstruction of nicotinic acetylcholine receptora7 ligands. J Med Chem 53: 7192-201 (2010)
- Zlotos, DP; Buller, S; Tränkle, C; Mohr, K Bisquaternary caracurine V derivatives as allosteric modulators of ligand binding to M2 acetylcholine receptors. Bioorg Med Chem Lett 10: 2529-32 (2001)
- Pegoli, A; Wifling, D; Gruber, CG; She, X; H?bner, H; Bernhardt, G; Gmeiner, P; Keller, M Conjugation of Short Peptides to Dibenzodiazepinone-Type Muscarinic Acetylcholine Receptor Ligands Determines M J Med Chem 62: 5358-5369 (2019)
- Beinat, C; Banister, SD; van Prehn, S; Doddareddy, MR; Hibbs, D; Sako, M; Chebib, M; Tran, T; Al-Muhtasib, N; Xiao, Y; Kassiou, M Consequences of linker length alteration of thea7 nicotinic acetylcholine receptor (nAChR) agonist, SEN12333. Bioorg Med Chem Lett 22: 2380-4 (2012)
- Gruber, CG; Pegoli, A; M?ller, C; Gr?tz, L; She, X; Keller, M Differently fluorescence-labelled dibenzodiazepinone-type muscarinic acetylcholine receptor ligands with high M RSC Med Chem 11: 823-832 (2020)
- Bodnar, AL; Cortes-Burgos, LA; Cook, KK; Dinh, DM; Groppi, VE; Hajos, M; Higdon, NR; Hoffmann, WE; Hurst, RS; Myers, JK; Rogers, BN; Wall, TM; Wolfe, ML; Wong, E Discovery and structure-activity relationship of quinuclidine benzamides as agonists of alpha7 nicotinic acetylcholine receptors. J Med Chem 48: 905-8 (2005)
- Lainé, DI; Xie, H; Buffet, N; Foley, JJ; Buckley, P; Webb, EF; Widdowson, KL; Palovich, MR; Belmonte, KE Discovery of novel 8-azoniabicyclo[3.2.1]octane carbamates as muscarinic acetylcholine receptor antagonists. Bioorg Med Chem Lett 17: 6066-9 (2007)
- Wang, S; Zhu, X; Zhangsun, M; Wu, Y; Yu, J; Harvey, PJ; Kaas, Q; Zhangsun, D; Craik, DJ; Luo, S Engineered Conotoxin Differentially Blocks and Discriminates Rat and Human ?7 Nicotinic Acetylcholine Receptors. J Med Chem 64: 5620-5631 (2021)
- Acharya, R; Burnett, DA; Bursavich, MG; Cook, AS; Harrison, BA; Koenig, G; Mcriner, AJ Geminal substituted quinuclidine amide compounds as agonists of α-7 nicotonic acetylcholine receptors US Patent US10183938 (2019)
- Fitch, RW; Kaneko, Y; Klaperski, P; Daly, JW; Seitz, G; Gündisch, D Halogenated and isosteric cytisine derivatives with increased affinity and functional activity at nicotinic acetylcholine receptors. Bioorg Med Chem Lett 15: 1221-4 (2005)
- Mowrey, DD; Liu, Q; Bondarenko, V; Chen, Q; Seyoum, E; Xu, Y; Wu, J; Tang, P Insights into distinct modulation of a7 and a7ß2 nicotinic acetylcholine receptors by the volatile anesthetic isoflurane. J Biol Chem 288: 35793-800 (2013)
- Khan, IM; Yaksh, TL; Taylor, P Ligand specificity of nicotinic acetylcholine receptors in rat spinal cord: studies with nicotine and cytisine. J Pharmacol Exp Ther 270: 159-66 (1994)
- Gazzard, L; Williams, K; Chen, H; Axford, L; Blackwood, E; Burton, B; Chapman, K; Crackett, P; Drobnick, J; Ellwood, C; Epler, J; Flagella, M; Gancia, E; Gill, M; Goodacre, S; Halladay, J; Hewitt, J; Hunt, H; Kintz, S; Lyssikatos, J; Macleod, C; Major, S; M?dard, G; Narukulla, R; Ramiscal, J; Schmidt, S; Seward, E; Wiesmann, C; Wu, P; Yee, S; Yen, I; Malek, S Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1. J Med Chem 58: 5053-74 (2015)
- Del Bello, F; Bonifazi, A; Giorgioni, G; Petrelli, R; Quaglia, W; Altomare, A; Falcicchio, A; Matucci, R; Vistoli, G; Piergentili, A Novel muscarinic acetylcholine receptor hybrid ligands embedding quinuclidine and 1,4-dioxane fragments. Eur J Med Chem 137: 327-337 (2017)
- Mazurov, AA; Kombo, DC; Akireddy, S; Murthy, S; Hauser, TA; Jordan, KG; Gatto, GJ; Yohannes, D Novel nicotinic acetylcholine receptor agonists containing carbonyl moiety as a hydrogen bond acceptor. Bioorg Med Chem Lett 23: 3927-34 (2013)
- Bourdin, CM; Lebreton, J; Math?-Allainmat, M; Thany, SH Pharmacological profile of zacopride and new quaternarized fluorobenzamide analogues on mammaliana7 nicotinic acetylcholine receptor. Bioorg Med Chem Lett 25: 3184-8 (2015)
- Sippy, KB; Anderson, DJ; Bunnelle, WH; Hutchins, CW; Schrimpf, MR Preparation and characterization of N-(3-pyridinyl) spirocyclic diamines as ligands for nicotinic acetylcholine receptors. Bioorg Med Chem Lett 19: 1682-5 (2009)
- Quadri, M; Stokes, C; Gulsevin, A; Felts, ACJ; Abboud, KA; Papke, RL; Horenstein, NA Sulfonium as a Surrogate for Ammonium: A New?7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity. J Med Chem 60: 7928-7934 (2017)
- Lewis, LM; Sheffler, D; Williams, R; Bridges, TM; Kennedy, JP; Brogan, JT; Mulder, MJ; Williams, L; Nalywajko, NT; Niswender, CM; Weaver, CD; Conn, PJ; Lindsley, CW Synthesis and SAR of selective muscarinic acetylcholine receptor subtype 1 (M1 mAChR) antagonists. Bioorg Med Chem Lett 18: 885-90 (2008)
- Jin, Z; Khan, P; Shin, Y; Wang, J; Lin, L; Cameron, MD; Lindstrom, JM; Kenny, PJ; Kamenecka, TM Synthesis and activity of substituted heteroaromatics as positive allosteric modulators fora4ß2a5 nicotinic acetylcholine receptors. Bioorg Med Chem Lett 24: 674-8 (2014)
- Tu, Z; Zhang, X; Jin, H; Yue, X; Padakanti, PK; Yu, L; Liu, H; Flores, HP; Kaneshige, K; Parsons, SM; Perlmutter, JS Synthesis and biological characterization of a promising F-18 PET tracer for vesicular acetylcholine transporter. Bioorg Med Chem 23: 4699-709 (2015)
- Huang, M; Suk, DH; Cho, NC; Bhattarai, D; Kang, SB; Kim, Y; Pae, AN; Rhim, H; Keum, G Synthesis and biological evaluation of isoxazoline derivatives as potent M1 muscarinic acetylcholine receptor agonists. Bioorg Med Chem Lett 25: 1546-51 (2015)
- Efange, SM; Khare, AB; von Hohenberg, K; Mach, RH; Parsons, SM; Tu, Z Synthesis and in vitro biological evaluation of carbonyl group-containing inhibitors of vesicular acetylcholine transporter. J Med Chem 53: 2825-35 (2010)
- Carroll, FI; Robinson, TP; Brieaddy, LE; Atkinson, RN; Mascarella, SW; Damaj, MI; Martin, BR; Navarro, HA Synthesis and nicotinic acetylcholine receptor binding properties of bridged and fused ring analogues of epibatidine. J Med Chem 50: 6383-91 (2007)
- Carroll, FI; Hu, X; Navarro, HA; Deschamps, J; Abdrakhmanova, GR; Damaj, MI; Martin, BR Synthesis and pharmacological characterization of nicotinic acetylcholine receptor properties of (+)- and (-)-pyrido-[3,4-b]homotropanes. J Med Chem 49: 3244-50 (2006)
- Sharples, CG; Karig, G; Simpson, GL; Spencer, JA; Wright, E; Millar, NS; Wonnacott, S; Gallagher, T Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165. J Med Chem 45: 3235-45 (2002)
- Murineddu, G; Murruzzu, C; Curzu, MM; Chelucci, G; Gotti, C; Gaimarri, A; Legnani, L; Toma, L; Pinna, GA Synthesis of 3,6-diazabicyclo[3.1.1]heptanes as novel ligands for neuronal nicotinic acetylcholine receptors. Bioorg Med Chem Lett 18: 6147-50 (2008)
- Wei, ZL; Petukhov, PA; Xiao, Y; T?ckmantel, W; George, C; Kellar, KJ; Kozikowski, AP Synthesis, nicotinic acetylcholine receptor binding affinities, and molecular modeling of constrained epibatidine analogues. J Med Chem 46: 921-4 (2003)
- Petersen, IN; Crestey, F; Jensen, AA; Indurthi, DC; Pedersen, H; Andreasen, JT; Balle, T; Kristensen, JL Tying up Nicotine: New Selective Competitive Antagonist of the Neuronal Nicotinic Acetylcholine Receptors. ACS Med Chem Lett 6: 472-5 (2015)
- Wu, Y; Zhangsun, D; Zhu, X; Kaas, Q; Zhangsun, M; Harvey, PJ; Craik, DJ; McIntosh, JM; Luo, S a-Conotoxin [S9A]TxID Potently Discriminates betweena3ß4 anda6/a3ß4 Nicotinic Acetylcholine Receptors. J Med Chem 60: 5826-5833 (2017)
- Kagabu, S; Maienfisch, P; Zhang, A; Granda-Minones, J; Haettenschwiler, J; Kayser, H; Maetzke, T; Casida, JE 5-Azidoimidacloprid and an acyclic analogue as candidate photoaffinity probes for mammalian and insect nicotinic acetylcholine receptors. J Med Chem 43: 5003-9 (2001)
- Choi, KI; Cha, JH; Cho, YS; Pae, AN; Jin, C; Yook, J; Cheon, HG; Jeong, D; Kong, JY; Koh, HY Binding affinities of 3-(3-phenylisoxazol-5-yl)methylidene-1-azabicycles to acetylcholine receptors. Bioorg Med Chem Lett 9: 2795-800 (1999)
- Bannon, AW; Decker, MW; Holladay, MW; Curzon, P; Donnelly-Roberts, D; Puttfarcken, PS; Bitner, RS; Diaz, A; Dickenson, AH; Porsolt, RD; Williams, M; Arneric, SP Broad-spectrum, non-opioid analgesic activity by selective modulation of neuronal nicotinic acetylcholine receptors. Science 279: 77-81 (1998)
- Balsera, B; Mulet, J; Fern?ndez-Carvajal, A; de la Torre-Mart?nez, R; Ferrer-Montiel, A; Hern?ndez-Jim?nez, JG; Est?vez-Herrera, J; Borges, R; Freitas, AE; L?pez, MG; Garc?a-L?pez, MT; Gonz?lez-Mu?iz, R; P?rez de Vega, MJ; Valor, LM; Svobodov?, L; Sala, S; Sala, F; Criado, M Chalcones as positive allosteric modulators ofa7 nicotinic acetylcholine receptors: a new target for a privileged structure. Eur J Med Chem 86: 724-39 (2014)
- de la Fuente Revenga, M; Balle, T; Jensen, AA; Fr?lund, B Conformationally restrained carbamoylcholine homologues. Synthesis, pharmacology at neuronal nicotinic acetylcholine receptors and biostructural considerations. Eur J Med Chem 102: 352-62 (2015)
- Melancon, BJ; Gogliotti, RD; Tarr, JC; Saleh, SA; Chauder, BA; Lebois, EP; Cho, HP; Utley, TJ; Sheffler, DJ; Bridges, TM; Morrison, RD; Daniels, JS; Niswender, CM; Conn, PJ; Lindsley, CW; Wood, MR Continued optimization of the MLPCN probe ML071 into highly potent agonists of the hM1 muscarinic acetylcholine receptor. Bioorg Med Chem Lett 22: 3467-72 (2012)
- Lainé, DI; Yan, H; Xie, H; Davis, RS; Dufour, J; Widdowson, KL; Palovich, MR; Wan, Z; Foley, JJ; Schmidt, DB; Hunsberger, GE; Burman, M; Bacon, AM; Webb, EF; Luttmann, MA; Salmon, M; Sarau, HM; Umbrecht, ST; Landis, PS; Peck, BJ; Busch-Petersen, J Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists. Bioorg Med Chem Lett 22: 3366-9 (2012)
- Disingrini, T; Muth, M; Dallanoce, C; Barocelli, E; Bertoni, S; Kellershohn, K; Mohr, K; De Amici, M; Holzgrabe, U Design, synthesis, and action of oxotremorine-related hybrid-type allosteric modulators of muscarinic acetylcholine receptors. J Med Chem 49: 366-72 (2006)
- Crestey, F; Jensen, AA; Borch, M; Andreasen, JT; Andersen, J; Balle, T; Kristensen, JL Design, synthesis, and biological evaluation of Erythrina alkaloid analogues as neuronal nicotinic acetylcholine receptor antagonists. J Med Chem 56: 9673-82 (2014)
- Liang, J; Tae, HS; Xu, X; Jiang, T; Adams, DJ; Yu, R Dimerization of ?-Conotoxins as a Strategy to Enhance the Inhibition of the Human ?7 and ?9?10 Nicotinic Acetylcholine Receptors. J Med Chem 63: 2974-2985 (2020)
- PubChem, PC Discovery of Novel Allosteric Modulators of the Muscarinic Receptor M5: [3H]N-methylscopolamine Competition with Acetylcholine PubChem Bioassay (2009)
- Spearing, PK; Cho, HP; Luscombe, VB; Blobaum, AL; Boutaud, O; Engers, DW; Rodriguez, AL; Niswender, CM; Jeffrey Conn, P; Lindsley, CW; Bender, AM Discovery of a novel class of heteroaryl-pyrrolidinones as positive allosteric modulators of the muscarinic acetylcholine receptor M Bioorg Med Chem Lett 47: (2021)
- Ledneczki, I; Tapolcs?nyi, P; G?bor, E; Visegr?dy, A; Vass, M; ?les, J; Holm, P; Horv?th, A; Pocsai, A; Mah?, S; Greiner, I; Kr?mos, B; B?ni, Z; K?ti, J; K?ncz, AE; Th?n, M; Kolok, S; Laszy, J; Bal?zs, O; Bugovits, G; Nagy, J; Vastag, M; Sz?jli, ?; Boz?, ?; L?vay, G; Lendvai, B; N?methy, Z Discovery of novel positive allosteric modulators of the ?7 nicotinic acetylcholine receptor: Scaffold hopping approach. Eur J Med Chem 214: (2021)
- Huang, Y; Zhu, Z; Xiao, Y; Laruelle, M Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors. Bioorg Med Chem Lett 15: 4385-8 (2005)
- Ledneczki, I; Horv?th, A; Tapolcs?nyi, P; ?les, J; Moln?r, KD; V?g?, I; Visegr?dy, A; Kiss, L; Szigetv?ri, ?; K?ti, J; Kr?mos, B; Mah?, S; Holm, P; Kolok, S; Fodor, L; Th?n, M; Kostyalik, D; Bal?zs, O; Vastag, M; Greiner, I; L?vay, G; Lendvai, B; N?methy, Z HTS-based discovery and optimization of novel positive allosteric modulators of the ?7 nicotinic acetylcholine receptor. Eur J Med Chem 222: (2021)
- Zhang, A; Kayser, H; Maienfisch, P; Casida, JE Insect nicotinic acetylcholine receptor: conserved neonicotinoid specificity of [(3)H]imidacloprid binding site. J Neurochem 75: 1294-303 (2000)
- Chen, J; Norrholm, S; Dwoskin, LP; Crooks, PA; Bai, D N,N-disubstituted piperazines: synthesis and affinities at alpha4beta2(*) and alpha7(*) neuronal nicotinic acetylcholine receptors. Bioorg Med Chem Lett 13: 97-100 (2002)
- Sabnis, RW Novel Spiropiperidine Allosteric Modulators of Nicotinic Acetylcholine Receptors for Treating Central Nervous System Disorders. ACS Med Chem Lett 12: 1866-1867 (2021)
- Latli, B; D'Amour, K; Casida, JE Novel and potent 6-chloro-3-pyridinyl ligands for the alpha4beta2 neuronal nicotinic acetylcholine receptor. J Med Chem 42: 2227-34 (1999)
- Rotella, DP Substituted Benzylspiroindolin-2-one Analogues as Positive Allosteric Modulators of the Muscarinic Acetylcholine Receptor M1. ACS Med Chem Lett 4: (2013)
- Kozaka, T; Uno, I; Kitamura, Y; Miwa, D; Ogawa, K; Shiba, K Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT). Bioorg Med Chem 20: 4936-41 (2012)
- Tu, Z; Wang, W; Cui, J; Zhang, X; Lu, X; Xu, J; Parsons, SM Synthesis and evaluation of in vitro bioactivity for vesicular acetylcholine transporter inhibitors containing two carbonyl groups. Bioorg Med Chem 20: 4422-9 (2012)
- Kane, BE; Grant, MK; El-Fakahany, EE; Ferguson, DM Synthesis and evaluation of xanomeline analogs--probing the wash-resistant phenomenon at the M1 muscarinic acetylcholine receptor. Bioorg Med Chem 16: 1376-92 (2008)
- Assaad, T; Mavel, S; Parsons, SM; Kruse, S; Galineau, L; Allouchi, H; Kassiou, M; Chalon, S; Guilloteau, D; Emond, P Synthesis and in vitro evaluation of N-substituted aza-trozamicol analogs as vesicular acetylcholine transporter ligands. Bioorg Med Chem Lett 16: 2654-7 (2006)
- Liu, Y; Paige, M; Olson, TT; Al-Muhtasib, N; Xie, T; Hou, S; White, MP; Cordova, A; Guo, JL; Kellar, KJ; Xiao, Y; Brown, ML Synthesis and pharmacological characterization of new neuronal nicotinic acetylcholine receptor ligands derived from Sazetidine-A. Bioorg Med Chem Lett 24: 2954-6 (2014)
- Sarasamkan, J; Scheunemann, M; Apaijai, N; Palee, S; Parichatikanond, W; Arunrungvichian, K; Fischer, S; Chattipakorn, S; Deuther-Conrad, W; Sch??rmann, G; Brust, P; Vajragupta, O Varying Chirality Across Nicotinic Acetylcholine Receptor Subtypes: Selective Binding of Quinuclidine Triazole Compounds. ACS Med Chem Lett 7: 890-895 (2016)
- Efange, SM; Michelson, RH; Dutta, AK; Parsons, SM Acyclic analogues of 2-(4-phenylpiperidino)cyclohexanol (vesamicol): conformationally mobile inhibitors of vesicular acetylcholine transport. J Med Chem 34: 2638-43 (1991)
- Whiteaker, P; Sharples, CG; Wonnacott, S Agonist-induced up-regulation of alpha4beta2 nicotinic acetylcholine receptors in M10 cells: pharmacological and spatial definition. Mol Pharmacol 53: 950-62 (1998)
- Bräuner-Osborne, H; Ebert, B; Brann, MR; Falch, E; Krogsgaard-Larsen, P Annulated heterocyclic bioisosteres of norarecoline. Synthesis and molecular pharmacology at five recombinant human muscarinic acetylcholine receptors. J Med Chem 38: 2188-95 (1995)
- Hansen, CP; Jensen, AA; Balle, T; Bitsch-Jensen, K; Hassan, MM; Liljefors, T; Frølund, B Carbamoylcholine analogs as nicotinic acetylcholine receptor agonists--structural modifications of 3-(dimethylamino)butyl dimethylcarbamate (DMABC). Bioorg Med Chem Lett 19: 87-91 (2008)
- Luo, S; Zhangsun, D; Zhu, X; Wu, Y; Hu, Y; Christensen, S; Harvey, PJ; Akcan, M; Craik, DJ; McIntosh, JM Characterization of a novela-conotoxin TxID from Conus textile that potently blocks rata3ß4 nicotinic acetylcholine receptors. J Med Chem 56: 9655-63 (2014)
- Ullrich, T; Krich, S; Binder, D; Mereiter, K; Anderson, DJ; Meyer, MD; Pyerin, M Conformationally constrained nicotines: polycyclic, bridged, and spiro-annulated analogues as novel ligands for the nicotinic acetylcholine receptor. J Med Chem 45: 4047-54 (2002)
- Yenugonda, VM; Xiao, Y; Levin, ED; Rezvani, AH; Tran, T; Al-Muhtasib, N; Sahibzada, N; Xie, T; Wells, C; Slade, S; Johnson, JE; Dakshanamurthy, S; Kong, HS; Tomita, Y; Liu, Y; Paige, M; Kellar, KJ; Brown, ML Design, synthesis and discovery of picomolar selective α4β2 nicotinic acetylcholine receptor ligands. J Med Chem 56: 8404-21 (2013)
- Albrecht, BK; Berry, V; Boezio, AA; Cao, L; Clarkin, K; Guo, W; Harmange, JC; Hierl, M; Huang, L; Janosky, B; Knop, J; Malmberg, A; McDermott, JS; Nguyen, HQ; Springer, SK; Waldon, D; Woodin, K; McDonough, SI Discovery and optimization of substituted piperidines as potent, selective, CNS-penetrant alpha4beta2 nicotinic acetylcholine receptor potentiators. Bioorg Med Chem Lett 18: 5209-12 (2008)
- Chang, YP; Banerjee, J; Dowell, C; Wu, J; Gyanda, R; Houghten, RA; Toll, L; McIntosh, JM; Armishaw, CJ Discovery of a potent and selectivea3ß4 nicotinic acetylcholine receptor antagonist from ana-conotoxin synthetic combinatorial library. J Med Chem 57: 3511-21 (2014)
- Liu, J; Yu, LF; Eaton, JB; Caldarone, B; Cavino, K; Ruiz, C; Terry, M; Fedolak, A; Wang, D; Ghavami, A; Lowe, DA; Brunner, D; Lukas, RJ; Kozikowski, AP Discovery of isoxazole analogues of sazetidine-A as selectivea4ß2-nicotinic acetylcholine receptor partial agonists for the treatment of depression. J Med Chem 54: 7280-8 (2011)
- Hughes, AD; Chin, KH; Dunham, SL; Jasper, JR; King, KE; Lee, TW; Mammen, M; Martin, J; Steinfeld, T Discovery of muscarinic acetylcholine receptor antagonist and beta 2 adrenoceptor agonist (MABA) dual pharmacology molecules. Bioorg Med Chem Lett 21: 1354-8 (2011)
- Sumiyoshi, T; Enomoto, T; Takai, K; Takahashi, Y; Konishi, Y; Uruno, Y; Tojo, K; Suwa, A; Matsuda, H; Nakako, T; Sakai, M; Kitamura, A; Uematsu, Y; Kiyoshi, A Discovery of novel N-substituted oxindoles as selective m1 and m4 muscarinic acetylcholine receptors partial agonists. ACS Med Chem Lett 4: 244-8 (2013)
- Kombo, DC; Mazurov, AA; Chewning, J; Hammond, PS; Tallapragada, K; Hauser, TA; Speake, J; Yohannes, D; Caldwell, WS Discovery of novela7 nicotinic acetylcholine receptor ligands via pharmacophoric and docking studies of benzylidene anabaseine analogs. Bioorg Med Chem Lett 22: 1179-86 (2012)
- Akincioglu, A; Akincioglu, H; G?l?in, I; Durdagi, S; Supuran, CT; G?ksu, S Discovery of potent carbonic anhydrase and acetylcholine esterase inhibitors: novel sulfamoylcarbamates and sulfamides derived from acetophenones. Bioorg Med Chem 23: 3592-602 (2015)
- Enz, A; Feuerbach, D; Frederiksen, MU; Gentsch, C; Hurth, K; Müller, W; Nozulak, J; Roy, BL Gamma-lactams--a novel scaffold for highly potent and selective alpha 7 nicotinic acetylcholine receptor agonists. Bioorg Med Chem Lett 19: 1287-91 (2009)
- Bisson, WH; Scapozza, L; Westera, G; Mu, L; Schubiger, PA Ligand selectivity for the acetylcholine binding site of the rat alpha4beta2 and alpha3beta4 nicotinic subtypes investigated by molecular docking. J Med Chem 48: 5123-30 (2005)
- Carroll, FI; Blough, BE; Mascarella, SW; Navarro, HA; Eaton, JB; Lukas, RJ; Damaj, MI Nicotinic Acetylcholine Receptor Efficacy and Pharmacological Properties of 3-(Substituted phenyl)-2ß-substituted Tropanes. J Med Chem 53: 8345-53 (2010)
- Nielsen, SF; Nielsen, EO; Olsen, GM; Liljefors, T; Peters, D Novel potent ligands for the central nicotinic acetylcholine receptor: synthesis, receptor binding, and 3D-QSAR analysis. J Med Chem 43: 2217-26 (2000)
- Zaveri, N; Jiang, F; Olsen, C; Polgar, W; Toll, L Novela3ß4 nicotinic acetylcholine receptor-selective ligands. Discovery, structure-activity studies, and pharmacological evaluation. J Med Chem 53: 8187-91 (2010)
- Rötering, S; Scheunemann, M; Fischer, S; Hiller, A; Peters, D; Deuther-Conrad, W; Brust, P Radiosynthesis and first evaluation in mice of [(18)F]NS14490 for molecular imaging ofa7 nicotinic acetylcholine receptors. Bioorg Med Chem 21: 2635-42 (2013)
- Haydar, SN; Ghiron, C; Bettinetti, L; Bothmann, H; Comery, TA; Dunlop, J; La Rosa, S; Micco, I; Pollastrini, M; Quinn, J; Roncarati, R; Scali, C; Valacchi, M; Varrone, M; Zanaletti, R SAR and biological evaluation of SEN12333/WAY-317538: Novel alpha 7 nicotinic acetylcholine receptor agonist. Bioorg Med Chem 17: 5247-58 (2009)
- Almeida, LE; Pereira, EF; Camara, AL; Maelicke, A; Albuquerque, EX Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation. Bioorg Med Chem Lett 14: 1879-87 (2004)
- Wang, X; Xiao, H; Wang, J; Huang, Z; Peng, G; Xie, W; Bian, X; Liu, H; Shi, C; Yang, T; Li, X; Gao, J; Meng, Y; Jiang, Q; Chen, W; Hu, F; Wei, N; Wang, X; Zhang, L; Wang, K; Sun, Q Synthesis and Biological Evaluation of Novel Triazine Derivatives as Positive Allosteric Modulators of ?7 Nicotinic Acetylcholine Receptors. J Med Chem 64: 12379-12396 (2021)
- Simoni, D; Rondanin, R; Marchetti, P; Rullo, C; Baruchello, R; Grisolia, G; Barbato, G; Giovannini, R; Marchioro, C; Capelli, AM; Virginio, C; Bozzoli, A; Borea, PA; Merighi, S; Donati, D Synthesis and biological activity of a novel class nicotinic acetylcholine receptors (nAChRs) ligands structurally related to anatoxin-a. Bioorg Med Chem Lett 21: 5423-7 (2011)
- Toyooka, N; Kobayashi, S; Zhou, D; Tsuneki, H; Wada, T; Sakai, H; Nemoto, H; Sasaoka, T; Garraffo, HM; Spande, TF; Daly, JW Synthesis of poison-frog alkaloids 233A, 235U, and 251AA and their inhibitory effects on neuronal nicotinic acetylcholine receptors. Bioorg Med Chem Lett 17: 5872-5 (2007)
- Tasso, B; Canu Boido, C; Terranova, E; Gotti, C; Riganti, L; Clementi, F; Artali, R; Bombieri, G; Meneghetti, F; Sparatore, F Synthesis, binding, and modeling studies of new cytisine derivatives, as ligands for neuronal nicotinic acetylcholine receptor subtypes. J Med Chem 52: 4345-57 (2009)
- Ivy Carroll, F; Yokota, Y; Ma, W; Lee, JR; Brieaddy, LE; Burgess, JP; Navarro, HA; Damaj, MI; Martin, BR Synthesis, nicotinic acetylcholine receptor binding, and pharmacological properties of 3'-(substituted phenyl)deschloroepibatidine analogs. Bioorg Med Chem 16: 746-54 (2008)
- Yamauchi, JG; Gomez, K; Grimster, N; Dufouil, M; Nemecz, A; Fotsing, JR; Ho, K; Talley, TT; Sharpless, K; Fokin, VV; Taylor, P Synthesizing Selective Agonists for the ?7 Nicotinic Receptor with in situ Click-Chemistry on Acetylcholine Binding Protein Templates. Mol Pharmacol 82: 687-699 (2014)
- Zheng, N; Christensen, SB; Blakely, A; Dowell, C; Purushottam, L; McIntosh, JM; Chou, DH Development of Conformationally Constrained ?-RgIA Analogues as Stable Peptide Antagonists of Human ?9?10 Nicotinic Acetylcholine Receptors. J Med Chem 63: 8380-8387 (2020)
- Lindemann, M; Deuther-Conrad, W; Moldovan, R; Sekhar, KVGC; Brust, P; Wenzel, B Do spiroindolines have the potential to replace vesamicol as lead compound for the development of radioligands targeting the vesicular acetylcholine transporter? Bioorg Med Chem 25: 5107-5113 (2017)
- Raasch, A; Scharfenstein, O; Tr?nkle, C; Holzgrabe, U; Mohr, K Elevation of ligand binding to muscarinic M(2) acetylcholine receptors by bis(ammonio)alkane-type allosteric modulators. J Med Chem 45: 3809-12 (2002)
- Rizzi, L; Dallanoce, C; Matera, C; Magrone, P; Pucci, L; Gotti, C; Clementi, F; De Amici, M Epiboxidine and novel-related analogues: a convenient synthetic approach and estimation of their affinity at neuronal nicotinic acetylcholine receptor subtypes. Bioorg Med Chem Lett 18: 4651-4 (2008)
- Matera, C; Quadri, M; Sciaccaluga, M; Pom?, DY; Fasoli, F; De Amici, M; Fucile, S; Gotti, C; Dallanoce, C; Grazioso, G Modification of the anabaseine pyridine nucleus allows achieving binding and functional selectivity for thea3ß4 nicotinic acetylcholine receptor subtype. Eur J Med Chem 108: 392-405 (2016)
- Yu, R; Tae, HS; Tabassum, N; Shi, J; Jiang, T; Adams, DJ Molecular Determinants Conferring the Stoichiometric-Dependent Activity of ?-Conotoxins at the Human ?9?10 Nicotinic Acetylcholine Receptor Subtype. J Med Chem 61: 4628-4634 (2018)
- Audouze, K; Nielsen, E?; Olsen, GM; Ahring, P; J?rgensen, TD; Peters, D; Liljefors, T; Balle, T New ligands with affinity for the alpha4beta2 subtype of nicotinic acetylcholine receptors. Synthesis, receptor binding, and 3D-QSAR modeling. J Med Chem 49: 3159-71 (2006)
- Dallanoce, C; Frigerio, F; Grazioso, G; Matera, C; Visconti, GL; De Amici, M; Pucci, L; Pistillo, F; Fucile, S; Gotti, C; Clementi, F; De Micheli, C New spirocyclic¿²-isoxazoline derivatives related to selective agonists ofa7 neuronal nicotinic acetylcholine receptors. Eur J Med Chem 46: 5790-9 (2011)
- Barthel, C; Sorger, D; Deuther-Conrad, W; Scheunemann, M; Schweiger, S; J?ckel, P; Roghani, A; Steinbach, J; Sch??rmann, G; Sabri, O; Brust, P; Wenzel, B New systematically modified vesamicol analogs and their affinity and selectivity for the vesicular acetylcholine transporter - A critical examination of the lead structure. Eur J Med Chem 100: 50-67 (2015)
- Jensen, AA; Zlotos, DP; Liljefors, T Pharmacological characteristics and binding modes of caracurine V analogues and related compounds at the neuronal alpha7 nicotinic acetylcholine receptor. J Med Chem 50: 4616-29 (2007)
- Kombo, DC; Hauser, TA; Grinevich, VP; Melvin, MS; Strachan, JP; Sidach, SS; Chewning, J; Fedorov, N; Tallapragada, K; Breining, SR; Miller, CH Pharmacological properties and predicted binding mode of arylmethylene quinuclidine-like derivatives at the ?3?4 nicotinic acetylcholine receptor (nAChR). Bioorg Med Chem Lett 23: 1450-5 (2013)
- Yu, J; Zhu, X; Harvey, PJ; Kaas, Q; Zhangsun, D; Craik, DJ; Luo, S Single Amino Acid Substitution in ?-Conotoxin TxID Reveals a Specific ?3?4 Nicotinic Acetylcholine Receptor Antagonist. J Med Chem 61: 9256-9265 (2018)
- Strømgaard, K; Mellor, IR; Andersen, K; Neagoe, I; Pluteanu, F; Usherwood, PN; Krogsgaard-Larsen, P; Jaroszewski, JW Solid-phase synthesis and pharmacological evaluation of analogues of PhTX-12-A potent and selective nicotinic acetylcholine receptor antagonist. Bioorg Med Chem Lett 12: 1159-62 (2002)
- Gopalakrishnan, M; Monteggia, LM; Anderson, DJ; Molinari, EJ; Piattoni-Kaplan, M; Donnelly-Roberts, D; Arneric, SP; Sullivan, JP Stable expression, pharmacologic properties and regulation of the human neuronal nicotinic acetylcholine alpha 4 beta 2 receptor. J Pharmacol Exp Ther 276: 289-97 (1996)
- Cheng, J; Zhang, C; Stevens, ED; Izenwasser, S; Wade, D; Chen, S; Paul, D; Trudell, ML Synthesis and biological evaluation at nicotinic acetylcholine receptors of N-arylalkyl- and N-aryl-7-azabicyclo[2.2.1]heptanes. J Med Chem 45: 3041-7 (2002)
- Zhang, HK; Eaton, JB; Fedolak, A; Gunosewoyo, H; Onajole, OK; Brunner, D; Lukas, RJ; Yu, LF; Kozikowski, AP Synthesis and biological evaluation of novel hybrids of highly potent and selectivea4ß2-Nicotinic acetylcholine receptor (nAChR) partial agonists. Eur J Med Chem 124: 689-697 (2016)
- Frost, JM; Bunnelle, WH; Tietje, KR; Anderson, DJ; Rueter, LE; Curzon, P; Surowy, CS; Ji, J; Daanen, JF; Kohlhaas, KL; Buckley, MJ; Henry, RF; Dyhring, T; Ahring, PK; Meyer, MD Synthesis and structure-activity relationships of 3,8-diazabicyclo[4.2.0]octane ligands, potent nicotinic acetylcholine receptor agonists. J Med Chem 49: 7843-53 (2006)
- Skaddan, MB; Kilbourn, MR; Snyder, SE; Sherman, PS; Desmond, TJ; Frey, KA Synthesis, (18)F-labeling, and biological evaluation of piperidyl and pyrrolidyl benzilates as in vivo ligands for muscarinic acetylcholine receptors. J Med Chem 43: 4552-62 (2000)
- Carroll, FI; Ma, W; Yokota, Y; Lee, JR; Brieaddy, LE; Navarro, HA; Damaj, MI; Martin, BR Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-substituted deschloroepibatidine analogues. Novel nicotinic antagonists. J Med Chem 48: 1221-8 (2005)
- Ondachi, PW; Ye, Z; Castro, AH; Luetje, CW; Damaj, MI; Mascarella, SW; Navarro, HA; Carroll, FI Synthesis, nicotinic acetylcholine receptor binding, in vitro and in vivo pharmacology properties of 3'-(substituted pyridinyl)-deschloroepibatidine analogs. Bioorg Med Chem 23: 5693-701 (2015)
- Gohlke, H; Schwarz, S; G?ndisch, D; Tilotta, MC; Weber, A; Wegge, T; Seitz, G 3D QSAR analyses-guided rational design of novel ligands for the (alpha4)2(beta2)3 nicotinic acetylcholine receptor. J Med Chem 46: 2031-48 (2003)
- Kovac, M; Mavel, S; Deuther-Conrad, W; Méheux, N; Glöckner, J; Wenzel, B; Anderluh, M; Brust, P; Guilloteau, D; Emond, P 3D QSAR study, synthesis, and in vitro evaluation of (+)-5-FBVM as potential PET radioligand for the vesicular acetylcholine transporter (VAChT). Bioorg Med Chem 18: 7659-67 (2010)
- Akdemir, A; Rucktooa, P; Jongejan, A; Elk, R; Bertrand, S; Sixma, TK; Bertrand, D; Smit, AB; Leurs, R; de Graaf, C; de Esch, IJ Acetylcholine binding protein (AChBP) as template for hierarchical in silico screening procedures to identify structurally novel ligands for the nicotinic receptors. Bioorg Med Chem 19: 6107-19 (2011)
- Nassif-Makki, T; Tränkle, C; Zlotos, D; Bejeuhr, G; Cambareri, A; Pfletschinger, C; Kostenis, E; Mohr, K; Holzgrabe, U Bisquaternary ligands of the common allosteric site of M2 acetylcholine receptors: search for the minimum essential distances between the pharmacophoric elements. J Med Chem 42: 849-58 (1999)
- Hone, AJ; Kaas, Q; Kearns, I; Hararah, F; Gajewiak, J; Christensen, S; Craik, DJ; McIntosh, JM Computational and Functional Mapping of Human and Rat ?6?4 Nicotinic Acetylcholine Receptors Reveals Species-Specific Ligand-Binding Motifs. J Med Chem 64: 1685-1700 (2021)
- Deligia, F; Deiana, V; Gotti, C; Lazzari, P; Bottazzi, ME; Pucci, L; Fasoli, F; Ragusa, G; Pinna, GA; Murineddu, G Design of novel 3,6-diazabicyclo[3.1.1]heptane derivatives with potent and selective affinities fora4ß2 neuronal nicotinic acetylcholine receptors. Eur J Med Chem 103: 429-37 (2015)
- Uruno, Y; Konishi, Y; Suwa, A; Takai, K; Tojo, K; Nakako, T; Sakai, M; Enomoto, T; Matsuda, H; Kitamura, A; Sumiyoshi, T Discovery of dihydroquinazolinone derivatives as potent, selective, and CNS-penetrant M(1) and M(4) muscarinic acetylcholine receptors agonists. Bioorg Med Chem Lett 25: 5357-61 (2015)
- Bolchi, C; Bavo, F; Gotti, C; Fumagalli, L; Fasoli, F; Binda, M; Mucchietto, V; Sciaccaluga, M; Plutino, S; Fucile, S; Pallavicini, M From pyrrolidinyl-benzodioxane to pyrrolidinyl-pyridodioxanes, or from unselective antagonism to selective partial agonism at?4?2 nicotinic acetylcholine receptor. Eur J Med Chem 125: 1132-1144 (2017)
- Zhu, X; Pan, S; Xu, M; Zhang, L; Yu, J; Yu, J; Wu, Y; Fan, Y; Li, H; Kasheverov, IE; Kudryavtsev, DS; Tsetlin, VI; Xue, Y; Zhangsun, D; Wang, X; Luo, S High Selectivity of an ?-Conotoxin LvIA Analogue for ?3?2 Nicotinic Acetylcholine Receptors Is Mediated by ?2 Functionally Important Residues. J Med Chem 63: 13656-13668 (2020)
- Huang, X; Zheng, F; Stokes, C; Papke, RL; Zhan, CG Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding. J Med Chem 51: 6293-302 (2008)
- Bolchi, C; Bavo, F; Fumagalli, L; Gotti, C; Fasoli, F; Moretti, M; Pallavicini, M Novel 5-substituted 3-hydroxyphenyl and 3-nitrophenyl ethers of S-prolinol asa4ß2-nicotinic acetylcholine receptor ligands. Bioorg Med Chem Lett 26: 5613-5617 (2016)
- Murineddu, G; Gotti, C; Asproni, B; Corona, P; Martinello, K; Plutino, S; Fucile, S; Temml, V; Moretti, M; Viani, P; Schuster, D; Piras, S; Deligia, F; Pinna, GA Novel N-aryl nicotinamide derivatives: Taking stock on 3,6-diazabicyclo[3.1.1]heptanes as ligands for neuronal acetylcholine receptors. Eur J Med Chem 180: 51-61 (2019)
- Scanio, MJ; Shi, L; Bunnelle, WH; Anderson, DJ; Helfrich, RJ; Malysz, J; Thorin-Hagene, KK; Van Handel, CE; Marsh, KC; Lee, CH; Gopalakrishnan, M Structure-activity studies of diazabicyclo[3.3.0]octane-substituted pyrazines and pyridines as potent ?4?2 nicotinic acetylcholine receptor ligands. J Med Chem 54: 7678-92 (2011)
- Edink, E; Akdemir, A; Jansen, C; van Elk, R; Zuiderveld, O; de Kanter, FJ; van Muijlwijk-Koezen, JE; Smit, AB; Leurs, R; de Esch, IJ Structure-based design, synthesis and structure-activity relationships of dibenzosuberyl- and benzoate-substituted tropines as ligands for acetylcholine-binding protein. Bioorg Med Chem Lett 22: 1448-54 (2012)
- Horti, AG; Scheffel, U; Kimes, AS; Musachio, JL; Ravert, HT; Mathews, WB; Zhan, Y; Finley, PA; London, ED; Dannals, RF Synthesis and evaluation of N-[11C]methylated analogues of epibatidine as tracers for positron emission tomographic studies of nicotinic acetylcholine receptors. J Med Chem 41: 4199-206 (1998)
- Tu, Z; Efange, SM; Xu, J; Li, S; Jones, LA; Parsons, SM; Mach, RH Synthesis and in vitro and in vivo evaluation of 18F-labeled positron emission tomography (PET) ligands for imaging the vesicular acetylcholine transporter. J Med Chem 52: 1358-69 (2009)
- Ondachi, PW; Castro, AH; Bartkowiak, JM; Luetje, CW; Damaj, MI; Mascarella, SW; Navarro, HA; Carroll, FI Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 2'-fluoro-3'-(substituted pyridinyl)-7-deschloroepibatidine analogues. J Med Chem 57: 836-48 (2014)
- Carroll, FI; Ma, W; Deng, L; Navarro, HA; Damaj, MI; Martin, BR Synthesis, nicotinic acetylcholine receptor binding, and antinociceptive properties of 3'-(substituted phenyl)epibatidine analogues. Nicotinic partial agonists. J Nat Prod 73: 306-12 (2010)
- Takahata, H; Takahashi, S; Azer, N; Eldefrawi, AT; Eldefrawi, ME Total synthesis of pyrrolizidines 223H', 239K', 265H', and 267H' found in Madagascan frogs (Mantella) and their affinities for nicotinic acetylcholine receptor. Bioorg Med Chem Lett 10: 1293-5 (2000)
- ChEMBL_532109 Inhibition of rat brain acetylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay
- ChEMBL_450457 Inhibition of acetylcholine esterase
- ChEMBL_1549986 Mixed inhibition of electric eel acetylcholine esterase using acetylcholine iodide as substrate by Ellman's method
- ChEBML_138564 muscarinic acetylcholine receptor M1
- ChEMBL_1281569 Inhibition of human acetylcholine esterase
- ChEMBL_138564 muscarinic acetylcholine receptor M1
- ChEMBL_714885 Inhibition of human acetylcholine esterase
- ChEMBL_1549993 Non-competitive inhibition of electric eel acetylcholine esterase using acetylcholine iodide as substrate by Ellman's method
- ChEMBL_532107 Inhibition of electric eel acetylcholine esterase type V-S in presence of acetylcholine substrate by chemiluminescent assay
- ChEBML_138180 Affinity for Muscarinic acetylcholine receptor M2
- ChEBML_144330 Affinity for nicotinic acetylcholine receptor alpha7
- ChEMBL_144171 Affinity for Nicotinic acetylcholine receptor alpha7
- ChEMBL_1454323 Inhibition of acetylcholine esterase (unknown origin)
- ChEMBL_138372 In vitro antagonistic activity against peripheral Muscarinic acetylcholine receptor in guinea pig ileum as inhibition of acetylcholine induced muscle contraction
- ChEMBL_2129874 Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization
- ChEMBL_139465 Binding affinity was measured for Muscarinic acetylcholine receptor
- ChEMBL_140138 Binding affinity towards Muscarinic acetylcholine receptor
- ChEMBL_140140 Binding affinity towards Muscarinic acetylcholine receptor
- ChEMBL_143876 Affinity for nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143877 Affinity for nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_1454326 Binding affinity to acetylcholine esterase (unknown origin)
- ChEMBL_29095 Inhibitory activity against acetylcholine esterase (AChE)
- ChEMBL_302412 Affinity for rat Muscarinic acetylcholine receptor M2
- ChEMBL_302413 Affinity for rat Muscarinic acetylcholine receptor M3
- ChEMBL_697209 Binding affinity to muscarinic acetylcholine receptor M1
- ChEMBL_697210 Binding affinity to muscarinic acetylcholine receptor M2
- ChEMBL_697211 Binding affinity to muscarinic acetylcholine receptor M3
- ChEMBL_697212 Binding affinity to muscarinic acetylcholine receptor M4
- ChEMBL_697213 Binding affinity to muscarinic acetylcholine receptor M5
- ChEMBL_1588015 Positive allosteric modulation at rat muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
- ChEMBL_1588017 Positive allosteric modulation at human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
- ChEMBL_1712855 Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization
- ChEMBL_1444281 Negative allosteric modulation of human muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
- ChEMBL_1444284 Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo4AM staining-based fluorescence assay
- ChEMBL_1613481 Activity at human muscarinic acetylcholine receptor M1 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
- ChEMBL_1613482 Activity at human muscarinic acetylcholine receptor M3 transfected in CHO-K1 cells assessed as intracellular calcium levels in presence of acetylcholine by FLIPR assay
- ChEMBL_2104990 Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
- ChEMBL_2104993 Positive allosteric modulation of human muscarinic acetylcholine M3 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
- ChEMBL_2104995 Positive allosteric modulation of human muscarinic acetylcholine M5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
- ChEMBL_2129875 Antagonist activity at human muscarinic acetylcholine M4 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization relative to control
- ChEMBL_510504 Antagonist activity at human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
- ChEMBL_510508 Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
- ChEMBL_1284790 Negative allosteric modulation of rat muscarinic acetylcholine receptor M5 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
- ChEMBL_1284798 Negative allosteric modulation of rat muscarinic acetylcholine receptor M4 expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization incubated for 150 secs prior to acetylcholine induction by Fluo-4 AM staining-based fluorescence assay
- ChEMBL_1668507 Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization preincubated for 10 mins followed by acetylcholine addition by Fluo-8-AM dye based FLIPR assay
- ChEBML_138181 Binding affinity to cloned Muscarinic acetylcholine receptor M2
- ChEBML_138401 Affinity towards human muscarinic acetylcholine receptor M1
- ChEBML_138418 Binding affinity against Muscarinic acetylcholine receptor M1
- ChEBML_138698 Affinity towards human muscarinic acetylcholine receptor M3
- ChEBML_138712 Binding affinity against Muscarinic acetylcholine receptor M3
- ChEBML_138981 Binding affinity to cloned Muscarinic acetylcholine receptor M3
- ChEBML_139120 Affinity towards human Muscarinic acetylcholine receptor M4
- ChEBML_139127 Binding affinity against Muscarinic acetylcholine receptor M4
- ChEBML_139215 Binding affinity to cloned Muscarinic acetylcholine receptor M1
- ChEBML_139258 Binding affinity to cloned Muscarinic acetylcholine receptor M4
- ChEBML_139391 Affinity towards human Muscarinic acetylcholine receptor M5
- ChEBML_139519 Binding affinity to cloned Muscarinic acetylcholine receptor M5
- ChEBML_139642 Affinity towards human muscarinic acetylcholine receptor M2
- ChEBML_139750 Antagonistic activity against Muscarinic acetylcholine receptor M2
- ChEBML_139773 Binding affinity against Muscarinic acetylcholine receptor M2
- ChEBML_140179 Binding affinity towards Muscarinic acetylcholine receptor M2
- ChEBML_1688610 Inhibition of muscarinic acetylcholine M5 receptor (unknown origin)
- ChEMBL_138129 Pseudo hill coefficient at Muscarinic acetylcholine receptor M1
- ChEMBL_138181 Binding affinity to cloned Muscarinic acetylcholine receptor M2
- ChEMBL_138186 Inhibitory activity against Muscarinic acetylcholine receptor M2
- ChEMBL_138280 Binding affinity against muscarinic acetylcholine receptor M1
- ChEMBL_138383 Dissociation constant of the drug-Muscarinic acetylcholine receptor complex.
- ChEMBL_139209 Binding affinity to cloned Muscarinic acetylcholine receptor M1
- ChEMBL_139263 Binding affinity against Muscarinic acetylcholine receptor M4
- ChEMBL_139387 Binding affinity against muscarinic acetylcholine receptor M5
- ChEMBL_139623 Binding affinity against muscarinic acetylcholine receptor M2
- ChEMBL_139751 Antagonistic activity against Muscarinic acetylcholine receptor M2
- ChEMBL_139752 Antagonistic activity against muscarinic acetylcholine receptor M2
- ChEMBL_139756 Binding affinity against muscarinic acetylcholine receptor M2
- ChEMBL_139757 Binding affinity against muscarinic acetylcholine receptor M2
- ChEMBL_139759 Binding affinity for human Muscarinic acetylcholine receptor M2
- ChEMBL_143089 Agonist activity against Nicotinic acetylcholine receptor (nAchR)
- ChEMBL_1496344 Inhibition of muscarinic acetylcholine receptor M1 (unknown origin)
- ChEMBL_1496345 Inhibition of muscarinic acetylcholine receptor M2 (unknown origin)
- ChEMBL_1496346 Inhibition of muscarinic acetylcholine receptor M4 (unknown origin)
- ChEMBL_213558 Binding to vesicular acetylcholine transporter of torpedo synaptic vesicles
- ChEMBL_2163946 Inhibition of alpha7 nicotinic acetylcholine receptor (unknown origin)
- ChEMBL_223060 Binding affinity against nicotinic acetylcholine receptor (nAChR)
- ChEMBL_302296 Ki value for rat Muscarinic acetylcholine receptor M3
- ChEMBL_320786 Inhibition constant against nicotinic acetylcholine receptor alpha7
- ChEMBL_320815 Affinity towards cloned Muscarinic acetylcholine receptor M1
- ChEMBL_320816 Affinity towards cloned Muscarinic acetylcholine receptor M2
- ChEMBL_320817 Affinity towards cloned Muscarinic acetylcholine receptor M3
- ChEMBL_320818 Affinity towards cloned Muscarinic acetylcholine receptor M4
- ChEMBL_320819 Affinity towards cloned Muscarinic acetylcholine receptor M5
- ChEMBL_321367 Inhibitory concentration against muscarinic acetylcholine receptor M1
- ChEMBL_321368 Inhibitory concentration against muscarinic acetylcholine receptor M2
- ChEMBL_909611 Inhibition of alpha4beta2 nicotinic acetylcholine receptor (unknown origin)
- ChEMBL_1549983 Inhibition of electric eel acetylcholine esterase preincubated for 10 mins followed by the addition of acetylcholine iodide as substrate measured after 5 mins by Ellman's method
- ChEMBL_2104992 Positive allosteric modulation of human muscarinic acetylcholine M2/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
- ChEMBL_2104994 Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
- ChEMBL_2145726 Positive allosteric modulation of human muscarinic acetylcholine M4/Gqi5 receptor expressed in CHO cells in presence of acetylcholine at EC20 concentration by calcium mobilization assay
- ChEMBL_790181 Antagonist activity at human muscarinic acetylcholine receptor 4 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization
- ChEMBL_790182 Antagonist activity at human muscarinic acetylcholine receptor 1 expressed in CHO cells co-expressing Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization
- ChEMBL_1770306 Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 2.5 mins followed by acetylcholine addition measured after 1 min by Fluo-4AM-based FLIPR assay
- ChEMBL_1436836 Antagonist activity at muscarinic acetylcholine receptor M2 (unknown origin) expressed in CHOK1 cells after 15 mins by calcium flux/FLIPR assay in presence of acetylcholine
- ChEMBL_1549987 Inhibition of human acetylcholine esterase preincubated for 10 mins followed by the addition of 550 uM of acetylcholine iodide as substrate measured after 20 mins by Ellman's method
- ChEMBL_2023308 Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Galpha15 assessed as inhibition of acetylcholine-induced calcium mobilization relative to acetylcholine
- ChEMBL_510506 Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by FLIPR assay
- ChEMBL_915450 Inhibition of [3H]nicotine binding to alpha4 nicotinic acetylcholine receptor in Mus musculus (mouse) M10 cells co-expressing beta2 nicotinic acetylcholine receptor subunits
- ChEMBL_1770303 Positive allosteric modulation of human muscarinic acetylcholine receptor M1 expressed in CHO-NFAT cells assessed as potentiation of acetylcholine-induced calcium mobilization preincubated for 4 mins followed by acetylcholine addition measured after 4 mins by Fluo-4AM-based FLIPR assay
- ChEBML_138398 Dissociation constant for human Muscarinic acetylcholine receptor M1 was determined.
- ChEBML_139639 Dissociation constant for human Muscarinic acetylcholine receptor M2 was determined.
- ChEBML_140145 Compound was tested for inhibitory activity against Muscarinic acetylcholine receptor
- ChEMBL_138763 Binding affinity to Muscarinic acetylcholine receptor in rat cerebral cortex
- ChEMBL_139096 Binding affinity for rat cortex Muscarinic acetylcholine receptor M1
- ChEMBL_139464 Binding affinity towards Muscarinic acetylcholine receptor in rat was determined
- ChEMBL_143404 Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta4
- ChEMBL_143409 Agonistic potency against nicotinic acetylcholine receptor alpha3-beta4
- ChEMBL_143410 Inhibitory activity against nicotinic acetylcholine receptor alpha3-beta4
- ChEMBL_143698 Affinity for Nicotinic acetylcholine receptor alpha4-beta2 in rat brain
- ChEMBL_1437330 Allosteric agonist activity at human muscarinic acetylcholine receptor M5
- ChEMBL_143882 Binding affinity towards nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143883 Binding affinity towards nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_144175 Binding affinity at rat brain Nicotinic acetylcholine receptor alpha7
- ChEMBL_1473617 Binding affinity to muscarinic M1 acetylcholine receptor (unknown origin)
- ChEMBL_1712854 Positive allosteric modulation of human muscarinic acetylcholine M1 receptor
- ChEMBL_1712856 Positive allosteric modulation of rat muscarinic acetylcholine M1 receptor
- ChEMBL_1789227 Antagonist activity at muscarinic acetylcholine receptor M1 (unknown origin)
- ChEMBL_1979085 Binding affinity to muscarinic acetylcholine receptor M1 (unknown origin)
- ChEMBL_1979086 Binding affinity to muscarinic acetylcholine receptor M2 (unknown origin)
- ChEMBL_1979087 Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)
- ChEMBL_1979088 Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)
- ChEMBL_1979089 Binding affinity to muscarinic acetylcholine receptor M5 (unknown origin)
- ChEMBL_2068302 Binding affinity to muscarinic acetylcholine receptor M1 (unknown origin)
- ChEMBL_2068303 Binding affinity to muscarinic acetylcholine receptor M2 (unknown origin)
- ChEMBL_2068304 Binding affinity to muscarinic acetylcholine receptor M3 (unknown origin)
- ChEMBL_2068305 Binding affinity to muscarinic acetylcholine receptor M4 (unknown origin)
- ChEMBL_213559 Displacement of [3H]vesamicol from Vesicular Acetylcholine Transporter (VAChT)
- ChEMBL_302242 Dissociation constant against Nicotinic acetylcholine receptor alpha3-beta2
- ChEMBL_302243 Dissociation constant against Nicotinic acetylcholine receptor alpha3-beta4
- ChEMBL_302244 Dissociation constant against Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_302786 Binding affinity for rat Nicotinic acetylcholine receptor alpha2-beta2
- ChEMBL_302787 Binding affinity for rat Nicotinic acetylcholine receptor alpha2-beta4
- ChEMBL_302788 Binding affinity for rat Nicotinic acetylcholine receptor alpha3-beta2
- ChEMBL_302789 Binding affinity for rat Nicotinic acetylcholine receptor alpha3-beta4
- ChEMBL_302790 Binding affinity for rat Nicotinic acetylcholine receptor alpha4-beta4
- ChEMBL_304161 Effective concentration against rat alpha7 nicotinic acetylcholine receptor
- ChEMBL_304167 Effective concentration against Nicotinic acetylcholine receptor alpha 7
- ChEMBL_304195 Effective concentration against Nicotinic acetylcholine receptor alpha2-beta4
- ChEMBL_304196 Effective concentration against Nicotinic acetylcholine receptor alpha3-beta2
- ChEMBL_304198 Effective concentration against Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_305504 Inhibitory concentration against Nicotinic acetylcholine receptor alpha 7
- ChEMBL_305538 Inhibitory concentration against Nicotinic acetylcholine receptor alpha 7
- ChEMBL_305724 Inhibitory concentration against Nicotinic acetylcholine receptor alpha2-beta2
- ChEMBL_305725 Inhibitory concentration against Nicotinic acetylcholine receptor alpha2-beta4
- ChEMBL_305726 Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta2
- ChEMBL_305728 Inhibitory concentration against Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_305760 Inhibitory concentration against Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_306021 Inhibitory concentration against human Muscarinic acetylcholine receptor M1
- ChEMBL_659488 Binding affinity to human acetylcholine esterase by radioligand displacement assay
- ChEMBL_982013 Binding affinity to muscarinic acetylcholine receptor M2 (unknown origin)
- ChEMBL_510505 Antagonist activity at human muscarinic acetylcholine M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
- ChEMBL_510509 Antagonist activity at human muscarinic acetylcholine M3 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
- ChEMBL_820325 Inhibition of electric eel acetylcholine esterase using acetylcholine chloride as substrate incubated for 5 mins prior to substrate addition measured every 3 mins by Ellman's assay
- ChEMBL_823696 Inhibition of electric eel acetylcholine esterase using acetylcholine chloride as substrate incubated for 15 mins prior to substrate addition measured every 1 min by Ellman's assay
- ChEMBL_915451 Inhibition of [3H]nicotine binding to alpha3 nicotinic acetylcholine receptor in Homo sapiens (human) SH-SY5Y cells co-expressing beta2beta4alpha5 Nicotinic acetylcholine receptor subunits
- ChEMBL_915454 Inhibition of [3H]alpha-BGT binding to alpha1 nicotinic acetylcholine receptor in Homo sapiens (human) TE671 cells co-expressing gammaalpha1deltabeta1 nicotinic acetylcholine receptor subunits
- ChEBML_138412 Binding affinity towards the cloned human Muscarinic acetylcholine receptor M1
- ChEBML_138806 Displacement of [3H]pirenzepine from cerebral Muscarinic acetylcholine receptor M1
- ChEBML_139395 The compound was tested for the binding affinity against Muscarinic acetylcholine receptor M5
- ChEBML_139762 Binding affinity against cloned human muscarinic acetylcholine receptor M2.
- ChEBML_139763 Binding affinity towards the cloned human Muscarinic acetylcholine receptor M2
- ChEBML_139772 Binding affinity against human cloned Muscarinic acetylcholine receptor M2.
- ChEBML_140175 Binding affinity at human cloned acetylcholine receptor M2 in CHO cells.
- ChEBML_143096 Alpha 7 nicotinic acetylcholine receptor binding activity in PC12 cells
- ChEBML_143223 Binding affinity towards alpha3-beta4 neuronal nicotinic acetylcholine receptor
- ChEMBL_138191 Dissociation constant at muscarinic acetylcholine receptor M3 guinea pig bladder.
- ChEMBL_138192 Dissociation constant at muscarinic acetylcholine receptor M3 of guinea pig ileum.
- ChEMBL_138211 In vitro binding affinity against Muscarinic acetylcholine receptors in rat brain.
- ChEMBL_138261 Displacement of [3H]QNB from rat ileum Muscarinic acetylcholine receptor
- ChEMBL_138381 Dissociation constant towards Muscarinic acetylcholine receptor in guinea pig ileum
- ChEMBL_138412 Binding affinity towards the cloned human Muscarinic acetylcholine receptor M1
- ChEMBL_138635 Dissociation constant towards Muscarinic acetylcholine receptor in guinea pig ileum
- ChEMBL_138690 Binding affinity towards Muscarinic acetylcholine receptor M1 of cerebral cortex
- ChEMBL_138762 Binding affinity against the Muscarinic acetylcholine receptor using [3H]- QNB
- ChEMBL_138806 Displacement of [3H]pirenzepine from cerebral Muscarinic acetylcholine receptor M1
- ChEMBL_138855 Binding affinity against muscarinic acetylcholine receptor M2 of rat heart.
- ChEMBL_138919 The compound was tested for inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor
- ChEMBL_138944 Binding affinity towards rat Muscarinic acetylcholine receptor M1 was determined
- ChEMBL_138945 Affinity for rat M1 acetylcholine receptor using [3H]pirenzepine displacement.
- ChEMBL_138953 Binding affinity against Muscarinic acetylcholine receptor M1 sites of rat
- ChEMBL_139256 Inhibition of NG 108-15 binding to Muscarinic acetylcholine receptor M4
- ChEMBL_139763 Binding affinity towards the cloned human Muscarinic acetylcholine receptor M2
- ChEMBL_140180 Binding affinity towards rat Muscarinic acetylcholine receptor M2 was determined
- ChEMBL_143096 Alpha 7 nicotinic acetylcholine receptor binding activity in PC12 cells
- ChEMBL_143102 Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta2
- ChEMBL_143103 Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta2
- ChEMBL_143230 Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta4
- ChEMBL_143231 Tested for binding affinity against Nicotinic acetylcholine receptor alpha2-beta4
- ChEMBL_143244 Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta2
- ChEMBL_143245 Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta2
- ChEMBL_143394 Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta4
- ChEMBL_143395 Tested for binding affinity against Nicotinic acetylcholine receptor alpha3-beta4
- ChEMBL_143544 Binding affinity against human Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143565 Functional potency for Nicotinic acetylcholine receptor alpha4-beta2 (rat brain)
- ChEMBL_143696 Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143702 Binding potency for Nicotinic acetylcholine receptor alpha4-beta2 (rat brain)
- ChEMBL_143706 Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143710 Evaluated for binding affinity towards nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143718 Inhibition of [3H]-nicotine binding at the nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_144012 Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta4
- ChEMBL_144013 Tested for binding affinity against Nicotinic acetylcholine receptor alpha4-beta4
- ChEMBL_144041 Functional potency for Nicotinic acetylcholine receptor alpha-7 (rat brain)
- ChEMBL_144042 Functional potency for Nicotinic acetylcholine receptor alpha-7 (rat brain)
- ChEMBL_144176 Binding affinity in rat hippocampi against Nicotinic acetylcholine receptor alpha7
- ChEMBL_144182 Binding potency for Nicotinic acetylcholine receptor alpha-7 (rat brain)
- ChEMBL_144183 Binding potency for Nicotinic acetylcholine receptor alpha-7 (rat brain)
- ChEMBL_1500179 Inhibition of human acetylcholine esterase by horseradish peroxidase-coupled fluorescence assay
- ChEMBL_1700418 Displacement of [3H]NMS from human muscarinic acetylcholine receptor M2
- ChEMBL_223059 Compound was evaluated for the binding constant for association with nicotinic acetylcholine receptor (nAChR)
- ChEMBL_303090 Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2; Not significant
- ChEMBL_303167 Binding affinity against nicotinic acetylcholine receptor subtype alpha2-beta2
- ChEMBL_303210 Inhibition of [3H]MLA binding to rat alpha7 nicotinic acetylcholine receptor
- ChEMBL_303420 Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha3-beta2
- ChEMBL_304157 Effective concentration against alpha3-beta4 Nicotinic acetylcholine receptor (nAChR)
- ChEMBL_304158 Effective concentration against rat alpha-7 nicotinic acetylcholine receptor
- ChEMBL_304171 Effective concentration against rat alpha3-beta4 nicotinic acetylcholine receptor
- ChEMBL_304172 Effective concentration against rat alpha4-beta2 nicotinic acetylcholine receptor
- ChEMBL_469306 Activity at alpha7 nACh receptor assessed as modulation of acetylcholine-induced response
- ChEMBL_73104 Agonist activity at muscarinic acetylcholine receptor in isolated guinea pig ileum.
- ChEMBL_73105 Agonist activity at muscarinic acetylcholine receptor in isolated guinea pig ileum.
- ChEMBL_816768 Inhibition of electric eel AChE using acetylcholine as substrate by Ellman's method
- ChEMBL_851198 Antagonist activity at alpha7 nAChR assessed as amplitude of acetylcholine evoked currents
- ChEMBL_851200 Antagonist activity at alpha4beta2 nAChR assessed as amplitude of acetylcholine evoked currents
- ChEMBL_915457 Inhibition of [3H]IMI binding to Drosophila melanogaster neuronal acetylcholine receptor
- ChEMBL_983858 Positive allosteric modulation at muscarinic acetylcholine receptor M1(unknown origin)
- ChEMBL_1729568 Antagonist activity at mAChR M3 in human CCRF-CEM cells assessed as inhibition of acetylcholine-mediated calcium flux incubated for 25 mins followed by acetylcholine stimulation measured for 90 secs
- ChEMBL_510507 Antagonist activity at human muscarinic acetylcholine M2 receptor expressed in CHO cells coexpressed with Gqi5 assessed as inhibition of acetylcholine-induced calcium mobilization by single concentration kinetic FLIPR assay
- ChEBML_138302 Muscarinic acetylcholine receptor M3 agonistic/antagonistic activity in guinea pig ileum
- ChEBML_138940 Binding affinity against muscarinic acetylcholine receptor M1 of rat cerebral cortex.
- ChEBML_139201 Binding affinity against muscarinic acetylcholine receptor M3 of rat sabmandibular glands
- ChEBML_140152 Binding affinity for Muscarinic acetylcholine receptor was determined by using [3H]QNB as radioligand
- ChEBML_143888 Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in cultured hippocampal neurons
- ChEBML_144198 Inhibition of [3H]-MLA binding to Nicotinic acetylcholine receptor alpha7 in rat brain
- ChEBML_1685391 Activity at human M2 receptor assessed as increase in acetylcholine-induced calcium mobilization
- ChEBML_184442 Evaluated for the phosphatidyl inositol turnover at Muscarinic acetylcholine receptor M1 in rat cortex
- ChEBML_27376 Compound was evaluated for reversible inhibition of hydrolysis acetylcholine by acetylcholinesterase and represented as KI(competitive)
- ChEMBL_138172 Inhibition of [3H]NMS binding to rat heart Muscarinic acetylcholine receptor M2
- ChEMBL_138302 Muscarinic acetylcholine receptor M3 agonistic/antagonistic activity in guinea pig ileum
- ChEMBL_138312 Dissociation constant for complex with muscarinic acetylcholine receptor M3 of guinea pig ileum
- ChEMBL_138918 Displacement of [3H]QNB from Muscarinic acetylcholine receptor of rat brain membrane
- ChEMBL_138940 Binding affinity against muscarinic acetylcholine receptor M1 of rat cerebral cortex.
- ChEMBL_139318 Inhibition of [3H]QNB binding against muscarinic acetylcholine receptor in rat brain.
- ChEMBL_139319 Inhibition of [3H]QNB binding against muscarinic acetylcholine receptor in rat heart.
- ChEMBL_139322 Inhibition of [3H]pirenzepine binding against muscarinic acetylcholine receptor in rat brain.
- ChEMBL_139641 Affinity for human muscarinic acetylcholine receptor M2 expressed in CHO-K1 cells
- ChEMBL_140144 Binding affinity against Muscarinic acetylcholine receptor using [3H]quinuclidinyl benzilate
- ChEMBL_140153 Binding affinity against Muscarinic acetylcholine receptor using [3H]QNB as the radioligand.
- ChEMBL_140177 Binding affinity against muscarinic acetylcholine receptor M3 of rat sabmandibular glands
- ChEMBL_142767 The compound was tested for inhibitory potency against Nicotinic acetylcholine receptor in Rat muscle.
- ChEMBL_143095 Binding affinities for the alpha 7 nicotinic acetylcholine receptor was determined in PC12 cells
- ChEMBL_143243 Inhibition of rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in Xenopus Oocytes
- ChEMBL_143563 Compound was evaluated for functional potencies and efficacies at ratNicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143700 Binding affinity in rat forebrain against Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143884 In vitro Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 was determined
- ChEMBL_143887 Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in acute hippocampal slices
- ChEMBL_143888 Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in cultured hippocampal neurons
- ChEMBL_144023 Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha7
- ChEMBL_144030 Binding affinity against human Nicotinic acetylcholine receptor alpha-7 was determined
- ChEMBL_144331 Blockage of Nicotinic acetylcholine receptor alpha-7 noncompetitively in cultured hippocampal neurons
- ChEMBL_144332 Blockage of Nicotinic acetylcholine receptor alpha-7 noncompetitively in hippocampal primary cultures
- ChEMBL_144957 Inhibition of recombinant embryonic mouse muscle Nicotinic Acetylcholine Receptor (3 oocytes)
- ChEMBL_1504716 Displacement of [3H]-nicotine from alpha4beta2 nicotine acetylcholine receptor (unknown origin)
- ChEMBL_1557341 Binding affinity to human muscarinic acetylcholine M5 receptor by radioligand binding assay
- ChEMBL_184442 Evaluated for the phosphatidyl inositol turnover at Muscarinic acetylcholine receptor M1 in rat cortex
- ChEMBL_1888969 Inhibition of AChE (unknown origin) using acetylcholine iodide as substrate by Ellman method
- ChEMBL_222719 Binding affinity against muscarinic acetylcholine receptor M1 of rat cerebral cortex.
- ChEMBL_27375 Compound was evaluated for reversible inhibition of hydrolysis acetylcholine by acetylcholinesterase and represented as KI(com)
- ChEMBL_27376 Compound was evaluated for reversible inhibition of hydrolysis acetylcholine by acetylcholinesterase and represented as KI(competitive)
- ChEMBL_27377 Compound was evaluated for reversible inhibition of hydrolysis acetylcholine by acetylcholinesterase and represented as KI(noncompetitive)
- ChEMBL_27378 Compound was evaluated for reversible inhibition of hydrolysis of acetylcholine by acetylcholinesterase and represented as KI(competitive)
- ChEMBL_302237 Dissociation constant for rat Nicotinic acetylcholine receptor alpha-7 at 45 pM
- ChEMBL_303011 Inhibition of [3H]-MLA binding to rat alpha-7 nicotinic acetylcholine receptor
- ChEMBL_303189 Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_303228 Inhibition of [3H]nicotine binding to rat alpha4-beta2 nicotinic acetylcholine receptor
- ChEMBL_303347 Inhibition of [125I]alpha-bungarotoxin binding to rat nicotinic acetylcholine receptor alpha7
- ChEMBL_303477 Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha3-beta4
- ChEMBL_303478 Inhibition of [3H]epibatidine binding to rat Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_306411 Inhibition of [125I]alpha-bungarotoxin binding to rat nicotinic acetylcholine receptor alpha7
- ChEMBL_310491 Change in membrane potential in TE-671 cells expressing acetylcholine neuromuscular receptors
- ChEMBL_532108 Inhibition of horse serum butyrylcholine esterase in presence of acetylcholine substrate by chemiluminescent assay
- ChEMBL_741147 Mixed inhibition of Electrophorus electricus acetylcholinesterase using acetylcholine as substrate by Ellman's method
- ChEMBL_935571 Positive allosteric modulation of rat muscarinic M5 receptor assessed as acetylcholine response
- ChEMBL_935573 Positive allosteric modulation of rat muscarinic M3 receptor assessed as acetylcholine response
- ChEMBL_935576 Positive allosteric modulation of rat muscarinic M2 receptor assessed as acetylcholine response
- ChEMBL_935580 Positive allosteric modulation of rat muscarinic M1 receptor assessed as acetylcholine response
- ChEMBL_935589 Positive allosteric modulation of rat muscarinic M4 receptor assessed as acetylcholine response
- ChEMBL_980915 Inhibition of purified human erythrocyte AChE using acetylcholine as substrate by Ellman's method
- ChEMBL_1741062 Antagonist activity at mAChR in human CCRF-CEM cells assessed as inhibition of acetylcholine-induced calcium release preincubated for 25 mins followed by acetylcholine stimulation and measured for 90 secs by calcium flux assay
- ChEBML_1712853 Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO-NFAT cells assessed as potentiation of acetylcholine-induced calcium mobilization after 4 hrs by CCF4-AM dye-based assay
- ChEBML_1734264 Antagonist activity at mAChR in human CCRF-CEM cells assessed as inhibition of acetylcholine-induced calcium flux pretreated for 25 mins followed by acetylcholine addition measured for 90 secs by calcium-dye based assay
- ChEMBL_1712853 Positive allosteric modulation of human muscarinic acetylcholine M1 receptor expressed in CHO-NFAT cells assessed as potentiation of acetylcholine-induced calcium mobilization after 4 hrs by CCF4-AM dye-based assay
- ChEMBL_1734264 Antagonist activity at mAChR in human CCRF-CEM cells assessed as inhibition of acetylcholine-induced calcium flux pretreated for 25 mins followed by acetylcholine addition measured for 90 secs by calcium-dye based assay
- ChEMBL_2172717 Inhibition of human (alpha4)3(beta2)2 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response in presence of 100 uM acetylcholine by two-electrode voltage-clamp method
- ChEMBL_2172719 Inhibition of human (alpha4)2(beta2)3 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced current response in presence of 3 uM acetylcholine by two-electrode voltage-clamp method
- ChEBML_138407 Binding affinity against human Muscarinic acetylcholine receptor M1 in transfected CHO cells
- ChEBML_138413 Binding affinity against Muscarinic acetylcholine receptor M1 expressed in CHO-K1 cells
- ChEBML_138643 Compound was tested for the binding affinity towards muscarinic acetylcholine receptor in mouse brain membrane
- ChEBML_138705 Binding affinity against human muscarinic acetylcholine receptor M3 in transfected CHO cells
- ChEBML_138706 Binding affinity against Muscarinic acetylcholine receptor M3 expressed in CHO-K1 cells
- ChEBML_138792 Inhibition of [3H]pirenzepine binding to rat brain membrane Muscarinic acetylcholine receptor M1
- ChEBML_138852 Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M3 transfected with CHO cell
- ChEBML_138935 Inhibition of [3H]QNB binding to Muscarinic acetylcholine receptor M1 transfected with CHO cell
- ChEBML_138954 Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 of rat brain membrane
- ChEBML_139068 Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 in rat cortex homogenates
- ChEBML_139069 Ability to displace [3H]pirenzepine radioligand for the Muscarinic acetylcholine receptor M1 in rat brain
- ChEBML_139463 Binding affinity to muscarinic acetylcholine receptor was determined in presence of [3H]QNB radioligand (in vitro)
- ChEBML_139466 Inhibition of [3H]N-methylscopolamine binding to muscarinic acetylcholine receptor of rat cerebral cortex.
- ChEBML_139760 Binding affinity against human muscarinic acetylcholine receptor M2 in transfected CHO cells
- ChEBML_1696021 Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced response
- ChEBML_27660 Inhibition of active transport of [3H]acetylcholine using purified Torpedo californica synaptic vesicles
- ChEMBL_138132 Compound is evaluated for in vitro receptor binding affinity against Muscarinic acetylcholine receptor M1
- ChEMBL_138264 Compound was tested for its potency against Muscarinic acetylcholine receptor in guinea pig ileum
- ChEMBL_138316 Binding affinity towards Muscarinic acetylcholine receptor M3 was determined in guinea pig ileum
- ChEMBL_138351 Compound was evaluated for binding activity against [3H]dexetimide as radioligand for muscarinic-acetylcholine receptor
- ChEMBL_138385 Inhibition of [3H]QNB binding against muscarinic acetylcholine receptor in guinea pig ileum
- ChEMBL_138539 Affinity for Muscarinic acetylcholine receptor M1 expressed in CHO cells by [3H]NMS displacement.
- ChEMBL_138542 Compound was tested for binding affinity against human cloned Muscarinic acetylcholine receptor M1
- ChEMBL_138556 Tested against Muscarinic acetylcholine receptor M1 expressed in A9 L cell line
- ChEMBL_138643 Compound was tested for the binding affinity towards muscarinic acetylcholine receptor in mouse brain membrane
- ChEMBL_138645 Dissociation constant towards Muscarinic acetylcholine receptor was determined by using [3H]4NMPB as radioligand
- ChEMBL_138646 Compound was tested for the binding affinity towards muscarinic acetylcholine receptor in mouse brain membrane
- ChEMBL_138647 Dissociation constant towards Muscarinic acetylcholine receptor was determined by using [3H]4NMPB as radioligand
- ChEMBL_138656 Displacement of [3H]quinuclidinyl benzilate (QNB) from Muscarinic acetylcholine receptor in rat brain
- ChEMBL_138657 Displacement of [3H]quinuclidinyl benzilate(QNB) from Muscarinic acetylcholine receptor in rat brain
- ChEMBL_138660 Binding affinity against Muscarinic acetylcholine receptor in rat brain using [3H]- QNB
- ChEMBL_138775 Binding affinity against Muscarinic acetylcholine receptor in rat brain using [3H]- QNB
- ChEMBL_138778 Inhibition of [3H]oxotremorine-M binding to rat brain membrane Muscarinic acetylcholine receptor
- ChEMBL_138803 Displacement of [3H]pirenzepine (Pz) from rat hippocampus muscarinic acetylcholine receptor M1
- ChEMBL_138827 Affinity for Muscarinic acetylcholine receptor M3 expressed in CHO cells by [3H]-NMS displacement.
- ChEMBL_138834 Tested against Muscarinic acetylcholine receptor M3 expressed in A9 L cell line
- ChEMBL_138952 Binding affinity against Muscarinic acetylcholine receptor M1 by using [3H]pirenzepine as a radioligand
- ChEMBL_138954 Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 of rat brain membrane
- ChEMBL_138959 Compound was evaluated for its binding affinity towards muscarinic acetylcholine receptor in rat cortex
- ChEMBL_138975 Inhibition of [3H]NMS binding to rat submaxillary gland Muscarinic acetylcholine receptor M3
- ChEMBL_139069 Ability to displace [3H]pirenzepine radioligand for the Muscarinic acetylcholine receptor M1 in rat brain
- ChEMBL_139224 Dissociation constant at muscarinic acetylcholine receptor M2 guinea pig heart(atria force).
- ChEMBL_139225 Dissociation constant at muscarinic acetylcholine receptor M2 of guinea pig heart(atria rate).
- ChEMBL_139240 Affinity for Muscarinic acetylcholine receptor M4 expressed in CHO cells by [3H]NMS displacement.
- ChEMBL_139314 Inhibition of [3H]QNB binding to muscarinic acetylcholine receptor of rat heart membrane preparation.
- ChEMBL_139341 Compound is evaluated for in vitro receptor binding affinity against Muscarinic acetylcholine receptor M2
- ChEMBL_139382 Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells
- ChEMBL_139383 Agonistic activity against muscarinic acetylcholine receptor M5 expressed in NIH 3T3 cells.
- ChEMBL_139389 Inhibition of [3H]- NMS binding against human recombinant Muscarinic acetylcholine receptor M5
- ChEMBL_139390 Affinity for human muscarinic acetylcholine receptor M5 subtype expressed in CHO-K1 cells
- ChEMBL_139394 Inhibition of [3H]- NMS binding against human recombinant Muscarinic acetylcholine receptor M5
- ChEMBL_139457 Binding affinity against Muscarinic acetylcholine receptor using [3H]-OXO-M as the radioligand.
- ChEMBL_139463 Binding affinity to muscarinic acetylcholine receptor was determined in presence of [3H]QNB radioligand (in vitro)
- ChEMBL_139466 Inhibition of [3H]N-methylscopolamine binding to muscarinic acetylcholine receptor of rat cerebral cortex.
- ChEMBL_139512 Affinity for Muscarinic acetylcholine receptor M5 expressed in CHO cells by [3H]NMS displacement.
- ChEMBL_139885 Affinity for Muscarinic acetylcholine receptor M2 expressed in CHO cells by [3H]NMS displacement.
- ChEMBL_139889 Compound was tested for binding affinity against human cloned Muscarinic acetylcholine receptor M2
- ChEMBL_140045 Inhibition of [3H]quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M2 of rat heart
- ChEMBL_140141 The compound was tested for binding affinity against Muscarinic acetylcholine receptor using QNB as radioligand
- ChEMBL_140142 The compound was tested for binding affinity against muscarinic acetylcholine receptor using QNB as radioligand
- ChEMBL_140161 Binding affinity towards Muscarinic acetylcholine receptor M1 was determined in calf brain membrane
- ChEMBL_140178 Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M2 of rat heart
- ChEMBL_140181 Affinity for rat M1 acetylcholine receptor using [3H]-AF DX 384 displacement.
- ChEMBL_143225 Binding affinity towards nicotinic acetylcholine receptor alpha2-beta2 using [3H]epibatidine
- ChEMBL_143232 Binding affinity towards Nicotinic acetylcholine receptor alpha2-beta4 using [3H]epibatidine
- ChEMBL_143249 Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta2 using [3H]epibatidine
- ChEMBL_143405 Binding affinity towards Nicotinic acetylcholine receptor alpha3-beta4 using [3H]epibatidine
- ChEMBL_143541 Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143543 Compound was evaluated for functional potency and efficacy at human Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143552 Antagonism of ACh response at Nicotinic acetylcholine receptor alpha4-beta2 expressed in xenopus oocytes
- ChEMBL_143560 Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143564 Compound was evaluated for functional potency and efficacy at human Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_143697 Displacement of [3H]cytisine from Nicotinic acetylcholine receptor alpha4-beta2 in rat forebrain
- ChEMBL_143728 Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 using [3H]epibatidine
- ChEMBL_143866 Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 in rat brain
- ChEMBL_143873 [3H](+/-)-epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes
- ChEMBL_143886 Blockage of Nicotinic acetylcholine receptor alpha4-beta2 noncompetitively in CA1 stratum radiatum interneurons
- ChEMBL_144015 Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta4 using [3H]epibatidine
- ChEMBL_144034 Compound was evaluated for inhibition of rat Nicotinic acetylcholine receptor alpha7 (nAChR) in Xenopus Oocytes
- ChEMBL_144168 Binding affinity of Norditerpenoid Alkaloids at rat neuronal alpha7-type nicotinic acetylcholine receptor
- ChEMBL_144964 Compound was evaluated for inhibition of [3H]TCP binding to Nicotinic acetylcholine receptor of Torpedo californica
- ChEMBL_1504717 Displacement of [3H]-methyllycaconitine from alpha7 nicotine acetylcholine receptor in rat brain membranes
- ChEMBL_1746221 Positive allosteric modulation of human M1 receptor assessed as increase in acetylcholine-induced response
- ChEMBL_1746222 Positive allosteric modulation of human M2 receptor assessed as increase in acetylcholine-induced response
- ChEMBL_1746223 Positive allosteric modulation of human M3 receptor assessed as increase in acetylcholine-induced response
- ChEMBL_1746224 Positive allosteric modulation of human M5 receptor assessed as increase in acetylcholine-induced response
- ChEMBL_1804487 Activity of compound against Muscarinic acetylcholine receptor M1 (CHRM1) by displacement of 3H-QNB
- ChEMBL_1804550 Activity of compound against Muscarinic acetylcholine receptor M2 (CHRM2) by displacement of 3H-QNB
- ChEMBL_1804551 Activity of compound against Muscarinic acetylcholine receptor M3 (CHRM3) by displacement of 3H-QNB
- ChEMBL_1804552 Activity of compound against Muscarinic acetylcholine receptor M4 (CHRM4) by displacement of 3H-QNB
- ChEMBL_1804553 Activity of compound against Muscarinic acetylcholine receptor M5 (CHRM5) by displacement of 3H-QNB
- ChEMBL_222735 Tested for affinity against muscarinic acetylcholine using [3H]quinuclidinyl benzylate in rat brain
- ChEMBL_27660 Inhibition of active transport of [3H]acetylcholine using purified Torpedo californica synaptic vesicles
- ChEMBL_28502 In vitro inhibitory concentration against Muscarinic acetylcholine receptor derived from rat adrenals
- ChEMBL_303377 Inhibition of [3H]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha7 of IMR32 cells
- ChEMBL_304220 Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor expressed in IMR32 cell
- ChEMBL_304305 Effective concentration against Nicotinic acetylcholine receptor alpha 7 expressed in xenopus oocytes
- ChEMBL_304329 Effective concentration against Nicotinic acetylcholine receptor alpha3-beta2 expressed in xenopus oocytes
- ChEMBL_306078 Inhibitory concentration against Nicotinic acetylcholine receptor alpha7; Range is 0.5-8 nM
- ChEMBL_306101 Inhibitory concentration against Nicotinic acetylcholine receptor alpha7; Range is 100-200 nM
- ChEMBL_306102 Inhibitory concentration against Nicotinic acetylcholine receptor alpha9; Range is 100-200 nM
- ChEMBL_306126 Inhibitory concentration against Nicotinic acetylcholine receptor alpha7; Range is 0.3-1.5 nM
- ChEMBL_306143 Inhibitory concentration against Nicotinic acetylcholine receptor alpha7; Range is 0.3-1.5 nM
- ChEMBL_306526 Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta2 expressed in xenopus oocytes
- ChEMBL_320891 Binding affinity for rat cortex muscarinic acetylcholine receptor M1 using [3H]pirenzepine
- ChEMBL_321674 Agonistic activity against Muscarinic acetylcholine receptor of guinea pig ileal longitudinal muscle
- ChEMBL_39943 Effect on alpha3-beta4 neuronal nicotinic acetylcholine receptor-stimulated adrenal catecholamine secretion
- ChEMBL_613843 Inhibition of human recombinant AChE-mediated hydrolysis of acetylcholine by Lineweaver-Burke plot analysis
- ChEMBL_653619 Displacement of acetylcholine from AChE in Swiss Webster mouse brain after 5 mins
- ChEMBL_674713 Inhibition of equine BChE after 15 mins by Ellman's method using acetylcholine as substrate
- ChEMBL_851173 Partial agonist activity at human alpha7 nAChR expressed in Xenopus oocytes relative to acetylcholine
- ChEMBL_851174 Partial agonist activity at human alpha7 nAChR expressed in GH4C1 cells relative to acetylcholine
- ChEMBL_1809635 Positive allosteric modulation of human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as increase in acetylcholine-induced channel current by measuring acetylcholine EC50 at 10 uM at -90 mV holding potential preincubated for 2 mins followed by co-application with acetylcholine for 10 secs by two-electrode voltage clamp method (Rvb = 256.4 +/- 20.1 uM)
- ChEMBL_1888405 Positive allosteric modulation activity at human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as increase in acetylcholine-induced channel current by measuring acetylcholine EC50 at 10 uM at -90 mV holding potential preincubated for 2 mins followed by co-application with acetylcholine for 10 secs by two-electrode voltage clamp method (Rvb = 231.8 +/- 2 uM)
- ChEMBL_1508833 Antagonist activity at rat alpha-7 nicotinic acetylcholine receptor expressed in Xenopus oocytes assessed as inhibition of acetylcholine-induced currents preincubated for 10 mins followed by nicotine induction by two-electrode voltage-clamp electrophysiology assay
- ChEMBL_1636028 Antagonist activity at human 5-HT3A expressed in HEK293 cells assessed as reduction in acetylcholine-induced activity preincubated for 30 mins followed by addition of acetylcholine measured for 2 mins by Fluo-4AM dye based FLIPR assay
- ChEMBL_830306 Positive allosteric modulation of human M4 receptor expressed in CHO-K1 cells coexpressing Gqi5 assessed as potentiation of acetylcholine-mediated calcium mobilization incubated for 144 secs prior to acetylcholine addition by Fluo-4-AM staining
- ChEBML_138139 Inhibition of [3H]QNB binding to CHO cells bearing transfected muscarinic acetylcholine receptor M1
- ChEBML_138278 Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
- ChEBML_138301 In vitro contraction of guinea pig myenteric plexus preparation (mediated by muscarinic acetylcholine receptor M3)
- ChEBML_138550 Inhibition of [3H]pirenzepine binding to mouse muscarinic acetylcholine receptor M1 from cerebral cortex
- ChEBML_138691 Binding affinity towards muscarinic receptor of cerebral cortex containing Muscarinic acetylcholine receptor M1
- ChEBML_138961 Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
- ChEBML_139462 Binding affinity to muscarinic acetylcholine receptor was determined in presence of [3H]OXO-M radioligand (in vitro)
- ChEBML_139765 Binding affinity against Muscarinic acetylcholine receptor M2 stably expressed in CHO-K1 cells.
- ChEBML_140042 Binding affinity towards muscarinic receptor of gastric fundus containing Muscarinic acetylcholine receptor M2
- ChEBML_140043 Displacement of [3H]QNB from Muscarinic acetylcholine receptor M2 from rat heart homogenates
- ChEBML_140160 Binding affinity against Muscarinic acetylcholine receptor M1 by displacement of [3H]pirenzepine in bovine striatum
- ChEBML_140188 Compound was evaluated for its binding affinity towards muscarinic acetylcholine receptor M2 in rat brainstem
- ChEBML_144181 Binding affinity towards Nicotinic acetylcholine receptor alpha-7 using [3H]-MLA as radioligand
- ChEBML_144185 Inhibition of [125I]MLA binding to Nicotinic acetylcholine receptor alpha7 from rat brain membranes
- ChEBML_1679911 Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
- ChEMBL_138140 Inhibition of [3H]QNB binding to CHO cells bearing transfected muscarinic acetylcholine receptor M3
- ChEMBL_138278 Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
- ChEMBL_138281 Binding affinity of [3H]-QNB to CHO cells expressing human Muscarinic acetylcholine receptor M1
- ChEMBL_138289 In vitro affinity against human Muscarinic acetylcholine receptor M1 using quinuclidynyl benzylate (QNB)
- ChEMBL_138395 In vitro inhibition of binding of (-)-[3H]-NMS to Muscarinic acetylcholine receptor of rat cerebral cortex was determined
- ChEMBL_138399 Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M1 expressed in CHO cells
- ChEMBL_138442 Compound was evaluated for its antagonist affinity towards Muscarinic acetylcholine receptor M3 of guinea pig
- ChEMBL_138443 The compound was tested for antagonistic activity against Muscarinic acetylcholine receptor M3 in guinea pig trachea
- ChEMBL_138544 Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M1 in transfected CHO cells.
- ChEMBL_138561 Compound was evaluated for its antagonist affinity towards Muscarinic acetylcholine receptor M3 of guinea pig
- ChEMBL_138658 Binding activity against muscarinic acetylcholine receptor in rat brain using [3H]QNB as the radioligand
- ChEMBL_138661 Binding affinity against Muscarinic acetylcholine receptor in rat striatal membrane using [3H]haloperidol
- ChEMBL_138696 Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 expressed in CHO cells
- ChEMBL_138765 Compound was evaluated for the inhibition of binding of [3H]QNB (quinuclidinyl benzilate) to striatal Muscarinic acetylcholine receptor
- ChEMBL_138784 Concentration of compound for 50% displacement of [3H]QNB from Muscarinic acetylcholine receptor in rat brain
- ChEMBL_138832 Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M3 in transfected CHO cells.
- ChEMBL_138903 In vitro displacement of [3H]oxotremorine-M from muscarinic acetylcholine receptor in rat brain cortex
- ChEMBL_138934 Binding activity against rat muscarinic acetylcholine receptor M1 using [3H]QNB as the radioligand
- ChEMBL_138942 Binding affinity towards Muscarinic acetylcholine receptor M1 using [3H]pirenzepine as radioligand was determined
- ChEMBL_138951 Binding affinity at Muscarinic acetylcholine receptor M1 in Rat brain homogenate by [3H]pirenzepine displacement.
- ChEMBL_138958 Compound was evaluated for its binding affinity towards Muscarinic acetylcholine receptor M1 in rat cortex
- ChEMBL_138961 Binding affinity to m-AcChR subtype Muscarinic acetylcholine receptor M3 of rat sabmandibular glands
- ChEMBL_138978 Binding activity against rat muscarinic acetylcholine receptor M3 using [3H]QNB as the radioligand
- ChEMBL_139075 Displacement of [3H]pirenzepine binding at Muscarinic acetylcholine receptor M1 in rat brain P2 membranes.
- ChEMBL_139238 Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells
- ChEMBL_139243 Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M4 in transfected CHO cells.
- ChEMBL_139311 Inhibition of [3H]- Oxo-M binding to muscarinic acetylcholine receptor of rat brain membrane preparations
- ChEMBL_139312 Inhibition of [3H]- Oxo-M binding to muscarinic acetylcholine receptor of rat heart membrane preparation.
- ChEMBL_139317 The compound was tested for inhibition of [3H]NMS binding against muscarinic acetylcholine receptor in rat brain
- ChEMBL_139320 Inhibition of [3H]OXO-M binding against muscarinic acetylcholine receptor in rat brain membranes
- ChEMBL_139452 Binding activity to the muscarinic acetylcholine receptor in rat cortex, assayed using [3H]CD as a radioligand.
- ChEMBL_139453 Binding activity to the muscarinic acetylcholine receptor in rat cortex, assayed using [3H]PZ as a radioligand.
- ChEMBL_139454 Binding activity against Muscarinic acetylcholine receptor in rat cortex, using [3H]QNB as a radioligand.
- ChEMBL_139456 Binding activity to muscarinic acetylcholine receptor in rat heart, assayed using [3H]-QNB as a radioligand.
- ChEMBL_139462 Binding affinity to muscarinic acetylcholine receptor was determined in presence of [3H]OXO-M radioligand (in vitro)
- ChEMBL_139517 Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M5 in transfected CHO cells.
- ChEMBL_139579 In vitro inhibition of binding of (-)-[3H]-NMS to Muscarinic acetylcholine receptor of rat cerebral cortex was determined
- ChEMBL_139581 In vitro for binding affinity for muscarinic acetylcholine receptors in homogenized rat brain in the presence of [3H]scopolamine.
- ChEMBL_139624 Binding affinity of [3H]QNB to CHO cells expressing human Muscarinic acetylcholine receptor M2
- ChEMBL_139640 Inhibition of [3H]NMS binding to human muscarinic acetylcholine receptor M2 expressed in CHO cells
- ChEMBL_139743 The ability to displace [3H]QNB from Muscarinic acetylcholine receptor in rat brain membrane was determined
- ChEMBL_139744 Binding activity against Muscarinic acetylcholine receptor in rat cortex, using [3H]QNB as a radioligand.
- ChEMBL_139767 Compound was tested for its binding affinity against cloned human Muscarinic acetylcholine receptor M2
- ChEMBL_139782 Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M2 expressed in A9 L cells
- ChEMBL_139858 Binding activity against Muscarinic acetylcholine receptor in rat cortex, using [3H]QNB as a radioligand.
- ChEMBL_139891 Inhibition of [3H]-NMS binding to human muscarinic acetylcholine receptor M2 in transfected CHO cells.
- ChEMBL_140026 Ability to dissociate radioligand [3H]NMS from muscarinic acetylcholine receptor M2 of porcine heart
- ChEMBL_140041 Inhibition of [3H]N-methylscopolamine to rat muscarinic acetylcholine receptor M2 from heart tissue
- ChEMBL_140044 Inhibition of [3H]quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M2 in rat brain membrane
- ChEMBL_140047 Inhibition of [3H]- Oxo-M binding at Muscarinic acetylcholine receptor M2 in rat brain membranes.
- ChEMBL_140157 The compound was evaluated for its ability to inhibit [3H]NMS binding to Muscarinic acetylcholine receptor in heart
- ChEMBL_140174 Binding affinity against Muscarinic acetylcholine receptor M2 by displacement of [3H]QNB in rat myocardium
- ChEMBL_140176 Binding affinity against m-AcChR subtype Muscarinic acetylcholine receptor M2 of rat heart.
- ChEMBL_140182 Inhibition of [3H]N-methylscopolamine binding to Muscarinic acetylcholine receptor M2 of rat heart membranes
- ChEMBL_140187 Compound was evaluated for its binding affinity towards Muscarinic acetylcholine receptor M2 in rat brainstem
- ChEMBL_140188 Compound was evaluated for its binding affinity towards muscarinic acetylcholine receptor M2 in rat brainstem
- ChEMBL_142900 Compound was evaluated for functional potencies and efficacies at rat Nicotinic acetylcholine receptor subtype PC12 (ganglionic)
- ChEMBL_143065 In vitro inhibition of 5-(125I)A-85380 binding to nicotinic acetylcholine receptor (nAChR) of rat brain
- ChEMBL_143715 Binding affinity towards Nicotinic acetylcholine receptor alpha4-beta2 using [3H]nicotine as radioligand
- ChEMBL_143729 Binding affinity towards nicotinic acetylcholine receptor alpha4-beta2 from rat brain homogenates
- ChEMBL_143859 Inhibition of [125I]-analogue binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes
- ChEMBL_143860 Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes
- ChEMBL_143861 Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes
- ChEMBL_143864 Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 from rat membranes
- ChEMBL_143867 Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 in rat brain membranes
- ChEMBL_144167 Compound was evaluated for inhibition of rat Nicotinic acetylcholine receptor alpha-7 (nAChR) in Xenopus Oocytes
- ChEMBL_144177 Binding affinity in rat hippocampi against Nicotinic acetylcholine receptor alpha7; value range is 1000.
- ChEMBL_144185 Inhibition of [125I]MLA binding to Nicotinic acetylcholine receptor alpha7 from rat brain membranes
- ChEMBL_144958 Inhibition of currents when compound wascoapplied with acetylcholine to recombinant Torpedo nAcChoR (from 6 oocytes)
- ChEMBL_144959 Inhibition of currents when compound wascoapplied with acetylcholine to recombinant Torpedo nAcChoR (from 6 oocytes)
- ChEMBL_1588013 Positive allosteric modulation at human muscarinic acetylcholine receptor M1 assessed as effect on receptor internalization
- ChEMBL_1679911 Positive allosteric modulation of rat M4 receptor assessed as increase in acetylcholine-induced calcium mobilization
- ChEMBL_1700417 Displacement of [3H]NMS from human muscarinic acetylcholine receptor M2 expressed in CHOK1 cells
- ChEMBL_1810469 Positive allosteric modulation of M5 AchR (unknown origin) assessed as increase in acetylcholine-induced response
- ChEMBL_1929130 Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium response
- ChEMBL_1929131 Antagonist activity at human muscarinic M1 receptor assessed as inhibition of acetylcholine-induced calcium response
- ChEMBL_1929132 Antagonist activity at human muscarinic M2 receptor assessed as inhibition of acetylcholine-induced calcium response
- ChEMBL_1929133 Antagonist activity at human muscarinic M3 receptor assessed as inhibition of acetylcholine-induced calcium response
- ChEMBL_1929134 Antagonist activity at human muscarinic M4 receptor assessed as inhibition of acetylcholine-induced calcium response
- ChEMBL_1993992 Inhibition of Electric eel AChE using acetylcholine iodide as substrate by spectrophotometry based Ellman's method
- ChEMBL_2130782 Inhibition of electric eel AChE using acetylcholine iodide as a substrate by Cornish-Bowden plot analysis
- ChEMBL_223069 Ability to block activation of acetylcholine-stimulated currents in human alpha-7 homomers expressed in oocytes
- ChEMBL_303326 Inhibition of [3H]-MLA binding to alpha-7 nicotinic acetylcholine receptor of rat brain membrane
- ChEMBL_303385 Inhibition of [3H]MLA binding to alpha4-beta2 nicotinic acetylcholine receptor of rat brain membrane
- ChEMBL_303391 Inhibition of methyllycaconitine (MLA) binding to Nicotinic acetylcholine receptor alpha-7 in rat brain homogenates
- ChEMBL_303459 Inhibition of [3H]nicotine binding to alpha4-beta2 nicotinic acetylcholine receptor of rat brain membrane
- ChEMBL_303479 Inhibition of [3H]nicotine binding to alpha4-beta2 nicotinic acetylcholine receptor of rat brain membrane
- ChEMBL_303546 Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortex
- ChEMBL_303577 Inhibition of [3H]-BTX binding to Nicotinic acetylcholine receptor alpha-7 of rat hippocampal membranes
- ChEMBL_303639 Inhibition of [3H]nicotine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes
- ChEMBL_303640 Inhibition of [3H]- cytisine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes
- ChEMBL_303641 Inhibition of [3H]cytisine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes
- ChEMBL_303642 Inhibition of [3H]cytisine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes
- ChEMBL_303679 Inhibition of [3H]epibatidine binding to Nicotinic acetylcholine receptor alpha4-beta2 of rat cortical membranes
- ChEMBL_303683 Displacement of [3H]-cytisine from Alpha4-beta2 Nicotinic acetylcholine receptor of rat brain homogenates
- ChEMBL_303705 Displacement of [3H]epibatidine from Alpha3 Beta4 Nicotinic acetylcholine receptor of rat brain homogenates
- ChEMBL_304253 Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor (nAChR) expressed in IMR32 cell
- ChEMBL_304254 Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor (nAChR) expressed in IMR32 cell
- ChEMBL_304259 Effective concentration against Nicotinic acetylcholine receptor alpha 7 in rat mid brain slices
- ChEMBL_304286 Effective concentration against alpha3-beta4 nicotinic acetylcholine receptor (nAChR) expressed in Xenopus oocytes
- ChEMBL_305955 Inhibitory concentration against Nicotinic acetylcholine receptor alpha-7 Range is 3-5 nM
- ChEMBL_306141 Inhibitory concentration against Nicotinic acetylcholine receptor alpha4-beta2; Range is 3-5 nM
- ChEMBL_306172 Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta2; Range is 3-5 nM
- ChEMBL_306215 Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta2; Range is 0.5-8 nM
- ChEMBL_306217 Inhibitory concentration against Nicotinic acetylcholine receptor alpha4-beta2; Range is 0.5-8 nM
- ChEMBL_306274 Inhibitory concentration against Nicotinic acetylcholine receptor alpha2-beta2; Range is 0.3-1.5 nM
- ChEMBL_306275 Inhibitory concentration against Nicotinic acetylcholine receptor alpha2-beta4; Range is 0.3-1.5 nM
- ChEMBL_306276 Inhibitory concentration against Nicotinic acetylcholine receptor alpha3-beta2; Range is 0.3-1.5 nM
- ChEMBL_306279 Inhibitory concentration against Nicotinic acetylcholine receptor alpha4-beta2; Range is 0.3-1.5 nM
- ChEMBL_306297 Inhibitory concentration against Nicotinic acetylcholine receptor alpha2-beta4; Range is 0.3-1.5 nM
- ChEMBL_306298 Inhibitory concentration against Nicotinic acetylcholine receptor alpha4-beta2; Range is 0.3-1.5 nM
- ChEMBL_320907 Binding affinity for rat heart muscarinic acetylcholine receptor M2 using [3H]quinuclidinyl benzilate
- ChEMBL_563561 Activity at human alpha7 nAChR expressed in Xenopus oocytes assessed as inhibition of acetylcholine-evoked current
- ChEMBL_563562 Activity at human alpha4beta2 nAChR expressed in Xenopus oocytes assessed as inhibition of acetylcholine-evoked current
- ChEMBL_611542 Displacement of [125I]BTX from rat alpha7 nicotinic acetylcholine receptor expressed in GH4C1 cells
- ChEMBL_611804 Displacement of [125I]BTX from human alpha7 nicotinic acetylcholine receptor expressed in IMR32 cells
- ChEMBL_645015 Displacement of [125I]alpha-bungarotoxin from alpha7 nicotinic acetylcholine receptor in rat brain membrane
- ChEMBL_674712 Inhibition of electric eel AChE after 15 mins by Ellman's method using acetylcholine as substrate
- ChEMBL_792865 Inhibition of equine serum BuChE using acetylcholine as substrate preincubated for 15 mins by Ellman's method
- ChEMBL_828579 Antagonist activity at human muscarinic M2 receptor assessed as inhibition of acetylcholine-induced calcium mobilization
- ChEMBL_830694 Antagonist activity at human muscarinic M5 receptor assessed as inhibition of acetylcholine-induced calcium mobilization
- ChEMBL_830695 Antagonist activity at human muscarinic M4 receptor assessed as inhibition of acetylcholine-induced calcium mobilization
- ChEMBL_830696 Antagonist activity at human muscarinic M3 receptor assessed as inhibition of acetylcholine-induced calcium mobilization
- ChEMBL_908778 Displacement of [3H]IMI from Musca domestica (house fly) brain nicotinic acetylcholine receptor
- ChEMBL_939334 Competitive inhibition of Electrophorus electricus AChE using acetylcholine as substrate by Lineweaver-Burk plot method
- ChEMBL_957891 Competitive inhibition of equine serum BChE by Lineweaver Burk reciprocal plot analysis in presence of acetylcholine
- ChEMBL_960029 Positive allosteric modulation of rat muscarinic M5 receptor assessed as effect on acetylcholine-induced response
- ChEMBL_98931 Compound was tested for its agonist activity against M3-acetylcholine receptor of guinea pig ileum.
- ChEMBL_1700423 Ratio of binding affinity to human muscarinic acetylcholine receptor M2 expressed in CHOK9 cells assessed as dissociation rate constant to binding affinity to human muscarinic acetylcholine receptor M2 expressed in CHOK9 cells assessed as association rate constant
- ChEMBL_1863409 Positive allosteric modulatory activity at rat alpha7 nAChR expressed in GH4C1 cells assessed as potentiation of acetylcholine response at -70 mV holding potential preincubated for 30 secs followed by co-application with acetylcholine by manual patch clamp assay
- ChEMBL_1765196 Positive allosteric modulation of human muscarinic acetylcholine receptor M4 expressed in CHO-K1 cells coexpressing Galphaqi5 assessed as increase in acetylcholine-induced IP accumulation incubated for 16 to 20 hrs measured for 3.5 to 4 mins by FLIPR assay
- ChEMBL_1906149 Induction of desensitization at human alpha7 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine induced current treated with compound prior to 100 uM acetylcholine challenge at -90 mV holding potential by two-electrode voltage clamp method
- ChEBML_138791 Ability to displace [3H]pirenzepine (pir) from muscarinic acetylcholine receptor M1 in rat cortical tissue.
- ChEBML_138949 Binding affinity towards muscarinic acetylcholine receptor M1 in rat heart using [3H]pirenzepine as radioligand
- ChEBML_138964 Inhibition of binding of [3H]N-methylscopolamine to muscarinic acetylcholine receptor M3 of transfected rat A9L cells.
- ChEBML_138979 The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.
- ChEBML_138980 The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.
- ChEBML_139082 Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M1 of transfected A9L cells.
- ChEBML_139202 The compound was tested for binding activity against muscarinic acetylcholine receptor M1, using [3H]QNB as the radioligand.
- ChEBML_139254 Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.
- ChEBML_139764 Binding affinity against human muscarinic acetylcholine receptor M2 using [3H]N-methylscopolamine as radioligand
- ChEBML_140146 Compound was tested for the binding affinity against muscarinic acetylcholine receptor
by using [3H]QNB as radioligand
- ChEBML_140154 Muscarinic acetylcholine receptor binding affinity was determined using [3H]NMS for NG108-15 neuroblastoma cells
- ChEBML_144040 Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes
- ChEMBL_138277 Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
- ChEMBL_138477 Ability to displace [3H]QNB from HM1 receptor binding to acetylcholine was evaluated by ligand inhibition assay
- ChEMBL_138478 Ability to displace [3H]QNB from HM1 receptor binding to acetylcholine was evaluated by ligand inhibition assay
- ChEMBL_138483 Ability to displace [3H]QNB from HM2 receptor binding to acetylcholine was evaluated by ligand inhibition assay
- ChEMBL_138484 Ability to displace [3H]QNB from HM2 receptor binding to acetylcholine was evaluated by ligand inhibition assay
- ChEMBL_138522 Antagonist potency against carbachol induced contractions of isolated guinea pig ileum Muscarinic acetylcholine receptor
- ChEMBL_138523 Antagonist potency against carbachol induced contractions of isolated guinea pig ileum Muscarinic acetylcholine receptor
- ChEMBL_138524 Antagonist potency against carbachol induced contractions of isolated guinea pig ileum Muscarinic acetylcholine receptor
- ChEMBL_138557 Binding affinity against mouse Muscarinic acetylcholine receptor M1 using cerebral cortex and [3H]pirenzepine
- ChEMBL_138558 Binding affinity against mouse muscarinic acetylcholine receptor M1 using cerebral cortex and [3H]pirenzepine
- ChEMBL_138662 Binding affinity against Muscarinic acetylcholine receptor was measured using radioligand ([3H]QNB) binding assay
- ChEMBL_138764 Binding affinity was determined against Muscarinic acetylcholine receptor using [3H]QNB as radioligand in rat brain.
- ChEMBL_138772 In vitro ability to displace [3H]quinuclidinyl benzilate (QNB) from rat cerebral cortexMuscarinic acetylcholine receptor
- ChEMBL_138788 In Vitro binding affinity to the muscarinic acetylcholine receptor site in rat brain by using [3H]QNB as the radioligand.
- ChEMBL_138802 Displacement of [3H]oxotremorine-M (Oxo-M) from rat hippocampus muscarinic acetylcholine receptor M1
- ChEMBL_138812 Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]-Pz as the radioligand.
- ChEMBL_138949 Binding affinity towards muscarinic acetylcholine receptor M1 in rat heart using [3H]pirenzepine as radioligand
- ChEMBL_138966 Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M3 in rat cerebral cortical membranes
- ChEMBL_138980 The compound was tested for binding activity against muscarinic acetylcholine receptor M3, using [3H]-QNB as the radioligand.
- ChEMBL_139078 Inhibition of binding of [3H]oxotremorine M to Muscarinic acetylcholine receptor M1 in rat cerebral cortical membranes
- ChEMBL_139079 Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M1 in rat cerebral cortical membranes
- ChEMBL_139082 Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M1 of transfected A9L cells.
- ChEMBL_139125 Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M4 in CHO cell membranes
- ChEMBL_139126 Inhibition of [3H]- quinuclidinyl benzilate binding to Muscarinic acetylcholine receptor M4 expressed in CHO cell membranes
- ChEMBL_139202 The compound was tested for binding activity against muscarinic acetylcholine receptor M1, using [3H]QNB as the radioligand.
- ChEMBL_139239 Inhibitory activity was evaluated against Muscarinic acetylcholine receptor M4 expressed in A9 L cells; Not determined
- ChEMBL_139253 Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M4 in rat cerebral cortical membranes
- ChEMBL_139254 Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M4 of NG108-15 cells.
- ChEMBL_139458 Binding affinity against Muscarinic acetylcholine receptor using [3H]oxotremorine-M as radioligand in rat cortex
- ChEMBL_139460 Binding affinity against Muscarinic acetylcholine receptors using [3H]oxotremorine-M as radioligand in rat cortex
- ChEMBL_139634 Inhibitory activity against [3H]quinuclidinyl Benzilate binding to Muscarinic acetylcholine receptor M2 in the absence of GTP
- ChEMBL_139635 Inhibitory activity against [3H]quinuclidinyl Benzilate binding to Muscarinic acetylcholine receptor M2 in the presence of GTP
- ChEMBL_140197 Inhibition of binding of [3H]quinuclidinyl benzilate to Muscarinic acetylcholine receptor M2 in rat cerebral cortical membranes
- ChEMBL_142599 Compound was evaluated for functional potencies and efficacies at human Nicotinic acetylcholine receptor subtype IMR-32 (ganglionic)
- ChEMBL_142603 Compound was evaluated for functional potency and efficacy at human muscle type Nicotinic acetylcholine receptor in TE671 cells
- ChEMBL_142765 Binding affinity towards Nicotinic acetylcholine receptor by the displacement of [3H]-nicotine from rat cortical membranes
- ChEMBL_142899 The compound was tested for the inhibition of binding of [3H]epibatidine to central nicotinic acetylcholine receptor (nAChR) in rat brain.
- ChEMBL_1432884 Inhibition of AChE (unknown origin) assessed as inhibition of acetylcholine hydrolysis preincubated for 15 mins by Ellman method
- ChEMBL_143392 Antagonism of ACh-evoked responses at human Nicotinic acetylcholine receptor alpha3-beta4 expressed in xenopus oocytes
- ChEMBL_143402 Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha3-beta4 expressed in Xenopus oocytes
- ChEMBL_143704 Inhibition of binding of [3H]nicotine to Nicotinic acetylcholine receptor alpha4-beta2 in rat cerebral cortical membranes
- ChEMBL_143717 Inhibition of [3H]epibatidine binding at the nicotinic acetylcholine receptor alpha4-beta2 in male rat cerebral cortex
- ChEMBL_143719 Inhibition of [3H]pibatidine binding at the nicotinic acetylcholine receptor alpha4-beta2 in male rat cerebral cortex
- ChEMBL_143721 Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta2 expressed in Xenopus oocytes
- ChEMBL_143727 Binding affinity to Nicotinic acetylcholine receptor alpha4-beta2 using +/-[3H]epibatidine as radioligand in rat brain
- ChEMBL_143879 Binding affinity at heteropentameric Nicotinic acetylcholine receptor alpha4-beta2 subtype using [3H]bungarotoxin as radioligand
- ChEMBL_1439748 Inhibition of acetylcholinesterase (unknown origin) assessed as inhibition of acetylcholine hydrolysis after 30 mins by Ellmann's method
- ChEMBL_144014 Functional potency measured as stimulation at rat Nicotinic acetylcholine receptor alpha4-beta4 expressed in Xenopus oocytes
- ChEMBL_144025 Receptor activation after 10 uM application and 300 uM of ACh for Nicotinic acetylcholine receptor alpha7
- ChEMBL_144026 Receptor activation after 100 uM application and 300 uM of ACh for Nicotinic acetylcholine receptor alpha7
- ChEMBL_144040 Activation responses to that evoked by ACh at human Nicotinic acetylcholine receptor alpha-7 expressed in xenopus oocytes
- ChEMBL_144043 Potency was determined by measuring current activation in Xenopus oocytes expressing rat Nicotinic acetylcholine receptor alpha7
- ChEMBL_144180 Binding affinity to subtype Nicotinic acetylcholine receptor alpha7 using [3H]-MLA as radioligand in rat brain
- ChEMBL_1457825 Activity at human muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
- ChEMBL_1457827 Activity at human muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
- ChEMBL_1457828 Activity at rat muscarinic acetylcholine receptor subtype 5 expressed in CHO cells by calcium mobilization assay
- ChEMBL_1457830 Activity at rat muscarinic acetylcholine receptor subtype 3 expressed in CHO cells by calcium mobilization assay
- ChEMBL_1457832 Activity at rat muscarinic acetylcholine receptor subtype 1 expressed in CHO cells by calcium mobilization assay
- ChEMBL_1520448 Agonist activity at mouse neuronal acetylcholine receptor subunit alpha4beta2 expressed in HEK293T cells by FMP assay
- ChEMBL_1520450 Agonist activity at rat neuronal acetylcholine receptor subunit alpha3beta4 expressed in HEK293 cells by FMP assay
- ChEMBL_1588012 Positive allosteric modulation at human muscarinic acetylcholine receptor M1 assessed as effect on beta-arrestin recruitment
- ChEMBL_1984257 Inhibition of Electrophorus electricus AChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method
- ChEMBL_1993994 Inhibition of AChE (unknown origin) using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method
- ChEMBL_2032522 Inhibition of human serum BuChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method
- ChEMBL_2032523 Inhibition of human erythrocytes AChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method
- ChEMBL_2032526 Inhibition of Electrophorus electricus AChE using acetylcholine iodide as substrate incubated for 15 mins by Ellman's method
- ChEMBL_303295 Inhibition of [125I]-iodo-MLA binding to Nicotinic acetylcholine receptor alpha-7 of rat cerebral cortex
- ChEMBL_303475 Inhibition of [125I]-iodo-MLA binding to Nicotinic acetylcholine receptor alpha-7 in rat cerebral cortex
- ChEMBL_303631 Inhibition of [125I]alpha-bungarotoxin binding to nicotinic acetylcholine receptor alpha1 beta gamma delta of electroplax
- ChEMBL_303690 Inhibition of [3H](-)-nicotine binding to rat brain (minus cerebellum) Nicotinic acetylcholine receptor alpha4-beta2
- ChEMBL_303782 Inhibition of 3 nM [3H]-MLA binding to Nicotinic acetylcholine receptor alpha7 of rat brain membranes
- ChEMBL_310608 Potency against rat nicotinic acetylcholine alpha-7 subunit expressed in Xenopus oocytes as current activation
- ChEMBL_320917 Binding affinity for rat salivary gland muscarinic acetylcholine receptor M3 using [3H]N-methylscopolamine
- ChEMBL_320958 Binding affinity for rat brain Nicotinic acetylcholine receptor alpha4-beta2 using [3H]S-(-)-nicotine
- ChEMBL_546015 Displacement of (+/-)-[3H]epibatidine from alpha4beta2 nicotinic acetylcholine receptor in rat brain cortex membrane homogenates
- ChEMBL_546017 Displacement of [3H]cytisine from alpha4beta2 nicotinic acetylcholine receptor in rat brain cortex membrane homogenates
- ChEMBL_546018 Displacement of [3H]cytisine from alpha4beta2 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane
- ChEMBL_546019 Displacement of [3H]A585539 from alpha7 nicotinic acetylcholine receptor in rat brain minus cerebellum membrane
- ChEMBL_769761 Displacement of [3H]QNB from muscarinic acetylcholine M5 receptor after 1.5 hrs by scintillation counting
- ChEMBL_792862 Inhibition of electric eel AChE using acetylcholine chloride as substrate preincubated for 15 mins by Ellman's method
- ChEMBL_851712 Inhibition of electric eel AChE using acetylcholine iodide as substrate preincubated for 20 mins by Ellman's method
- ChEMBL_909515 Inhibition of Electrophorus electricus (electric eel) acetylcholinesterase (AChE) using acetylcholine iodide as substrate by Ellman method
- ChEMBL_939332 Non-competitive inhibition of Electrophorus electricus AChE using acetylcholine as substrate by Lineweaver-Burk plot method
- ChEMBL_948622 Inhibition of electric eel AChE using acetylcholine iodide as substrate after 10 mins by Ellman method
- ChEMBL_957892 Mixed-type inhibition of electric eel AChE by Lineweaver Burk reciprocal plot analysis in presence of acetylcholine
- ChEMBL_1780191 Positive allosteric modulation of rat M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
- ChEMBL_1780193 Positive allosteric modulation of human M1 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
- ChEMBL_1780206 Positive allosteric modulation of human M3 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
- ChEMBL_1780208 Positive allosteric modulation of human M5 receptor expressed in CHO cells assessed as increase in acetylcholine-induced calcium mobilization pretreated for 2.5 mins followed by acetylcholine addition and measured after 1 min by Fluo-4-AM dye based assay
- Cell-Based Functional Assay (M1) Muscarinic acetylcholine receptor M1 was cloned into an expression vector and transfected in CHO cells along with CRE-Luc reporter system. Isolated colonies were screened with 10,000 nM acetylcholine. Clones exhibiting highest acetylcholine dependent reporter gene induction were utilized in the evaluation of known and novel compounds. Increasing concentrations of the compound were incubated with or without 10,000 nM acetylcholine for antagonist or agonist mode, respectively, for 5 h in 96 well plate. After incubation, cells were harvested, lysed and reporter gene activity was determined.
- ChEMBL_935572 Positive allosteric modulation of human muscarinic M5 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
- ChEMBL_935574 Positive allosteric modulation of human muscarinic M3 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
- ChEMBL_935578 Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
- ChEMBL_935583 Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
- ChEMBL_935591 Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization assay
- ChEBML_131447 Binding affinity against mouse Muscarinic acetylcholine receptor M2 using heart tissue and [3H]N-methylscopolamine
- ChEBML_140039 Binding affinity against mouse Muscarinic acetylcholine receptor M2 using heart tissue and [3H]N-methylscopolamine
- ChEMBL_1355059 Mixed-type inhibition of horse serum butyrylcholinesterase using acetylcholine bromide as substrate by Lineweaver-Burk plot analysis
- ChEMBL_138128 Inhibition of [3H]NMS binding to cerebral cortex membranes which contain predominantly the muscarinic acetylcholine receptor M1
- ChEMBL_138163 Inhibition of binding of [3H]N-Methyl-scopolamine to Muscarinic acetylcholine receptor M2 of rat heart tissue membranes.
- ChEMBL_138416 Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M1 expressed in CHO cell membranes
- ChEMBL_138683 Compound was tested in vitro for depolarizing response on the rat superior cervical ganglion (mediated by muscarinic acetylcholine receptor M1)
- ChEMBL_138710 Inhibition of [3H]- quinuclidinyl benzilate binding to human Muscarinic acetylcholine receptor M3 expressed in CHO cell membranes
- ChEMBL_138769 In vitro ability to displace [3H]quinuclidinyl benzilate (QNB) from rat cerebral cortex Muscarinic acetylcholine receptor
- ChEMBL_138770 In vitro ability to displace [3H]quinuclidinyl benzilate (QNB) from rat cerebral cortex muscarinic acetylcholine receptor
- ChEMBL_138811 Binding activity against muscarinic acetylcholine receptor M1 in rat brain, using [3H]OXO-M as the radioligand.
- ChEMBL_139468 Compound was tested for the concentration that inhibited the specific binding of (-)-[3H]-NMS to muscarinic acetylcholine receptor in the rat cerebral cortex.
- ChEMBL_139769 Inhibition of [3H]- oxotremorine-M binding to human Muscarinic acetylcholine receptor M2 expressed in CHO cell membranes
- ChEMBL_140039 Binding affinity against mouse Muscarinic acetylcholine receptor M2 using heart tissue and [3H]N-methylscopolamine
- ChEMBL_140052 Inhibitory activity against [3H]N-methyl-scopolamine binding to Muscarinic acetylcholine receptor M2 in rat cerebellum
- ChEMBL_140193 Compound was tested for the binding affinity against rat heart Muscarinic acetylcholine receptor M2 by quinuclidinyl binding assay.
- ChEMBL_144327 Binding affinity at homopentameric Nicotinic acetylcholine receptor alpha-7 subtype using [3H]S-(-)-nicotine as radioligand
- ChEMBL_1872177 Positive allosteric modulation of Gqi5-fused human M4 AChR assessed as increase in acetylcholine-induced calcium mobilization
- ChEMBL_310669 Change in membrane potential in K-177 cells expressing acetylcholine central neuronal receptor alpha4-beta2 subunits
- ChEMBL_457604 Inhibition of alpha4beta2 nAchR expressed in Xenopus laevis oocytes assessed as acetylcholine-induced current by voltage-clamp method
- ChEMBL_815845 Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M1 receptor expressed in CHO cell membrane
- ChEMBL_815846 Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M2 receptor expressed in CHO cell membrane
- ChEMBL_815847 Displacement of [3H]-N-methyl scopolamine from muscarinic acetylcholine M3 receptor expressed in CHO cell membrane