Arginine Vasopressin Leiormone BDBM50044777 CHEBI:34543 Vasophysin Beta-Hypophamine Pitressin Vasopressin
BDBM50166222 Vasopressin Analogue CHEMBL410673
BDBM50166223 Vasopressin Analogue CHEMBL265137
BDBM50166224 Vasopressin Analogue CHEMBL410567
CHEMBL408657 BDBM50166221 Vasopressin Analogue
CHEMBL439430 Vasopressin Analogue BDBM50166227
Vasopressin Analogue CHEMBL264101 BDBM50166219
Vasopressin Analogue CHEMBL410401 BDBM50166225
CHEMBL373742 [3H]vasopressin BDBM35667 [3H]Arginine vasopressin US10131692, 44 (AVP) AVP [3H]Argipressin tannate
BDBM50016309 [Phe2Sar7]AVP (Arginine-vasopressin ) CHEMBL410025
BDBM50016313 [Val4Sar7]AVP (Arginine-vasopressin ) CHEMBL217517
BDBM50016315 [Val4MeAla7]AVP (Arginine-vasopressin ) CHEMBL437631
BDBM50016317 CHEMBL2371674 [Mpa1Val4MeAla7]AVP (Arginine-vasopressin )
CHEMBL265119 [Sar7D-Arg8]VP (Vasopressin ) BDBM50016312
CHEMBL267405 8-arginine vasopressin trisulphide BDBM50291329
CHEMBL406303 BDBM50016310 [Mpa1Val4Sar7]AVP (Arginine-vasopressin )
CHEMBL413706 BDBM50016316 [Phe2MeAla7]AVP (Arginine-vasopressin )
[MeAla7D-Arg8]VP (Vasopressin ) CHEMBL269715 BDBM50016314
[Mpa1Sar7,Drg8]VP (Vasopressin ) CHEMBL413249 BDBM50016311
BDBM50016318 [Mpa1,MeAla7,D-Arg8]VP (Vasopressin ) CHEMBL411357
1-[19-Amino-13-benzyl-10-(2-carbamoyl-ethyl)-7-carbamoylmethyl-16-(4-hydroxy-benzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaaza-cycloicosane-4-carbonyl]-pyrrolidine-2-carboxylic acid [1-(carbamoylmethyl-carbamoyl)-4-guanidino-butyl]-amide 8-arginine vasopressin cyclo[Cys-Tyr-Phe-Gln-Asn-Cys]-Pro-Arg-Gly-NH2 AVP (Arginine-vasopressin ) Arginine-vasopressin (AVP) [2-({1-[19-Amino-13-benzyl-10-(2-carbamoyl-ethyl)-7-carbamoylmethyl-16-(4-hydroxy-benzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaaza-cycloicosane-4-carbonyl]-pyrrolidine-2-carbonyl}-amino)-5-guanidino-pentanoylamino]-acetic acid(AVP) CHEMBL264048 BDBM50291330
BDBM50205291 CHEMBL376685 (S)-1-((4R,7S,10S,13S,16S)-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-benzyl-16-(4-hydroxybenzyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl)-N-((S)-1-(2-amino-2-oxoethylamino)-5-guanidino-1-oxopentan-2-yl)pyrrolidine-2-carboxamide deamino-[Cys1]arginine vasopressin
Vasopressin Analogue (2S)-2-[(2S)-2-[(2R)-2-azaniumyl-3-(4-benzoylphenyl)propanamido]-3-phenylpropanamido]-N-[(1S)-2-carbamoyl-1-{[(2S)-1-[(2R)-2-{[(1S)-1-{[(1S)-1-carbamoyl-2-(4-hydroxy-3-iodophenyl)ethyl]carbamoyl}-4-[(diaminomethylidene)amino]butyl]carbamoyl}pyrrolidin-1-yl]-5-[(diaminomethylidene)amino]-1-oxopentan-2-yl]carbamoyl}ethyl]pentanediamide BDBM50166218
Vasopressin Analogue (2S)-2-[(2S)-2-[(2S)-2-azaniumyl-3-(4-benzoylphenyl)propanamido]-3-phenylpropanamido]-N-[(1S)-2-carbamoyl-1-{[(2S)-1-[(2R)-2-{[(1S)-1-{[(1S)-1-carbamoyl-2-(4-hydroxy-3-iodophenyl)ethyl]carbamoyl}-4-[(diaminomethylidene)amino]butyl]carbamoyl}pyrrolidin-1-yl]-5-[(diaminomethylidene)amino]-1-oxopentan-2-yl]carbamoyl}ethyl]pentanediamide BDBM50166220
Vasopressin Analogue BDBM50166226 (2S)-2-[(2S)-2-[(2R)-2-[2-azaniumyl-3-(4-benzoylphenyl)propanamido]-3-(4-methoxyphenyl)propanamido]-3-phenylpropanamido]-N-[(1S)-2-carbamoyl-1-{[(2S)-1-[(2R)-2-{[(1S)-1-{[(1S)-1-carbamoyl-2-(4-hydroxy-3-iodophenyl)ethyl]carbamoyl}-4-[(diaminomethylidene)amino]butyl]carbamoyl}pyrrolidin-1-yl]-5-[(diaminomethylidene)amino]-1-oxopentan-2-yl]carbamoyl}ethyl]pentanediamide
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- Napier, SE; Letourneau, JJ; Ansari, N; Auld, DS; Baker, J; Best, S; Campbell-Wan, L; Chan, R; Craighead, M; Desai, H; Ho, KK; MacSweeney, C; Milne, R; Richard Morphy, J; Neagu, I; Ohlmeyer, MH; Pick, J; Presland, J; Riviello, C; Zanetakos, HA; Zhao, J; Webb, ML Synthesis and SAR studies of novel 2-(6-aminomethylaryl-2-aryl-4-oxo-quinazolin-3(4H)-yl)acetamide vasopressin V1b receptor antagonists. Bioorg Med Chem Lett 21: 3813-7 (2011)
- Kakefuda, A; Suzuki, T; Tobe, T; Tsukada, J; Tahara, A; Sakamoto, S; Tsukamoto, S Synthesis and pharmacological evaluation of 5-(4-biphenyl)-3-methyl-4-phenyl-1,2,4-triazole derivatives as a novel class of selective antagonists for the human vasopressin V(1A) receptor. J Med Chem 45: 2589-98 (2002)
- Tsukamoto, I; Koshio, H; Kuramochi, T; Saitoh, C; Yanai-Inamura, H; Kitada-Nozawa, C; Yamamoto, E; Yatsu, T; Shimada, Y; Sakamoto, S; Tsukamoto, S Synthesis and structure-activity relationships of amide derivatives of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetic acid as selective arginine vasopressin V2 receptor agonists. Bioorg Med Chem 17: 3130-41 (2009)
- Aranapakam, V; Albright, JD; Grosu, GT; Chan, PS; Coupet, J; Saunders, T; Ru, X; Mazandarani, H 4,10-dihydro-5H-thieno[3,2-c][1]benzazepine derivatives and 9,10-dihydro-4H-thieno[2,3-c][1]benzazepine derivatives as orally active arginine vasopressin receptor antagonists. Bioorg Med Chem Lett 9: 1733-6 (1999)
- Aranapakam, V; Albright, JD; Grosu, GT; Delos Santos, EG; Chan, PS; Coupet, J; Ru, X; Saunders, T; Mazandarani, H 5-fluoro-2-methyl-N-[5-(5H-pyrrolo[2,1-c][1,4]benzodiazepine-10(11H)-yl carbonyl)-2-pyridinyl]benzamide (CL-385004) and analogs as orally active arginine vasopressin receptor antagonists. Bioorg Med Chem Lett 9: 1737-40 (1999)
- Kondo, K; Ogawa, H; Yamashita, H; Miyamoto, H; Tanaka, M; Nakaya, K; Kitano, K; Yamamura, Y; Nakamura, S; Onogawa, T; Mori, T; Tominaga, M 7-Chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoyl-amino)benzoyl ]-2,3,4,5-tetrahydro-1H-1-benzazepine (OPC-41061): a potent, orally active nonpeptide arginine vasopressin V2 receptor antagonist. Bioorg Med Chem 7: 1743-54 (1999)
- Albright, JD; Reich, MF; Delos Santos, EG; Dusza, JP; Sum, FW; Venkatesan, AM; Coupet, J; Chan, PS; Ru, X; Mazandarani, H; Bailey, T 5-Fluoro-2-methyl-N-[4-(5H-pyrrolo[2,1-c]-[1, 4]benzodiazepin-10(11H)-ylcarbonyl)-3-chlorophenyl]benzamide (VPA-985): an orally active arginine vasopressin antagonist with selectivity for V2 receptors. J Med Chem 41: 2442-4 (1998)
- Kondo, K; Kan, K; Tanada, Y; Bando, M; Shinohara, T; Kurimura, M; Ogawa, H; Nakamura, S; Hirano, T; Yamamura, Y; Kido, M; Mori, T; Tominaga, M Characterization of orally active nonpeptide vasopressin V(2) receptor agonist. Synthesis and biological evaluation of both the (5R)- and (5S)-enantioisomers of 2-[1-(2-Chloro-4-pyrrolidin-1-yl-benzoyl)-2,3,4,5-tetrahydro-1H-1-benzazepin- 5-yl]-N-isopropylacetamide. J Med Chem 45: 3805-8 (2002)
- Serradeil-Le Gal, C; Wagnon, J; Simiand, J; Griebel, G; Lacour, C; Guillon, G; Barberis, C; Brossard, G; Soubrié, P; Nisato, D; Pascal, M; Pruss, R; Scatton, B; Maffrand, JP; Le Fur, G Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist. J Pharmacol Exp Ther 300: 1122-30 (2002)
- ChEMBL_661591 Displacement of [3H]vasopressin from human vasopressin V2 receptor
- ChEMBL_821173 Displacement of [3H]vasopressin from human vasopressin V1a receptor
- ChEMBL_821174 Displacement of [3H]vasopressin from human vasopressin V1b receptor
- ChEMBL_821175 Displacement of [3H]vasopressin from human vasopressin V2 receptor
- ChEMBL_214549 Inhibition of binding of [3H]vasopressin to rat liver vasopressin V1a receptor
- ChEMBL_214877 Inhibition of binding of [3H]vasopressin to rat kidney vasopressin V2 receptor
- ChEMBL_214384 Inhibition of [3H]arginine vasopressin binding to rat liver Vasopressin V1 receptor
- ChEMBL_214407 Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V1a receptor
- ChEMBL_214713 Inhibition of [3H]Arg-vasopressin binding to recombinant human vasopressin V2 receptor
- ChEMBL_661538 Displacement of [3H]vasopressin from vasopressin V1a receptor in human liver tissue
- ChEMBL_661539 Displacement of [3H]vasopressin from vasopressin V1a receptor in rat liver tissue
- ChEMBL_661540 Displacement of [3H]vasopressin from vasopressin V2 receptor in human kidney tissue
- ChEMBL_661541 Displacement of [3H]vasopressin from vasopressin V2 receptor in rat kidney tissue
- ChEBML_211078 Half-maximal inhibition of binding of [3H]vasopressin to vasopressin receptor 1 in rat liver
- ChEBML_211248 Half-maximal inhibition of binding of [3H]- vasopressin to the vasopressin receptor 2 in rat kidney
- ChEBML_214881 Compound was evaluated for half-maximal inhibition of binding of [3H]vasopressin to Vasopressin V2 receptor
- ChEBML_215028 Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
- ChEMBL_214546 Compound was tested for its ability to displace vasopressin from human Vasopressin V1a receptor
- ChEMBL_215028 Inhibition of [3H]arginine vasopressin binding to rat kidney medulla Vasopressin V2 receptor
- ChEMBL_661553 Displacement of [3H]vasopressin from human vasopressin V1a receptor expressed in CHO cells
- ChEMBL_661557 Displacement of [3H]vasopressin from rat vasopressin V1a receptor expressed in CHO cells
- ChEMBL_661558 Displacement of [3H]vasopressin from rat vasopressin V2 receptor expressed in CHO cells
- ChEMBL_661559 Displacement of [3H]vasopressin from human vasopressin V2 receptor expressed in CHO cells
- ChEMBL_661572 Displacement of [3H]vasopressin from rat vasopressin V1b receptor expressed in CHO cells
- ChEMBL_661576 Displacement of [3H]vasopressin from human vasopressin V1b receptor expressed in CHO cells
- ChEBML_215042 Compound was tested for its ability to inhibit binding of arginine vasopressin to Vasopressin receptor (V1 subtype)
- ChEMBL_451555 Activity at vasopressin V1A receptor
- ChEBML_214852 Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
- ChEBML_214867 Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
- ChEMBL_1472815 Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V1a receptor transfected in CHO cell membranes
- ChEMBL_1472817 Displacement of [3H]-(Arg8)-vasopressin from human vasopressin V2 receptor transfected in CHO cell membranes
- ChEMBL_214852 Inhibition constant for vasopressin-stimulated adenylate cyclase (Vasopressin V2 receptor) of medullary membranes of human kidney
- ChEMBL_214867 Inhibition constant for vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney (Vasopressin V2 receptor)
- ChEMBL_458590 Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_458592 Displacement of [3H]Arg-vasopressin from human recombinant vasopressin V2 receptor expressed in HEK293 cells
- ChEMBL_661560 Displacement of [3H]vasopressin from human vasopressin V1a receptor expressed in CHO cells at 10 uM
- ChEMBL_578261 Antagonist activity at vasopressin V1a receptor in phenoxybenzamine-treated Wistar rat uterus assessed as inhibition of vasopressin-induced arterial vasopressor activity treated 1 min prior to vasopressin challenge
- ChEMBL_1473356 Displacement of [3H]-vasopressin from human vasopressin 1b receptor after 1 hr by scintillation proximity assay
- ChEMBL_211099 Inhibition of human V1A vasopressin receptor
- ChEMBL_329920 Binding affinity to vasopressin 1 receptor
- ChEMBL_329921 Binding affinity to vasopressin 2 receptor
- ChEMBL_485639 Binding affinity to vasopressin V1a receptor
- ChEMBL_513958 Antagonist activity at vasopressin V1a receptor
- ChEMBL_513960 Antagonist activity at vasopressin V2 receptor
- ChEMBL_651957 Antagonist activity at vasopressin 1a receptor
- ChEMBL_651958 Antagonist activity at vasopressin 2 receptor
- ChEMBL_864208 Binding affinity to vasopressin V2 receptor
- ChEMBL_864209 Binding affinity to vasopressin V1a receptor
- ChEMBL_798001 Displacement of [3H]arginine-vasopressin from human Vasopressin V1a receptor after 30 mins by liquid scintillation counter
- ChEMBL_458595 Antagonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
- ChEMBL_458598 Antagonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced cAMP levels
- ChEMBL_1726377 Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin-induced IP1 accumulation preincubated for 30 mins followed by vasopressin addition measured after 1 hr by HTRF assay
- ChEMBL_1865147 Antagonist activity at human vasopressin V2R receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated cAMP level treated with compound for 30 mins followed by vasopressin stinulation for 30 mins by microplate reader assay
- ChEBML_214391 Negative log of Kd for Vasopressin V1 receptor
- ChEMBL_1644277 Antagonist activity at human vasopressin 1a receptor
- ChEMBL_214391 Negative log of Kd for Vasopressin V1 receptor
- ChEMBL_214413 Binding affinity for human Vasopressin V1a receptor
- ChEMBL_304151 Effective concentration for human Vasopressin V2 receptor
- ChEMBL_465439 Binding affinity to human vasopressin V1a receptor
- ChEMBL_465440 Binding affinity to human vasopressin V1b receptor
- ChEMBL_465441 Binding affinity to human vasopressin V2 receptor
- ChEMBL_615225 Antagonist activity at human vasopressin V1A receptor
- ChEMBL_798003 Binding affinity to human vasopressin V2 receptor
- ChEMBL_458594 Antagonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
- ChEMBL_458597 Antagonist activity at rat vasopressin V1a receptor expressed in HEK293 cells assessed as inhibition of Arg-vasopressin-induced intracellular calcium level
- ChEMBL_590264 Displacement of [3H]Arg8-vasopressin from rat vasopressin V1a receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
- ChEMBL_590267 Displacement of [3H]Arg8-vasopressin from human vasopressin V1b receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
- ChEMBL_590268 Displacement of [3H]Arg8-vasopressin from rat vasopressin V1b receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
- ChEMBL_590269 Displacement of [3H]Arg8-vasopressin from human vasopressin V1a receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
- ChEMBL_590270 Displacement of [3H]Arg8-vasopressin from human vasopressin V2 receptor expressed in CHO-K1 cells by Packard Topcount scintillation counter
- ChEMBL_1473355 Displacement of [3H]-vasopressin from human vasopressin 1a receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
- ChEMBL_1473358 Displacement of [3H]-vasopressin from mouse vasopressin 1a receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
- ChEMBL_1473359 Displacement of [3H]-vasopressin from human vasopressin V2 receptor expressed in HEK293 cell membranes after 1 hr by scintillation proximity assay
- ChEMBL_1726374 Displacement of [3H]-vasopressin from human vasopressin V1a receptor expressed in HEK293 cell membranes after 90 mins by radioligand binding assay
- ChEMBL_651956 Antagonist activity at human vasopressin 1b receptor expressed in CHO cells assessed as inhibition of vasopressin-induced intracellular calcium mobilization by FLPR assay
- ChEBML_215037 Binding affinity against Vasopressin receptor in rat liver
- ChEMBL_1555994 Binding affinity to vasopressin 1a receptor (unknown origin)
- ChEMBL_1750004 Agonist activity at vasopressin 1a receptor (unknown origin)
- ChEMBL_214573 Binding affinity towards human Vasopressin V1b receptor
- ChEMBL_214719 Binding affinity towards human Vasopressin V2 receptor
- ChEMBL_214878 Binding affinity towards rat Vasopressin V2 receptor
- ChEMBL_215037 Binding affinity against Vasopressin receptor in rat liver
- ChEMBL_302470 Binding affinity against rat vasopressin V1a receptor
- ChEMBL_540355 Binding affinity to vasopressin V1a receptor by filtration assay
- ChEMBL_540356 Binding affinity to vasopressin V1b receptor by filtration assay
- ChEMBL_540357 Binding affinity to vasopressin V2 receptor by filtration assay
- ChEMBL_658589 Binding affinity to human recombinant vasopressin V1a receptor
- ChEMBL_658590 Binding affinity to human recombinant vasopressin V2 receptor
- ChEMBL_1555981 Displacement of [3H]-vasopressin from human vasopressin 1a receptor expressed in HEK293 cells after 90 mins by microbeta 2 microplate-reader method
- ChEMBL_1724091 Displacement of [3H]-vasopressin from human vasopressin 1a receptor expressed in HEK293 cell membranes after 90 mins by microbeta scintillation counting method
- ChEMBL_1665974 Displacement of [3H] (Arg8)-vasopressin from human vasopressin V2 receptor expressed in CHOK1 cell membranes after 2 hrs by liquid scintillation counting method
- ChEBML_214557 Evaluated for binding affinity towards vasopressin V1a receptor in rat
- ChEBML_214866 Binding affinity towards Vasopressin V2 receptor in LLCPK cells
- ChEBML_215010 Evaluated for binding affinity towards vasopressin V2 receptor in rat
- ChEMBL_214393 Compound was evaluated for antagonistic activity against vasopressin V1 receptor
- ChEMBL_214394 Ability to displace [3H]AVP from vasopressin V1 receptor
- ChEMBL_214415 Binding affinity towards Vasopressin V1a receptor in human liver
- ChEMBL_214558 Evaluated for binding affinity towards vasopressin receptor V1a in rat
- ChEMBL_214562 Binding affinity towards Vasopressin V1a receptor in rat liver
- ChEMBL_214866 Binding affinity towards Vasopressin V2 receptor in LLCPK cells
- ChEMBL_215025 Vasopressin V2 receptor antagonistic activity in vivo in anesthetized rats
- ChEMBL_215029 Ability to displace [3H]AVP from Vasopressin V2 receptor
- ChEMBL_215036 Binding affinity against Vasopressin receptor in rat kidney medulla
- ChEMBL_321075 Displacement of [3H]oxytocin from human V2 vasopressin receptor
- ChEMBL_321076 Displacement of [3H]oxytocin from human V1b vasopressin receptor
- ChEMBL_321077 Displacement of [3H]oxytocin from human V1a vasopressin receptor
- ChEMBL_634856 Displacement [3H]Arg human recombinant Vasopressin V1a receptor
- ChEMBL_634857 Displacement [3H]Arg human recombinant Vasopressin V2 receptor
- ChEMBL_652648 Displacement of [3H]AVP from rat vasopressin V3 receptor
- ChEMBL_652650 Displacement of [3H]AVP from human vasopressin V2 receptor
- ChEMBL_727046 Displacement of [3H]AVP from human vasopressin V2 receptor
- ChEMBL_214261 Inhibition of [3H]AVP binding to recombinant human vasopressin V2 receptor
- ChEMBL_214388 Binding potency against Vasopressin V1 receptor in rat liver cells.
- ChEMBL_214395 Ability to displace [3H]arginine vasopressin in cloned human V1a receptor
- ChEMBL_214540 Inhibition of [3H]AVP binding to recombinant human vasopressin V1a receptor
- ChEMBL_214543 Inhibition of [3H]AVP binding to recombinant human vasopressin V1a receptor
- ChEMBL_214695 Ability to displace [3H]arginine vasopressin in cloned human V2 receptor
- ChEMBL_214876 Binding affinity against Vasopressin V2 receptor was determined in Brattleboro rats
- ChEMBL_941875 Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
- ChEBML_214416 Binding affinity towards human Vasopressin V1a receptor by using functional assay
- ChEBML_214555 Inhibition of [3H]AVP binding to Dawley rat hepatic vasopressin V1a receptor.
- ChEBML_214700 Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
- ChEMBL_214400 Inhibition of vasopressin induced calcium immobilization in human V1a receptor expressing cells
- ChEMBL_214700 Inhibition of vasopressin induced cAMP accumulation in human V2 receptor expressing cells
- ChEMBL_215035 Tested for inhibition of vasopressin-stimulated adenylate cyclase of medullary membranes of pig kidney.
- ChEMBL_215174 Displacement of [3H]AVP from vasopressin V2 receptor of rat kidney medulla.
- ChEMBL_215179 Displacement of [3H]-AVP from binding to Vasopressin receptor V2 of rat kidney
- ChEMBL_302930 Binding affinity against human vasopressin V1a receptor expressed in CHO cells
- ChEMBL_321349 Inhibitory concentration against [3H]AVP binding to human vasopressin V1a receptor
- ChEMBL_425925 Displacement of [3H]AVP from vasopressin V2 receptor in rat kidney membranes
- ChEMBL_425926 Displacement of [3H]AVP from vasopressin V1a receptor in rat liver membrane
- ChEMBL_441650 Binding affinity for human cloned vasopressin V1a receptor expressed in CHO cells
- ChEMBL_485637 Displacement of [3H]AVP from vasopressin V1a receptor in rat liver membrane
- ChEMBL_727045 Displacement of [3H]AVP from human vasopressin V1a receptor at 5 uM
- ChEBML_211079 Inhibition of radioligand [3H]AVP binding to the vasopressin V1 receptor in rat liver tissue
- ChEBML_211249 Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
- ChEBML_211254 Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
- ChEBML_214383 Compound was evaluated for its dissociation constant (Kd) to rat liver Vasopressin V1 receptor
- ChEBML_214535 Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEBML_214563 Binding affinity towards rat liver Vasopressin V1a receptor by using functional assay
- ChEBML_214711 Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
- ChEBML_214722 Binding affinity towards cloned human Vasopressin V2 receptor by using functional assay
- ChEBML_214854 Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEBML_215009 Inhibition of [3H]AVP binding to Dawley rat kidney medullary vasopressin V2 receptor.
- ChEBML_215014 Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
- ChEBML_215016 Binding affinity towards rat kidney Vasopressin V2 receptor by using functional assay
- ChEBML_215032 In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin receptor
- ChEBML_215034 Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
- ChEMBL_211079 Inhibition of radioligand [3H]AVP binding to the vasopressin V1 receptor in rat liver tissue
- ChEMBL_211080 Tested for the TYR(Me)2 arginine-vasopressin as radioligand at 0.3 nM in A7r5 cells
- ChEMBL_211249 Inhibition of [3H]arginine vasopressin binding to AVP-V2 site in rat kidney medulla.
- ChEMBL_211254 Inhibition of radioligand [3H]-AVP binding to the vasopressin V2 receptor in rat kidney tissue
- ChEMBL_214383 Compound was evaluated for its dissociation constant (Kd) to rat liver Vasopressin V1 receptor
- ChEMBL_214533 Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214534 Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214535 Inhibition of AVP mediated activation of human vasopressin V1a receptor expressed in HEK293 cells
- ChEMBL_214550 Binding affinity towards rat Vasopressin V1a receptor after peroral administration of the compound
- ChEMBL_214561 Binding affinity at Vasopressin V1a receptor, performed using [3H]AVP on rat liver
- ChEMBL_214696 Ability to displace [3H]arginine vasopressin in cloned human V2 receptor at 0.2 uM
- ChEMBL_214699 Binding affinity against human Vasopressin V2 receptor expressed in HeLa cells was determined
- ChEMBL_214707 Inhibition of [3H]AVP binding to human Vasopressin V2 receptor expressed in HeLa cells
- ChEMBL_214711 Evaluated for accumulation of cAMP in transfected HEK293 cells expressing human vasopressin V2 receptor
- ChEMBL_214722 Binding affinity towards cloned human Vasopressin V2 receptor by using functional assay
- ChEMBL_214851 Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEMBL_214854 Inhibition of AVP mediated activation of human vasopressin V2 receptor expressed in HEK293 cells
- ChEMBL_214879 Binding affinity towards rat Vasopressin V2 receptor after peroral administration of the compound
- ChEMBL_215014 Compound was evaluated for its dissociation constant (Kd) to rat kidney Vasopressin V2 receptor
- ChEMBL_215015 Binding affinity at Vasopressin V2 receptor, performed using [3H]AVP on rat kidney
- ChEMBL_215034 Tested for inhibition of [3H]LVP binding to vasopressin receptor in medullary membranes of pig kidney.
- ChEMBL_215167 Displacement of [3H]AVP from vasopressin receptor (V1a) from human platelet membranes.
- ChEMBL_425924 Displacement of [3H]AVP from rat vasopressin V1b receptor expressed in At-T20 cells
- ChEMBL_446241 Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cells
- ChEMBL_446242 Displacement of [3H]AVP from human vasopressin V1b receptor expressed in CHO cells
- ChEMBL_446243 Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
- ChEMBL_449800 Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
- ChEMBL_609618 Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cells
- ChEMBL_609622 Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells
- ChEMBL_634860 Antagonist activity at human Vasopressin 2 receptor assessed as inhibition of intracellular cAMP accumulation
- ChEMBL_748689 Displacement of [3H]-AVP from human vasopressin V1B receptor expressed in CHO cells
- ChEMBL_1865145 Antagonist activity at human vasopressin V1A receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assay
- ChEMBL_1865146 Antagonist activity at human vasopressin V1B receptor expressed in HEK293 cells assessed as decrease in vasopressin-stimulated calcium flux measured after 10 mins by Fluo-4 dye based microplate reader based assay
- ChEMBL_941874 Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with centrifuged compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
- ChEBML_211260 Compound was tested for inhibition against V2 vasopressin receptor in pig renal medullary membrane preparations.
- ChEBML_214408 In vitro inhibitory concentration against [3H]AVP binding to cloned human vasopressin V1a receptor
- ChEMBL_1456210 Antagonist activity at human vasopressin V1a receptor by double wash FLIPR/summary (Abse5) assay
- ChEMBL_214406 Evaluated for intracellular calcium mobilization in HEK293 cells transfected to express human vasopressin V1a receptor
- ChEMBL_214419 Displacement of [125I]- HO-LVA from human Vasopressin V1a receptor in membranes of CHO cells
- ChEMBL_215168 Displacement of (Phe-3,4,5-H) Vasopressin from V1a receptor from rat liver membranes.
- ChEMBL_215178 Displacement of [3H]AVP from binding to arginine vasopressin 1a (V1a) column of rat liver
- ChEMBL_449790 Displacement of [3H]AVP from human vasopressin V2 receptor expressed in mouse LV2 cells
- ChEMBL_449793 Displacement of [3H]manning ligand from human vasopressin V1a receptor expressed in CHO cells
- ChEMBL_540348 Antagonist activity at human recombinant vasopressin V1a receptor expressed in CHO cells by FLIPR assay
- ChEMBL_540352 Antagonist activity at human recombinant vasopressin V2 receptor expressed in yeast cells by FLIPR assay
- ChEMBL_561008 Binding affinity to human vasopressin V2 receptor expressed in HEK293 cells by radioligand binding assay
- ChEMBL_578146 Antagonist activity at human cloned vasopressin V1A receptor by cell based beta-lactamase assay
- ChEMBL_578148 Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase assay
- ChEMBL_604219 Antagonist activity at human cloned vasopressin V1a receptor by cell based beta lactamase assay
- ChEMBL_604220 Antagonist activity at human cloned vasopressin V2 receptor by cell based beta lactamase assay
- ChEMBL_748690 Displacement of [3H]-AVP from human vasopressin V1A receptor expressed in CHO cell membranes
- ChEMBL_748691 Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cell membranes
- ChEMBL_813469 Displacement of [125I]-LVA from prairie vole vasopressin V1A receptor after 72 hrs
- ChEMBL_1555983 Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cells assessed as inhibition of vasopressin induced IP1 accumulation pretreated for 30 mins measured 1 hr post Ab-Cryptate and IP1-d2 addition by HTRF assay
- ChEMBL_941873 Inhibition of vasopressin-stimulated vasopressin V2 receptor in human HTLA cells pre-incubated for 20 mins with Tween-80-treated compound solution measured on day 4 by beta arrestin-recruitment mediated luciferase reporter gene assay
- ChEBML_211234 Binding affinity towards rat liver V1a receptor was determined using [3H]arginine vasopressin as radioligand
- ChEBML_214260 Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
- ChEBML_214264 Compound was evaluated for half-maximal inhibition of binding of [3H]vasopressin toVasopressin V1 receptor in rat liver
- ChEBML_214539 Inhibition of 1 nM AVP-induced calcium mobilisation in cells expressing human vasopressin V1a receptor
- ChEBML_214692 In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in dog
- ChEBML_214849 In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in human
- ChEBML_215180 Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
- ChEMBL_1559803 Displacement of [3H]AVP from human recombinant arginine vasopressin receptor 1a expressed in CHO cells
- ChEMBL_211234 Binding affinity towards rat liver V1a receptor was determined using [3H]arginine vasopressin as radioligand
- ChEMBL_211257 Binding affinity towards rat kidney V2 receptor was determined using [3H]arginine vasopressin as radioligand
- ChEMBL_214260 Inhibition of 1 nM AVP-induced cAMP accumulation in cells expressing human vasopressin V2 receptor
- ChEMBL_214262 Inhibitory activity against arginine vasopressin V1 receptor using [3H]AVP as radioligand in human platelet
- ChEMBL_214265 Inhibitory activity against arginine vasopressin V1 receptor using [3H]AVP as radioligand in rat liver
- ChEMBL_214396 Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor
- ChEMBL_214539 Inhibition of 1 nM AVP-induced calcium mobilisation in cells expressing human vasopressin V1a receptor
- ChEMBL_214556 Compound was tested for the inhibition of [3H]AVP binding to Dawley rat kidney medullary Vasopressin V1a receptor
- ChEMBL_214698 Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V2 receptor
- ChEMBL_214849 In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in human
- ChEMBL_214850 In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in human
- ChEMBL_215180 Binding affinity of compound towards Vasopressin receptor by binding [3H]LVP to dog renal medullary preparation.
- ChEMBL_31424 In vitro antagonist activity was measured by inhibition of vasopressin-stimulated adenylate cyclase in renal medullary preparation in pig
- ChEMBL_326539 Displacement of [125I]LVA antagonist from human vasopressin 1a receptor expressed in HEK293-EBNA cells
- ChEMBL_326555 Displacement of [125I]LVA antagonist from human vasopressin 1b receptor expressed in HEK293-EBNA cells
- ChEMBL_326556 Displacement of [125I]LVA antagonist from human vasopressin 2 receptor expressed in HEK293-EBNA cells
- ChEMBL_485638 Displacement of [3H]AVP from vasopressin V1a receptor in rat liver membrane by competitive displacement assay
- ChEMBL_535597 Antagonist activity at human vasopressin V1a receptor by cell based beta-lactamase reporter gene assay
- ChEMBL_535598 Antagonist activity at human vasopressin V1b receptor by cell based beta-lactamase reporter gene assay
- ChEMBL_535599 Antagonist activity at human vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
- ChEMBL_609634 Activity at human vasopressin V1a receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
- ChEMBL_609635 Activity at human vasopressin V2 receptor expressed in CHO cells by NFAT-luciferase gene reporter assay
- ChEMBL_634859 Antagonist activity at human Vasopressin V1a receptor assessed as inhibition of intracellular calcium mobilization by FLIPR assay
- ChEMBL_748738 Displacement of [3H]AVP from human vasopressin V1b receptor expressed in CHO cells by scintillation counting
- ChEMBL_748739 Displacement of [3H]AVP from human vasopressin V1a receptor expressed in CHO cells by scintillation counting
- ChEMBL_748740 Displacement of [3H]AVP from human vasopressin V2 receptor expressed in CHO cells by scintillation counting
- ChEBML_214559 In vitro inhibition of (Phe-3,4,5 [3H]-) AVP binding towards isolated rat hepatic Vasopressin V1a receptor
- ChEBML_214566 Evaluated for the binding affinity towards Vasopressin V1a receptor in rat liver membrane using [3H]AVP as radioligand
- ChEBML_214705 Displacement of [3H]AVP from human vasopressin V2-receptor expressed in murine fibroblast cell (LV2) membranes
- ChEBML_215011 Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
- ChEBML_215019 Evaluated for the binding affinity towards Vasopressin V2 receptor in rat kidney membrane using [3H]-AVP as radioligand
- ChEMBL_211250 Concentration required to displace 50% of [3H]arginine vasopressin from rat kidney medullary (AVP-V2a site)
- ChEMBL_211258 Evaluated for the binding affinity towards vasopressin (V2) receptor in rat kidney membrane using [3H]AVP as radioligand
- ChEMBL_214559 In vitro inhibition of (Phe-3,4,5 [3H]-) AVP binding towards isolated rat hepatic Vasopressin V1a receptor
- ChEMBL_214566 Evaluated for the binding affinity towards Vasopressin V1a receptor in rat liver membrane using [3H]AVP as radioligand
- ChEMBL_214708 Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
- ChEMBL_214848 Concentration which inhibit [3H]AVP binding to human Vasopressin V2 receptor coded HeLa cells by 50%
- ChEMBL_215011 Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
- ChEMBL_215012 Inhibitory activity against arginine vasopressin V2 receptor using [3H]AVP as radioligand in rat adrenal medulla
- ChEMBL_515103 Displacement of [3H]oxytocin from human vasopressin V2 receptor expressed in CHO cells by filtration binding assay
- ChEMBL_624612 Antagonist activity at human cloned vasopressin V1A receptor by cell based beta-lactamase reporter gene assay
- ChEMBL_624613 Antagonist activity at human cloned vasopressin V2 receptor by cell based beta-lactamase reporter gene assay
- ChEMBL_743719 Displacement of [3H]AVP from human vasopressin V1a receptor expressed CHO cells after 60 mins
- ChEMBL_743720 Displacement of [3H]AVP from human vasopressin V1b receptor expressed CHO cells after 60 mins
- ChEMBL_743721 Displacement of [3H]AVP from human vasopressin V2 receptor expressed CHO cells after 60 mins
- ChEMBL_743730 Binding affinity to human vasopressin V1b receptor expressed CHO cells after 1 hr by spectrofluorimetry analysis
- ChEMBL_763490 Agonist activity at recombinant human vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
- ChEMBL_763492 Agonist activity at recombinant human vasopressin V2 receptor expressed in HEK293 cells by luciferase reporter gene assay
- ChEMBL_763496 Agonist activity at recombinant rat vasopressin V1a receptor expressed in HEK293 cells by luciferase reporter gene assay
- ChEMBL_813473 Displacement of [3H]-AVP from human vasopressin V2 receptor after 1.5 hrs by liquid scintillation counting
- ChEMBL_864198 Displacement of [3H]-AVP from human vasopressin V1b receptor expressed in CHO cells after 30 mins
- ChEMBL_864200 Displacement of [3H]-AVP from human vasopressin V1a receptor expressed in CHO cells after 30 mins
- ChEMBL_864210 Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins
- ChEMBL_864211 Displacement of [3H]-AVP from SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells by FRET assay
- ChEBML_211246 Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V2 receptor)
- ChEBML_214387 Ability to displace [3H]- Arginine Vasopressin (AVP) from its specific binding sites in rat liver (V1 receptor)
- ChEBML_214405 Evaluated for intracellular calcium mobilization in HEK- 293 cells transfected to express human vasopressin V1a receptor (Compound 7o)
- ChEBML_214714 Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
- ChEMBL_1766327 Displacement of [3H]-vasopressin from V1A receptor (unknown origin) expressed in HEK293 cell membranes incubated for 60 mins
- ChEMBL_214397 Binding affinity measured by inhibition of 3[H] AVP binding to cloned human vasopressin V1a receptor (Compound 7o)
- ChEMBL_214405 Evaluated for intracellular calcium mobilization in HEK- 293 cells transfected to express human vasopressin V1a receptor (Compound 7o)
- ChEMBL_214412 Binding affinity at cloned human Vasopressin V1a receptor stably expressed in CHO cells, using [3H]AVP as radioligand
- ChEMBL_214417 Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in human platelets
- ChEMBL_214418 Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in human platelets.
- ChEMBL_214564 Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in rat liver
- ChEMBL_214565 Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in rat liver.
- ChEMBL_214714 Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
- ChEMBL_214715 Inhibitory activity against human recombinant arginine vasopressin V2 receptor using [3H]AVP as radioligand in CHO cells
- ChEMBL_214718 Binding affinity at cloned human Vasopressin V2 receptor stably expressed in CHO cells, using [3H]AVP as radioligand
- ChEMBL_31440 Compound was evaluated for the inhibition constant for inhibition of 8-lysine-vasopressin stimulated adenylate cyclase of pig kidney medullary membrane
- ChEMBL_31441 Compound was evaluated for the inhibition constant for inhibition of 8-lysine-vasopressin stimulated adenylate cyclase of pig kidney medullary membrane
- ChEMBL_727043 Displacement of [3H]AVP from human vasopressin V1b receptor expressed in CHO cells by whole cell binding assay
- ChEMBL_727044 Displacement of [3H]AVP from rat vasopressin V1b receptor expressed in CHO cells by whole cell binding assay
- ChEMBL_763491 Agonist activity at recombinant human vasopressin V1b receptor expressed in Flp-In-293 cells by luciferase reporter gene assay
- ChEMBL_1451727 Agonist activity at human vasopressin V2 expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
- ChEMBL_1451728 Agonist activity at human vasopressin V1a expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
- ChEMBL_1451729 Agonist activity at human vasopressin V1b expressed in HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
- ChEMBL_446247 Inhibition of human vasopressin V1a receptor expressed in CHO cells by polarisation binding assay using 96-well plate membranes
- ChEMBL_446248 Inhibition of human vasopressin V1a receptor expressed in CHO cells by polarisation binding assay using 384-well plate membranes
- ChEMBL_446249 Inhibition of human vasopressin V1a receptor expressed in COS7 cells by HTRF-FRET assay using 96-well plate cells
- ChEMBL_446250 Inhibition of human vasopressin V1a receptor expressed in COS7 cells by HTRF-FRET assay using 96-well plate membranes
- ChEMBL_446251 Inhibition of human vasopressin V1a receptor expressed in COS7 cells by HTRF-FRET assay using 384-well plate membranes
- ChEMBL_864201 Binding affinity to SNAP-tagged vasopressin V2 receptor expressed in HEK293 cells after 1 hr by TR-FRET assay
- ChEBML_211240 Tested for the inhibition to V2 subtype receptor using [3H]- (VS2) as radioligand at 3 nM and arginine-vasopressin at 2 uM in LLCPKI cells
- ChEMBL_1560577 Displacement of [3H]AVP from human Vasopressin V2 receptor expressed in HeLa cells after 2 hrs by liquid scintillation counter
- ChEMBL_214392 Inhibition of the 3 nM VP stimulation of phospholipase-C in cultured WRK cells was used as a V1-mediated assay (Vasopressin V1 receptor)
- ChEMBL_214688 Compound was tested for its ability to displace [125I]- HO-LVA ligand from human Vasopressin V1b receptor in the membranes of CHO cells
- ChEMBL_214847 Compound was tested for its ability to of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
- ChEMBL_215171 Tested for inhibition constant determined from vasopressin induced inositol phosphates accumulation performed on WRK1 cell line of V1a receptor subtype
- ChEMBL_864205 Displacement of [3H]-AVP from human vasopressin V2 receptor expressed in CHO cells after 30 mins by saturation binding assay
- ChEMBL_1451733 Antagonist activity at human vasopressin V1a expressed in AVP-stimulated HEK293 cells after 5 hrs by firefly luciferase reporter gene assay
- ChEMBL_1711189 Displacement of [3H]AVP from human vasopressin V1b receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
- ChEMBL_1726376 Agonist activity at human vasopressin V1a receptor expressed in HEK293 cells assessed as induction of IP1 accumulation after 1 hr by HTRF assay
- ChEMBL_2015644 Inhibition of human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
- ChEMBL_214689 The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V1b receptor
- ChEMBL_214856 The inhibition constant (Ki(nM)) by displacement of [125I]- HO-LVA radiolabeled ligand using membranes of CHO cells of human Vasopressin V2 receptor
- ChEMBL_215017 Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats
- ChEMBL_215018 Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from rats.
- ChEMBL_1711188 Displacement of [3H]AVP from human liver vasopressin V1a receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
- ChEMBL_1711190 Displacement of [3H]AVP from human kidney vasopressin V2 receptor expressed in HEK293 cell membrane after 1 hr by scintillation counting method
- ChEMBL_2071783 Antagonist activity at human V1a receptor expressed in human 1321N1 cells assessed as decrease in Arg8-vasopressin-stimulated calcium flux by fluorometric calcium assay
- ChEMBL_214414 Binding affinity against human vasopressin V1a receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_214687 Binding affinity against human vasopressin V1b receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_214721 Binding affinity against human vasopressin V2 receptor was determined by using plasma membranes from CHO cells stably transfected with VP/OT receptors
- ChEMBL_2158237 Displacement of [3H]-arginine-vasopressin from human V1A receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
- ChEMBL_2158239 Displacement of [3H]-arginine-vasopressin from human V2 receptor expressed in human 1321N1 cell membranes incubated for 60 mins by radioligand binding assay
- ChEMBL_560999 Agonist activity at human vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
- ChEMBL_561010 Agonist activity at rat vasopressin V2 receptor expressed in HEK293 cells assessed as increase in intracellular cAMP level by CRE-luciferase reporter gene assay
- ChEMBL_748694 Antagonist activity at human vasopressin V1B receptor expressed in CHO cells assessed as inhibition of AVP-induced calcium mobilisation by luciferase reporter gene assay
- ChEMBL_1583335 Displacement of [3H]8-arginine-vasopressin from human oxytocin receptor expressed in CHO cell membrane incubated for 1 hr by liquid scintillation counting method
- ChEMBL_1794570 Displacement of [3H]AVP from human vasopressin V1b receptor expressed in CHO cell membranes after 60 mins by TopCount microplate scintillation counting method
- ChEMBL_700574 Antagonist activity at recombinant V1b receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining
- ChEMBL_700575 Antagonist activity at recombinant V1a receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining
- ChEMBL_700576 Antagonist activity at recombinant oxytocin receptor expressed in CHO cells assessed as inhibition of vasopressin-induced calcium release after 10 mins by Fluo4-AM staining
- Vasopressin V1B Receptor Antagonist Assay The purpose of the assay is to determine the inhibitory effect of synthesized compounds on the Vasopressin V1b receptor. The assay was performed in Chinese Hamster Ovary (CHO) cells expressing the human Arginine Vasopressin Receptor 1b (AVPR1b). Arginine Vasopressin (AVP) evokes an increase in intracellular calcium in CHO-AVPR1b cells which is measured in a fluorescence assay on the FLIPRTETRA using calcium sensitive dyes. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent reduction in the AVP-mediated fluorescence.CHO-AVPR1b cells were maintained in routine culture in T175 Flasks at 37° C., 5% CO2. The growth medium consisted of Ham's F12 media supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 0.4 mg/ml Geneticin G418.
- ChEMBL_214845 Binding affinity was evaluated by measuring the displacement of [3H]-AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors
- ChEMBL_214846 Binding affinity was evaluated by measuring the displacement of [3H]AVP (arginine vasopressin) from specific binding sites in kidney medulla obtained from early postmortem human donors.
- ChEMBL_743726 Agonist activity at human vasopressin V1b receptor expressed CHO cells assessed as induction of phospholipase C activity after 15 mins by inositol phosphate accumulation assay
- ChEMBL_1724079 Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced IP1 accumulation measured after 1 hr by fluorescence assay
- ChEMBL_749194 Displacement of [3H]AVP from human vasopressin V1b receptor expressed in CHO cells co-expressing VIP-luciferase by scintillation counting-based whole cell binding assay
- ChEMBL_1555982 Agonist activity at human vasopressin 1a receptor expressed in HEK293 cells assessed as increase in IP1 accumulation preincubated for 1 hr followed by addition of Ab-Cryptate and IP1-d2 by HTRF assay
- ChEMBL_1711196 Agonist activity at human vasopressin V1b receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
- Vasopressin V1A Receptor Antagonist Assay The purpose of this assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin V1a receptor. The assay as performed in Chinese Hamster Ovary (CHO) cells expressing the human Arginine Vasopressin Receptor 1a (AVPR1a). Arginine Vasopressin (AVP) evokes an increase in intracellular calcium in CHO-AVPR1a cells which is measured in a fluorescence assay on the FLIPRTETRA using calcium sensitive dyes. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent reduction in the AVP-mediated fluorescence. Compounds were tested in duplicate in a 10-point, 1:3 dilution series starting at a nominal concentration of 3 μM in the assay.CHO-AVPR1a cells were maintained in routine culture in T175 Flasks at 37° C., 5% CO2. The growth medium consists of Ham's F12 media supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 0.4 mg/ml Geneticin G418.
- ChEMBL_1711195 Agonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
- ChEMBL_1711197 Agonist activity at human kidney vasopressin V2 receptor expressed in CHO cells assessed as increase in intracellular calcium flux measured for 5 mins by Fluo-4-AM dye based FLIPR assay
- ChEMBL_1724085 Antagonist activity at human vasopressin 1a receptor expressed in CHO cell membranes assessed as inhibition of AVP-induced IP1 accumulation by measuring IP1 level measured after 1 hr by fluorescence assay
- ChEMBL_1865144 Antagonist activity at human OTR expressed in HEK293 cells assessed as decrease in calcium flux measured after 10 mins in presence of vasopressin by Fluo-4 dye based microplate reader based assay
- Binding Affinity Assay (Ki) and cAMP Accumulation Activity Assay (EC50) The affinities of test compounds for human V2 receptor were evaluated by the radioligand binding study using membrane fractions isolated from CHO cells expressing human V2 receptors. For the competitive binding study, drug compound solution and [3H]vasopressin were mixed with membrane suspension in reaction buffer. This mixture was incubated at room temperature for 60 min. Reactions were terminated by filtration through UniFilter GF/B (Perkin-Elmer) using a MicroMate Cell Harvester (Packard Instrument Company, Meriden, CT, USA). The radioactivity retained on the filter was counted by TopCountTM microplate scintillation counter (Perkin-Elmer) using the scintillation cocktail (MicroScinti-40TM, Perkin-Elmer). The concentration of each compound required to reduce specific binding of [3H]vasopressin by 50% (IC50 value) was obtained by non-linear regression analysis. A Kd value of [3H]vasopressin for each vasopressin receptor was yielded by Scatchard plot analysis. The affinity constants (Ki values) were calculated from the following equation, using the Kd values yielded from each separate experiment. Ki =IC50/(1 + [[3H]vasopressin concentration]/Kd). EC50 values were determined as the concentration of the test compound required to increase the cAMP level to 50% of the maximum response to AVP. All assays were performed in triplicate.
- Binding Assay for Human V2 Receptor The affinities of test compounds for human V2 receptor were evaluated by the radioligand binding study using membrane fractions isolated from CHO cells expressing human V2 receptors.. For the competitive binding study, drug compound solution and [3H]vasopressin were mixed with membrane suspension in reaction buffer. This mixture was incubated at room temperature for 60 min. Reactions were terminated by filtration through UniFilter GF/B (Perkin-Elmer) using a MicroMate Cell Harvester (Packard Instrument Company, Meriden, CT, USA). The radioactivity retained on the filter was counted by TopCountTM microplate scintillation counter (Perkin-Elmer) using the scintillation cocktail (MicroScinti-40TM, Perkin-Elmer). Nonspecific binding or total binding were determined by including 1 uM AVP or without test compounds in the reaction mixture, respectively. Specific binding was calculated as total binding minus nonspecific binding. The concentration of each compound required to reduce specific binding of [3H]vasopressin by 50% (IC50 value) was obtained by non-linear regression analysis. A Kd value of [3H]vasopressin for each vasopressin receptor was yielded by Scatchard plot analysis. The affinity constants (Ki values) were calculated from the following equation, using the Kd values yielded from each separate experiment. Ki =IC50/(1 + [[3H]vasopressin concentration]/Kd).
- ChEMBL_1665973 Displacement of [125I] phenylacetyl-D-Tyr(Me)-Phe-Gln-Asn-Arg-Pro-Arg-Tyr-NH2 from human recombinant vasopressin V1a receptor expressed in HEK293 after 2 hrs by liquid scintillation counting method
- Binding Assay for Human V1a Receptor Chinese hamster ovary (CHO) cells stably expressing human V1a receptors. Cells were washed with phosphate buffered saline, and then collected in ice-cold hypotonic buffer. Subsequently, cells were collected using a cell scraper and then homogenized using POLYTRON followed by centrifugation at 4 deg C. The supernatant was centrifuged (35,000g, 30 min) at 4 deg C, and the pellet was suspended in Tris buffer as membrane fractions. The affinities of test compounds for human V1a receptor were evaluated by the radioligand binding study. For the competitive binding study, drug compound solution and [3H]vasopressin were mixed with membrane suspension in reaction buffer. This mixture was incubated at room temperature for 60 min. Reactions were terminated by filtration through UniFilter GF/B (Perkin-Elmer) using a MicroMate Cell Harvester (Packard Instrument Company, Meriden, CT, USA). The radioactivity retained on the filter was counted by TopCountTM microplate scintillation counter (Perkin-Elmer) using the scintillation cocktail (MicroScinti-40TM, Perkin-Elmer). Nonspecific binding or total binding were determined by including 1 uM AVP or without test compounds in the reaction mixture, respectively. Specific binding was calculated as total binding minus nonspecific binding. The concentration of each compound required to reduce specific binding of [3H]vasopressin by 50% (IC50 value) was obtained by non-linear regression analysis. A Kd value of [3H]vasopressin for each vasopressin receptor was yielded by Scatchard plot analysis. The affinity constants (Ki values) were calculated from the following equation, using the Kd values yielded from each separate experiment. Ki =IC50/(1 + [[3H]vasopressin concentration]/Kd).
- ChEMBL_1711201 Antagonist activity at human liver vasopressin V1a receptor expressed in CHO cells assessed as inhibition of agonist-induced intracellular calcium flux preincubated for 20 mins followed by AVP addition measured for 5 mins by Fluo-4-AM dye based FLIPR assay
- ChEMBL_1724088 Antagonist activity at human vasopressin 1a receptor expressed in HEK293 cell membranes assessed as inhibition of AVP-induced increase in Ca2+ flux preincubated for 5 mins followed by AVP addition measured after 5 mins for every 2 secs by Ca5 dye based FLIPR assay
- Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: V1R_AG_FLUO8_1536_3XEC50 DRUN Name: Fluorescence-based cell-based high throughput dose response screening assay for agonists of the vasopressin 1 receptor (V1R). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence complex social behaviors such as trust, anxiety, and parent
- Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: V1R_AG_FLUO8_1536_3XEC50 OXTR DCSRUN Name: Counterscreen for Oxytocin Receptor (OXTR) agonists: Fluorescence-based cell-based high throughput dose response assay to identify agonists of the vasopressin 1 receptor (V1R). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence c
- Counterscreen for vasopressin 1 receptor (V1R) agonists: Fluorescence-based cell-based high throughput dose response assay for agonists of the Oxytocin Receptor (OXTR) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: OTR_AG_FLUO8_1536_3XEC50 V1R DCSRUN Name: Counterscreen for vasopressin 1 receptor (V1R) agonists: Fluorescence-based cell-based high throughput dose response assay for agonists of the Oxytocin Receptor (OXTR). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence complex so
- Cellular In Vitro Assay for Determining Vasopressin V1a Receptor Activity The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V2 Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations and the agonist [Arg8]-vasopressin at EC50 concentration are added together to the wells, and plates are incubated for 3 hours in a cell incubator. Upon addition of the cell lysis reagent Triton™ and the substrate luciferin, luminescence of firefly luciferase is measured in a luminometer.
- Cellular In Vitro Assay for Determining Vasopressin V2 Receptor Activity The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obelin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed V1a receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].Vasopressin V1a Receptor Cell Lines:On the day before the assay, the cells are plated out in culture medium (DMEM/F12, 2% FCS, 2 mM glutamine, 10 mM HEPES, 5 μg/ml coelenterazine) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, test compounds in various concentrations are placed for 10 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin at EC50 concentration is added. The resulting light signal is measured immediately in the luminometer.
- Vasopressin V2 Receptor Antagonist Assay The purpose of the assay was to determine the inhibitory effect of synthesized compounds on the Vasopressin receptor 2. The assay was performed in commercially available 1321N1 cells expressing the human Arginine Vasopressin Receptor V2 (AVPR2) (Perkin Elmer #ES-363-CF). Arginine Vasopressin (AVP) evokes an increase in intracellular cAMP in these cells which is measured in a TR-FRET assay using a Europium cAMP tracer and ULight labelled antibody reagents contained in a LANCE Ultra cAMP kit (Perkin Elmer #TRF0263). Increases in cAMP in the assay result in a reduction in TR-FRET as the cAMP produced by the stimulated cells competes with the Eu-cAMP tracer for binding sites on the ULight labelled antibody. Test compounds were assessed for their ability to affect the magnitude of the response to AVP, with antagonists showing a concentration-dependent decrease in the AVP-mediated reduction in TR-FRET signal.cAMPZen V2 assay ready cells were thawed at 37° C. and resuspended directly from frozen in 9 ml growth medium consisting of DMEM supplemented with 10% v/v fetal bovine serum, 1× non-essential amino acids, and 1 mM sodium pyruvate. Cells were spun at 1000 rpm for 3 minutes and the supernatant was carefully removed and discarded. The pellet was resuspended in 5 ml stimulation buffer and the cell density determined using the Vi-Cell automated cell counter. The cell suspension was diluted to a 0.2×106/ml suspension ready for plating. To all wells of a white 384-well Optiplate (Perkin Elmer #6007299) 5 μL of cells in stimulation buffer were dispensed (1,000 cells per well). Stimulation buffer consisted of HBSS (+Ca/+Mg) supplemented with 5 mM HEPES, 0.1% BSA stabiliser and 0.5 mM IBMX.
- Cellular In Vitro Assay for Determining Vasopressin Receptor Activity The identification of agonists and antagonists of the V1a and V2 vasopressin receptors from humans, rats and dogs as well as the quantification of the activity of the compounds of the invention is carried out using recombinant cell lines. These cell lines originally derive from a hamster's ovary epithelial cell (Chinese Hamster Ovary, CHO K1, ATCC: American Type Culture Collection, Manassas, Va. 20108, USA). The test cell lines constitutively express the human, rat or dog V1a or V2 receptors. In case of the Gαq-coupled V1a receptors, cells are also stably transfected with a modified form of the calcium-sensitive photoproteins aequorin (human and rat V1a) or obe-lin (dog V1a), which, after reconstitution with the cofactor coelenterazine, emit light when there are increases in free calcium concentrations [Rizzuto R, Simpson A W, Brini M, Pozzan T, Nature 358, 325-327 (1992); Illarionov B A, Bondar V S, Illarionova V A, Vysotski E S, Gene 153 (2), 273-274 (1995)]. The resulting vasopressin receptor cells react to stimulation of the recombinantly expressed Via receptors by intracellular release of calcium ions, which can be quantified by the resulting photoprotein luminescence. The Gs-coupled V2 receptors are stably transfected into cell lines expressing the gene for firefly luciferase under control of a CRE-responsible promoter. Activation of V2 receptors induces the activation of the CRE-responsive promoter via cAMP increase, thereby inducing the expression of firefly luciferase. The light emitted by photoproteins of V1a cell lines as well as the light emitted by firefly luciferase of V2 cell lines corresponds to the activation or inhibition of the respective vasopressin receptor. The bioluminescence of the cell lines is detected using a suitable luminometer [Milligan G, Marshall F, Rees S, Trends in Pharmacological Sciences 17, 235-237 (1996)].
- Cellular In Vitro Assay On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
- Cellular In Vitro Assay On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtiter plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtiter plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtiter plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
- Cellular in Vitro Assay On the day before the assay, the cells are plated out in culture medium (DMEM, 10% FCS, 2 mM glutamine, 10 mM HEPES) in 384-well microtitre plates and kept in a cell incubator (96% humidity, 5% v/v CO2, 37° C.). On the day of the assay, the culture medium is replaced by a Tyrode solution (140 mM NaCl, 5 mM KCl, 1 mM MgCl2, 2 mM CaCl2, 20 mM glucose, 20 mM HEPES), which additionally contains the cofactor coelenterazine (50 μM), and the microtitre plate is then incubated for a further 3-4 hours. The test substances in various concentrations are placed for 10 to 20 minutes in the wells of the microtitre plate before the agonist [Arg8]-vasopressin is added, and the resulting light signal is measured immediately in the luminometer.
- Oxytocin Receptor Antagonist Assay This assay was performed in CHEM-1 cells expressing the human Oxytocin Receptor (hOTR) to determine the inhibitory effect of the compounds of the invention on the human Oxytocin receptor. Oxytocin evokes an increase in intracellular calcium in CHEM-1-hOTR cells which is measured in a fluorescence assay on the FLIPRTETRA using calcium sensitive dyes. Test compounds were assessed for their ability to affect the magnitude of the response to oxytocin, with antagonists showing a concentration-dependent reduction in the oxytocin-mediated fluorescence. Compounds displaying potency at the vasopressin V1a receptor of <100 nM were progressed to selectivity testing against hOTR and were tested in triplicate in a 10-point, 1:3 dilution series starting at a nominal concentration of 3 μM in the assay.CHEM-1-hOTR ready was used to assay frozen cells (Eurofins #HTS090RTA) which are supplied with a proprietary Media Component.
- Binding Assay The binding assay was carried out by the method based on that of Tahara et al. (Tahara A et al., Brit. J. Pharmacol. 125, 1463-1470 (1998)).The incubation buffer was: 50 mM Tris, 10 mM MgCl2, 0.1% BSA, pH 7.4.In the assay mixture (200 μl), membranes (40 μg protein in incubation buffer) from CHO-K1 cells with stably expressed human V1a receptors (cell line hV1a_5_CHO) were incubated with 0.04 nM 125I-AVP (8-Arg-vasopressin, PerkinElmer NEX 128) in incubation buffer (50 mM Tris, 10 mM MgCl2, 0.1% BSA, pH 7.4) (total binding) or additionally with increasing concentrations of test substance (displacement experiment). The nonspecific binding was determined with 1 μM AVP (Fluka 94836). Duplicate determinations were carried out.After incubation (60 minutes at room temperature), the samples were processed as described for V1b.
- Fluorescence-based cell-based high throughput dose response assay for agonists of the Oxytocin Receptor (OXTR) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: OTR_AG_FLUO8_1536_3XEC50 DRUN Name: Fluorescence-based cell-based high throughput dose response assay for agonists of the Oxytocin Receptor (OXTR). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence complex social behaviors such as trust, anxiety, and parenting (5). Oxyto
- Fluorescence-based cell-based high throughput dose response assay for potentiators of Oxytocin Receptor (OXTR) Source (MLPCN Center Name): The Scripps Research Institute Molecular Screening Center (SRIMSC) Center Affiliation: The Scripps Research Institute (TSRI) Assay Provider: Michael Jarstfer, University of North Carolina at Chapel Hill (UNC) Network: Molecular Libraries Probe Production Centers Network (MLPCN) Grant Proposal Number: 1 R03 MH085678-01A1 Grant Proposal PI: Michael Jarstfer, UNC External Assay ID: OTR_POT_FLUO8_1536_3XEC50 DRUN Name: Fluorescence-based cell-based high throughput dose response assay for potentiators of Oxytocin Receptor (OXTR). Description: Heterotrimeric G-protein coupled receptors (GPCRs) are major targets for disease therapeutics, due in part to their broad tissue distribution, structural diversity, varied modes of action, disease-associated mutations (1-4). Certain GPCRs are involved in signaling pathways for neuropeptides such as oxytocin, serotonin, and vasopressin, and influence complex social behaviors such as trust, anxiety, and parenting (5). Oxyto
- Inhibition Activity Assay V1aR: The inhibition effect of the compounds of the present invention on the activity of human V1 aR protein expressed in HEK293/human V1aR stably transfected cells was determined by the following experimental method:I. Experimental Materials and Instruments1. Fluo-4 NW calcium assay kit (F36206, invitrogen)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. Flexstation 3 multi-function microplate reader (Molecular Devices)8. Poly-D-lysine 96-well plate, black/clear (356692, BD)9. Vasopressin (Tocris, 2935)10. pcDNA3.1 (invitrogen, V79020)11. pcDNA3.1-V1aR (NM-000706) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)12. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
- Inhibition Activity Assay V1bR: The inhibition effect of the compounds of the present invention on the activity of human V1bR protein expressed in HEK293/human V1bR cells was determined by the following experimental method:I. Experimental Materials and Instruments1. Fluo-4 NW calcium assay kit (F36206, invitrogen)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. Flexstation 3 multi-function microplate reader (Molecular Devices)8. Poly-D-lysine 96-well plate, black/clear (356692, BD)9. Vasopressin (Tocris, 2935)10. pcDNA3.1 (invitrogen, V79020)11. pcDNA3.1-V1bR (NM-000706) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)12. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)
- Binding Assay The binding assay was carried out by the method based on that of Tahara et al. (Tahara A et al., Brit. J. Pharmacol. 125, 1463-1470 (1998)). The incubation buffer was: 50 mM Tris, 10 mM MgCl2, 0.1% BSA, pH 7.4. In the assay mixture (200 μl), membranes (26 g protein in incubation buffer) from CHO-K1 cells with stably expressed human V1b receptors (cell line hV1b_3H2_CHO) were incubated with 1.5 nM3H-AVP (8-Arg-vasopressin, PerkinElmer, NET 800) in incubation buffer (50 mM Tris, 10 mM MgCl2, 0.1% BSA, pH 7.4) (total binding) or additionally with increasing concentrations of test substance (displacement experiment). The nonspecific binding was determined with 1 μM AVP (Fluka 94836). All determinations were carried out as duplicate determinations. After incubation (60 minutes at room temperature), the free radioligand was filtered off by vacuum filtration (Tomtec Mach III) through Wathman GF/B glass fiber filter plates (UniFilter, PerkinElmer 6005177). The liquid scintillation measurement took place in a Microbeta TriLux 12 (Wallac).
- competition binding assay The human V1a receptor was cloned by RT-PCR from total human liver RNA. The coding sequence was subcloned in an expression vector after sequencing to confirm the identity of the amplified sequence. To demonstrate the affinity of the compounds from the present invention to the human V1a receptor binding studies were performed. Cell membranes were prepared from HEK293 cells transiently transfected with the expression vector and grown in 20 liter fermenters with the following protocol.50 g of cells are re-suspended in 30 ml freshly prepared ice cold Lysis buffer (50 mM HEPES, 1 mM EDTA, 10 mM MgCl2 adjusted to pH=7.4+complete cocktail of protease inhibitor (Roche Diagnostics)). Homogenized with Polytron for 1 min and sonicated on ice for 2×2 minutes at 80% intensity (Vibracell sonicator). The preparation is centrifuged 20 min at 500 g at 4° C., the pellet is discarded and the supernatant centrifuged 1 hour at 43,000 g at 4° C. (19,000 rpm). The pellet is re-suspended in 12.5 ml Lysis buffer+12.5 ml Sucrose 20% and homogenized using a Polytron for 1-2 min. The protein concentration is determined by the Bradford method and aliquots are stored at −80° C. until use. For binding studies 60 mg Yttrium silicate SPA beads (Amersham) are mixed with an aliquot of membrane in binding buffer (50 mM Tris, 120 mM NaCl, 5 mM KCl, 2 mM CaCl2, 10 mM MgCl2) for 15 minutes with mixing. 50 μl of bead/membrane mixture is then added to each well of a 96 well plate, followed by 50 μl of 4 nM 3H-Vasopressin (American Radiolabeled Chemicals). For total binding measurement 100 μl of binding buffer are added to the respective wells, for non-specific binding 100 μl of 8.4 mM cold vasopressin and for compound testing 100 μl of a serial dilution of each compound in 2% DMSO. The plate is incubated 1 h at room temperature, centrifuged 1 min at 1000 g and counted on a Packard Top-Count. Non-specific binding counts are subtracted from each well and data is normalized to the maximum specific binding set at 100%. To calculate an IC 50 the curve is fitted using a non-linear regression model (XLfit) and the Ki is calculated using the Cheng-Prussoff equation.
- Inhibition Activity Assay V2R: The inhibition effect of the compounds of the present invention on the activity of human V2R protein expressed in HEK293/human V2R cells was determined by the following experimental method:I. Experimental Materials and Instruments1. cAMP dynamic 2 kit—1,000 tests (62AM4PEB, Cisbio)2. MEM (Hyclone, SH30024.01B)3. G418 sulfate (Enzo, ALX-380-013-G005)4. Fetal bovine serum (GIBCO, 10099)5. Sodium pyruvate solution (sigma, 58636-100ML)6. MEM non-essential amino acid solution (100×) (sigma, M7145-100ML)7. PheraStar multi-function microplate reader (BMG)8. Corning/Costar 384-well non-adsorbing microplate—black NBS plate (4514, Corning)9. Cell dissociation solution, enzyme-free, PBS (13151014-100 ml, Thermo Fisher Scientific)10. HBSS, calcium, magnesium, phenol red free (14025-092, Invitrogen)11. HEPES, 1M buffer (15630-080, GIBCO)12. BSA (0219989725, MP Biomedicals)13. IBMX (I7018-250MG, sigma)14. Vasopressin (Tocris, 2935)15. pcDNA3.1 (invitrogen, V79020)16. pcDNA3.1-V2R (NM-000054) (synthesized and constructed into pcDNA3.1 plasmid by GENEWIZ Biological Technology Co., Ltd)17. HEK293 cells (Cat. No. GNHu18, Cell Bank of Chinese Academy of Sciences)