BDBM162127 (S)-noradrenaline (+)-noradrenaline (+)-norepinephrine (S)-norepinephrine
DL-[7-3H]norepinephrine NOREPINEPHRINE BDBM35234 [3H]NE Noradrenaline,(+)
(R)-(-)-norepinephrine (R)-4-(2-amino-1-hydroxyethyl)-1,2-benzenediol BDBM50029051 CHEMBL1437 4-[(1R)-2-amino-1-hydroxyethyl]benzene-1,2-diol (R)-norepinephrine NOREPINEPHRINE (-)-noradrenaline (R)-noradrenaline US20250032476, Compound NorEpi (-)-norepinephrine (-)-arterenol
alpha-Methyl-(-)norepinephrine,(+/-) BDBM50027502 CHEMBL764 METHYLNORADRENALINE Aldoclor-150 4-(2-Amino-1-hydroxy-propyl)-benzene-1,2-diol alpha-Methyl-(+)norepinephrine,(+/-) Aldoclor-250 alpha-Methyl-(+/-)norepinephrine,(+/-)
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- Del Bello, F; Sakloth, F; Partilla, JS; Baumann, MH; Glennon, RA Ethylenedioxy homologs of N-methyl-(3,4-methylenedioxyphenyl)-2-aminopropane (MDMA) and its corresponding cathinone analog methylenedioxymethcathinone: Interactions with transporters for serotonin, dopamine, and norepinephrine. Bioorg Med Chem 23: 5574-9 (2015)
- Rafferty, MF; Wilson, DS; Monn, JA; Krass, P; Borchardt, RT; Grunewald, GL Importance of the aromatic ring in adrenergic amines. 7. Comparison of the stereoselectivity of norepinephrine N-methyltransferase for aromatic vs. nonaromatic substrates and inhibitors. J Med Chem 25: 1198-204 (1983)
- Hoepping, A; Johnson, KM; George, C; Flippen-Anderson, J; Kozikowski, AP Novel conformationally constrained tropane analogues by 6-endo-trig radical cyclization and stille coupling - switch of activity toward the serotonin and/or norepinephrine transporter. J Med Chem 43: 2064-71 (2000)
- Grunewald, GL; Monn, JA; Rafferty, MF; Borchardt, RT; Krass, P Probes of the active site of norepinephrine N-methyltransferase: effect of hydrophobic and hydrophilic interactions on side-chain binding of amphetamine and alpha-methylbenzylamine. J Med Chem 25: 1248-50 (1983)
- Zhang, P; Terefenko, EA; McComas, CC; Mahaney, PE; Vu, A; Trybulski, E; Koury, E; Johnston, G; Bray, J; Deecher, D Synthesis and activity of novel 1- or 3-(3-amino-1-phenyl propyl)-1,3-dihydro-2H-benzimidazol-2-ones as selective norepinephrine reuptake inhibitors. Bioorg Med Chem Lett 18: 6067-70 (2008)
- Zhou, J; Zhang, A; Kläss, T; Johnson, KM; Wang, CZ; Ye, YP; Kozikowski, AP Biaryl analogues of conformationally constrained tricyclic tropanes as potent and selective norepinephrine reuptake inhibitors: synthesis and evaluation of their uptake inhibition at monoamine transporter sites. J Med Chem 46: 1997-2007 (2003)
- Millan, MJ; Gobert, A; Lejeune, F; Newman-Tancredi, A; Rivet, JM; Auclair, A; Peglion, JL S33005, a novel ligand at both serotonin and norepinephrine transporters: I. Receptor binding, electrophysiological, and neurochemical profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine. J Pharmacol Exp Ther 298: 565-80 (2001)
- Bartolomé, JM; Alcudia, A; Andrés, JI; Cid, JM; García, M; Megens, A; Toledo, MA; Trabanco, AA Novel 2-N,N-dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo[2,3-d]oxepin derivatives displaying combined norepinephrine reuptake inhibition and 5-HT2A/2C receptor antagonism. Bioorg Med Chem Lett 15: 2898-901 (2005)
- Boja, JW; Kuhar, MJ; Kopajtic, T; Yang, E; Abraham, P; Lewin, AH; Carroll, FI Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters. J Med Chem 37: 1220-3 (1994)
- Santra, S; Sharma, H; Vedachalam, S; Antonio, T; Reith, M; Dutta, A Development of potent dopamine-norepinephrine uptake inhibitors (DNRIs) based on a (2S,4R,5R)-2-benzhydryl-5-((4-methoxybenzyl)amino)tetrahydro-2H-pyran-4-ol molecular template. Bioorg Med Chem 23: 821-8 (2015)
- Mladenova, G; Annedi, SC; Ramnauth, J; Maddaford, SP; Rakhit, S; Andrews, JS; Zhang, D; Porreca, F First-in-class, dual-action, 3,5-disubstituted indole derivatives having human nitric oxide synthase (nNOS) and norepinephrine reuptake inhibitory (NERI) activity for the treatment of neuropathic pain. J Med Chem 55: 3488-501 (2012)
- Carlier, PR; Lo, MM; Lo, PC; Richelson, E; Tatsumi, M; Reynolds, IJ; Sharma, TA Synthesis of a potent wide-spectrum serotonin-, norepinephrine-, dopamine-reuptake inhibitor (SNDRI) and a species-selective dopamine-reuptake inhibitor based on the gamma-amino alcohol functional group. Bioorg Med Chem Lett 8: 487-92 (1999)
- Zeng, F; Mun, J; Jarkas, N; Stehouwer, JS; Voll, RJ; Tamagnan, GD; Howell, L; Votaw, JR; Kilts, CD; Nemeroff, CB; Goodman, MM Synthesis, radiosynthesis, and biological evaluation of carbon-11 and fluorine-18 labeled reboxetine analogues: potential positron emission tomography radioligands for in vivo imaging of the norepinephrine transporter. J Med Chem 52: 62-73 (2009)
- Carroll, FI; Gray, JL; Abraham, P; Kuzemko, MA; Lewin, AH; Boja, JW; Kuhar, MJ 3-Aryl-2-(3'-substituted-1',2',4'-oxadiazol-5'-yl)tropane analogues of cocaine: affinities at the cocaine binding site at the dopamine, serotonin, and norepinephrine transporters. J Med Chem 36: 2886-90 (1993)
- Zhang, S; Zhen, J; Reith, ME; Dutta, AK Discovery of novel trisubstituted asymmetric derivatives of (2S,4R,5R)-2-benzhydryl-5-benzylaminotetrahydropyran-4-ol, exhibiting high affinity for serotonin and norepinephrine transporters in a stereospecific manner. J Med Chem 48: 4962-71 (2005)
- He, R; Kurome, T; Giberson, KM; Johnson, KM; Kozikowski, AP Further structure-activity relationship studies of piperidine-based monoamine transporter inhibitors: effects of piperidine ring stereochemistry on potency. Identification of norepinephrine transporter selective ligands and broad-spectrum transporter inhibitors. J Med Chem 48: 7970-9 (2005)
- Orjales, A; Mosquera, R; Toledo, A; Pumar, MC; García, N; Cortizo, L; Labeaga, L; Innerárity, A Syntheses and binding studies of new [(aryl)(aryloxy)methyl]piperidine derivatives and related compounds as potential antidepressant drugs with high affinity for serotonin (5-HT) and norepinephrine (NE) transporters. J Med Chem 46: 5512-32 (2003)
- Mishra, M; Kolhatkar, R; Zhen, J; Parrington, I; Reith, ME; Dutta, AK Further structural optimization of cis-(6-benzhydryl-piperidin-3-yl)-benzylamine and 1,4-diazabicyclo[3.3.1]nonane derivatives by introducing an exocyclic hydroxyl group: interaction with dopamine, serotonin, and norepinephrine transporters. Bioorg Med Chem 16: 2769-78 (2008)
- Altenbach, RJ; Black, LA; Strakhova, MI; Manelli, AM; Carr, TL; Marsh, KC; Wetter, JM; Wensink, EJ; Hsieh, GC; Honore, P; Garrison, TR; Brioni, JD; Cowart, MD Diaryldiamines with dual inhibition of the histamine H(3) receptor and the norepinephrine transporter and the efficacy of 4-(3-(methylamino)-1-phenylpropyl)-6-(2-(pyrrolidin-1-yl)ethoxy)naphthalen-1-ol in pain. J Med Chem 53: 7869-73 (2010)
- ChEMBL_582829 (CHEMBL1061665) Inhibition of [3H]norepinephrine reuptake at norepinephrine transporter
- ChEMBL_487427 (CHEMBL1020882) Inhibition of norepinephrine uptake at rat brain norepinephrine transporter
- ChEMBL_144991 (CHEMBL755917) Inhibition of [3H]norepinephrine uptake at the rat norepinephrine transporter.
- ChEBML_177242 Inhibition of norepinephrine uptake in synaptosomal preparation fro rat hypothalamus, using [3H]norepinephrine
- ChEMBL_144966 (CHEMBL755084) Inhibition of Norepinephrine (NA) reuptake using cloned human Norepinephrine transporter was determined
- ChEMBL_2261974 (CHEMBL5216985) Inhibition of norepinephrine transporter (unknown origin) assessed as inhibition of norepinephrine reuptake
- ChEMBL_306535 (CHEMBL827824) Inhibition of [3H]norepinephrine uptake in HEK293 cells expressing human norepinephrine transporter
- ChEMBL_608767 (CHEMBL1068359) Inhibition of [3H]norepinephrine reuptake at rat brain frontal cortex norepinephrine transporter
- ChEBML_142964 Norepinephrine transporter activity was determined by the ability of compound to inhibit the neurotransmitter norepinephrine-NE reuptake system using [3H]norepinephrine as radioligand
- ChEMBL_177242 (CHEMBL783715) Inhibition of norepinephrine uptake in synaptosomal preparation fro rat hypothalamus, using [3H]norepinephrine
- ChEMBL_487422 (CHEMBL1020016) Inhibition of norepinephrine uptake at human norepinephrine transporter expressed in MDCK-Net6 cells
- ChEMBL_142964 (CHEMBL750816) Norepinephrine transporter activity was determined by the ability of compound to inhibit the neurotransmitter norepinephrine-NE reuptake system using [3H]norepinephrine as radioligand
- ChEMBL_142620 (CHEMBL751158) Selectivity for norepinephrine transporter
- ChEMBL_495766 (CHEMBL1007885) Inhibition of norepinephrine transporter
- ChEMBL_761553 (CHEMBL1817433) Inhibition of norepinephrine transporter
- ChEMBL_1615835 (CHEMBL3857904) Inhibition of norepinephrine transporter (unknown origin) assessed as suppression of synaptosomal uptake of norepinephrine
- ChEBML_142643 Ability to inhibit reuptake of norepinephrine ([3H]NE) at norepinephrine transporter of rat parietal/occipital region
- ChEBML_143137 Compound was tested for its ability to inhibit the uptake of Norepinephrine in Norepinephrine transporter system
- ChEMBL_142801 (CHEMBL751374) Binding affinity against norepinephrine transporter
- ChEMBL_2433137 Inhibition of norepinephrine transporter (unknown origin)
- ChEMBL_2437095 Inhibition of norepinephrine transporter (unknown origin)
- ChEMBL_2521086 Inhibition of norepinephrine transporter (unknown origin)
- ChEMBL_321161 (CHEMBL885188) Inhibition constant against norepinephrine transporter
- ChEMBL_333146 (CHEMBL865923) Inhibition of reuptake of Norepinephrine
- ChEMBL_458982 (CHEMBL925076) Binding affinity to norepinephrine transporter
- ChEMBL_520036 (CHEMBL939875) Binding affinity to norepinephrine transporter
- ChEMBL_539366 (CHEMBL1027250) Binding affinity to norepinephrine transporter
- ChEMBL_806656 (CHEMBL1960298) Inhibition of human norepinephrine transporter
- ChEMBL_818589 (CHEMBL2032876) Binding affinity to norepinephrine transporter
- ChEMBL_142643 (CHEMBL747094) Ability to inhibit reuptake of norepinephrine ([3H]NE) at norepinephrine transporter of rat parietal/occipital region
- ChEMBL_142949 (CHEMBL750801) Compound was tested for the ability to inhibit [3H]norepinephrine binding to Norepinephrine transporter in rat synaptosomes
- ChEMBL_142950 (CHEMBL750802) Compound was tested for the ability to inhibit [3H]norepinephrine binding to Norepinephrine transporter in rat synaptosomes
- ChEMBL_2162544 (CHEMBL5047405) Inhibition of norepinephrine transporter (unknown origin)
- ChEMBL_320813 (CHEMBL872348) Binding inhibition towards human norepinephrine transporter
- ChEMBL_464100 (CHEMBL948141) Inhibition of NET mediated norepinephrine uptake
- ChEMBL_699574 (CHEMBL1647932) Inhibition of human recombinant norepinephrine transporter
- ChEMBL_726927 (CHEMBL1686716) Inhibition of human recombinant Norepinephrine transporter
- ChEMBL_761643 (CHEMBL1816547) Inhibition of recombinant human norepinephrine transporter
- ChEBML_142803 The compound was tested for inhibition of [3H]norepinephrine uptake in HEK cells by expressing cDNA for human norepinephrine transporter
- ChEBML_142625 Inhibition of [3H]mazindol binding to Norepinephrine transporter
- ChEBML_142956 Inhibition of Norepinephrine uptake from rat diencephalon-midbrain
- ChEBML_184434 Inhibition of norepinephrine (NE) into rat brain synaptosomes
- ChEMBL_142778 (CHEMBL883548) Displacement of [3H]-Nisoxetine from norepinephrine transporter
- ChEMBL_1525555 (CHEMBL3637062) Binding affinity to norepinephrine transporter (unknown origin)
- ChEMBL_320846 (CHEMBL884631) Inhibition of monoamine reuptake at norepinephrine transporter
- ChEMBL_486188 (CHEMBL1016596) Displacement of [3H]DMI from norepinephrine transporter
- ChEMBL_556594 (CHEMBL958093) Displacement of [3H]nisoxetine from norepinephrine transporter
- ChEMBL_658576 (CHEMBL1247909) Binding affinity to human recombinant norepinephrine transporter
- ChEMBL_807238 (CHEMBL1960168) Inhibition of rat NET-mediated norepinephrine reuptake
- ChEMBL_824331 (CHEMBL2044473) Inhibition of rat NET-mediated norepinephrine reuptake
- ChEMBL_142803 (CHEMBL751376) The compound was tested for inhibition of [3H]norepinephrine uptake in HEK cells by expressing cDNA for human norepinephrine transporter
- Norepinephrine Uptake Assay (IC50) IC50 Values were obtained from inhibition of norepinephrine uptake in MDCK-Net6 cells, stably transfected with the human NET.
- ChEBML_131452 Tested in vitro for norepinephrine (NE) neuronal uptake inhibition
- ChEBML_142612 Inhibition of [3H]nisoxetine binding to norepinephrine (NE) transporter
- ChEMBL_142625 (CHEMBL751162) Inhibition of [3H]mazindol binding to Norepinephrine transporter
- ChEMBL_142627 (CHEMBL751164) Inhibition of [3H]- nisoxatine binding to Norepinephrine transporter
- ChEMBL_142937 (CHEMBL750366) In vitro binding affinity on cloned Norepinephrine transporter
- ChEMBL_142948 (CHEMBL750800) Binding potency for Norepinephrine transporter using [3H]NE
- ChEMBL_144981 (CHEMBL754323) Inhibition of [3H]nisoxetine binding at norepinephrine transporter
- ChEMBL_184434 (CHEMBL789206) Inhibition of norepinephrine (NE) into rat brain synaptosomes
- ChEMBL_320832 (CHEMBL871674) In vitro binding affinity towards human norepinephrine transporter
- ChEMBL_491871 (CHEMBL946208) Inhibition of norepinephrine uptake at human cloned NET
- ChEBML_143113 Binding affinity to norepinephrine (NE) transporter in rat forebrain tissue
- ChEBML_143139 Binding affinity towards Norepinephrine transporter using [3H]nisoxitine as radioligand
- ChEBML_193336 Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes
- ChEMBL_131452 (CHEMBL740207) Tested in vitro for norepinephrine (NE) neuronal uptake inhibition
- ChEMBL_142638 (CHEMBL746906) Inhibition of reuptake of [3H]-NE at Norepinephrine transporter
- ChEMBL_142957 (CHEMBL750809) Inhibition of [3H]nisoxetine binding to norepinephrine (NE) transporter
- ChEMBL_143118 (CHEMBL748000) Evaluated for the Competitive inhibition of uptake of norepinephrine
- ChEMBL_143141 (CHEMBL872658) Compound was evaluated for binding to Norepinephrine Transporter (NET).
- ChEMBL_144985 (CHEMBL754327) Displacement of [3H]nisoxetine from rat brain norepinephrine transporter
- ChEMBL_144993 (CHEMBL755919) Affinity for norepinephrine transporter determined by [3H]nisoxetine displacement.
- ChEMBL_144998 (CHEMBL756260) Inhibitory constant against norepinephrine transporter receptor using [3H]radioligand
- ChEMBL_1803913 (CHEMBL4276205) Inhibition of [3H]norepinephrine uptake at NET (unknown origin)
- ChEMBL_2329125 Binding affinity at human Norepinephrine transporter assessed as inhibition constant
- ChEMBL_302810 (CHEMBL838518) Inhibition of [3H]-nisoxetine binding to rat norepinephrine transporter
- ChEMBL_303056 (CHEMBL828882) Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter
- ChEMBL_357806 (CHEMBL862270) Binding affinity to norepinephrine transporter by radioligand binding assay
- ChEBML_142629 In vitro inhibition of [3H]norepinephrine uptake in rat brain synaptosomes
- ChEBML_142786 Inhibitory activity against Norepinephrine N-methyl-transferase of bovine adrenal glands
- ChEBML_142787 Inhibitory activity against bovine adrenal norepinephrine N-methyl-transferase was determined
- ChEBML_142962 Inhibitory activity against radioligand [3H]nisoxetine binding at the norepinephrine transporter
- ChEBML_143115 Displacement of [3H]-nisoxatine from norepinephrine transporter of rat brain membrane
- ChEBML_177401 Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes
- ChEMBL_1344246 (CHEMBL3256076) Inhibition of NET-mediated norepinephrine uptake in rat brain synaptosomes
- ChEMBL_140884 (CHEMBL748007) Binding affinity for norepinephrine transporter (NET) labeled with [3H]nisoxetine
- ChEMBL_142775 (CHEMBL750496) Compound was tested for the inhibition of norepinephrine (NE) reuptake
- ChEMBL_142955 (CHEMBL750807) Inhibition of norepinephrine transporter (NET) determined using [3H]nisoxetine radioligand.
- ChEMBL_142961 (CHEMBL750813) Inhibitory activity against Norepinephrine transporter using 0.5 nM [3H]-radioligand
- ChEMBL_142963 (CHEMBL750815) Inhibitory concentration binding to Norepinephrine transporter using 0.2 nM paroxetine
- ChEMBL_142965 (CHEMBL750817) Selectivity for the norepinephrine transporter using [3H]nisoxetine binding assay
- ChEMBL_143116 (CHEMBL747998) Displacement of from norepinephrine transporter of frozen rat caudate membranes
- ChEMBL_143119 (CHEMBL748001) Evaluated for the Non competitive inhibition of uptake of norepinephrine
- ChEMBL_143122 (CHEMBL748004) Inhibition of 0.5 nM [3H]nisoxetine binding to Norepinephrine transporter
- ChEMBL_144980 (CHEMBL754322) Inhibition of [3H]nisoxetine binding at norepinephrine transporter was determined
- ChEMBL_144982 (CHEMBL754324) Inhibitory concentration binding to Norepinephrine transporter using 0.2 nM paroxetine
- ChEMBL_144990 (CHEMBL755916) Displacement of [3H]NE from Norepinephrine transporter of rat brain
- ChEMBL_144992 (CHEMBL755918) Inhibition of [3H]nisoxetine binding at norepinephrine transporter was determined
- ChEMBL_193336 (CHEMBL802855) Inhibition of uptake of tritiated norepinephrine (NE) in rat synaptosomes
- ChEMBL_348646 (CHEMBL866255) Inhibition of potassium-evoked [3H]norepinephrine release from rat neocortex
- ChEMBL_376176 (CHEMBL869312) Inhibition of rat NET-mediated norepinephrine uptake in CHO cells
- ChEMBL_491868 (CHEMBL946205) Inhibition of norepinephrine uptake at NET in rat brain synaptosome
- ChEMBL_976616 (CHEMBL2416948) Binding affinity to human norepinephrine transporter by ligand displacement assay
- ChEBML_142789 The inhibitory constant(Ki) value for Norepinephrine N-methyl-transferase was calculated
- ChEBML_142807 Ability to inhibit [3H]nisoxetine binding to cloned human norepinephrine (NE) transporter
- ChEBML_143128 Inhibition of [3H]NE binding to norepinephrine transporter of rat brain synaptosomes
- ChEBML_143135 Norepinephrine transporter activity was determined by inhibition of monoamine [3H]-NE reuptake
- ChEMBL_140759 (CHEMBL748033) In vitro inhibition of [3H]norepinephrine uptake in rat brain synaptosomes
- ChEMBL_142609 (CHEMBL751148) Ability to inhibit the reuptake of NE at human norepinephrine transporter
- ChEMBL_142629 (CHEMBL746897) In vitro inhibition of [3H]norepinephrine uptake in rat brain synaptosomes
- ChEMBL_142785 (CHEMBL752160) Inhibition of reuptake of [3H]-NE (20 nM) by norepinephrine transporter
- ChEMBL_142786 (CHEMBL752161) Inhibitory activity against Norepinephrine N-methyl-transferase of bovine adrenal glands
- ChEMBL_142799 (CHEMBL751372) Inhibition of [3H]norepinephrine uptake in HEK cells expressing human NET
- ChEMBL_142800 (CHEMBL751373) Inhibition of [3H]norepinephrine uptake in HEK cells expressing human NET
- ChEMBL_142802 (CHEMBL751375) Inhibition of [3H]- NE uptake in HEK cells expressing norepinephrine transporter
- ChEMBL_142952 (CHEMBL750804) In vitro inhibition of [3H]norepinephrine uptake in rat brain synaptosomes
- ChEMBL_142962 (CHEMBL750814) Inhibitory activity against radioligand [3H]nisoxetine binding at the norepinephrine transporter
- ChEMBL_142970 (CHEMBL751450) Displacement of [3H]-nisoxatine from Norepinephrine transporter of rat forebrain membrane
- ChEMBL_143110 (CHEMBL749359) Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat brain
- ChEMBL_143112 (CHEMBL749361) Binding affinity towards norepinephrine transporter was determined using [3H]nisoxetine radioligand.
- ChEMBL_143115 (CHEMBL747997) Displacement of [3H]-nisoxatine from norepinephrine transporter of rat brain membrane
- ChEMBL_143124 (CHEMBL744029) Inhibition of [3H]NE uptake by rat frontal cortex Norepinephrine transporter
- ChEMBL_144967 (CHEMBL755085) Inhibition of Norepinephrine (NA) reuptake using cloned human transporter was determined
- ChEMBL_177401 (CHEMBL782724) Inhibition of uptake of tritiated norepinephrine (NE) into rat brain synaptosomes
- ChEMBL_303198 (CHEMBL829824) Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]-NE
- ChEMBL_303312 (CHEMBL840038) Displacement of [3H]nisoxetine from norepinephrine transporter of rat cerebral cortex
- ChEMBL_303514 (CHEMBL839628) Inhibition of [3H]-nisoxetine binding to Norepinephrine transporter from rat cortex
- ChEMBL_303519 (CHEMBL839633) Binding affinity for Norepinephrine transporter (NET) expressed in LCK PK1 cells
- ChEMBL_305586 (CHEMBL828033) Inhibition of rat brain Norepinephrine transporter as accumulation of [3H]NE
- ChEMBL_306351 (CHEMBL828170) Inhibition of [3H]nisoxetine binding to rat cerebral cortex norepinephrine transporter
- ChEMBL_467790 (CHEMBL931354) Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
- ChEMBL_469595 (CHEMBL934068) Displacement of [3H]nisoxetine from norepinephrine transporter in rat brain homogenate
- ChEMBL_491609 (CHEMBL945185) Inhibition of norepinephrine uptake at human NET in human HEK293 cells
- ChEMBL_510054 (CHEMBL995197) Inhibition of norepinephrine uptake at human NET expressed in HEK cells
- ChEMBL_510091 (CHEMBL998745) Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
- ChEMBL_523089 (CHEMBL1004119) Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
- ChEMBL_535516 (CHEMBL986142) Inhibition of norepinephrine uptake at human NET expressed in MDCK cells
- ChEMBL_558433 (CHEMBL963839) Inhibition of norepinephrine uptake at human NET transfected in HEK cells
- ChEMBL_589388 (CHEMBL1047383) Inhibition of norepinephrine uptake at human NET expressed in HEK293 cells
- ChEMBL_634326 (CHEMBL1120739) Inhibition of human NET-mediated norepinephrine uptake in MDCK-Net6 cells
- ChEMBL_654118 (CHEMBL1228924) Inhibition of norepinephrine reuptake at human NET expressed in MDCK cells
- ChEBML_129897 In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices
- ChEBML_142631 Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum
- ChEBML_142958 Inhibition of the NE [3H]norepinephrine uptake by rat brain slices In vitro
- ChEBML_142968 Ability to displace [3H]- nisoxetin from Norepinephrine transporter in rat cerebral cortical homogenate
- ChEBML_143108 Binding affinity at norepinephrine transporter using [3H]nisoxetine as radioligand from rat brain
- ChEBML_144987 Inhibition of [3H]-NE reuptake at Norepinephrine transporter in rat parietal/occipital cortex
- ChEBML_144988 Ability to displace [3H]-nisoxatine radioligand for the Norepinephrine transporter in rat brain
- ChEMBL_140882 (CHEMBL752513) Compound was evaluated for its binding affinity towards human NET (norepinephrine) transporter
- ChEMBL_140883 (CHEMBL748006) Compound was evaluated for its binding affinity towards human NET(norepinephrine) transporter
- ChEMBL_142795 (CHEMBL751368) Binding affinity against norepinephrine transporter by using [3H]nisoxetine as a radioligand
- ChEMBL_142807 (CHEMBL882765) Ability to inhibit [3H]nisoxetine binding to cloned human norepinephrine (NE) transporter
- ChEMBL_142943 (CHEMBL750795) Binding affinity against Norepinephrine transporter using [3H]nisoxetine in midbrain of rat
- ChEMBL_142945 (CHEMBL750797) Binding affinity towards norepinephrine transporter was determined by using [3H]nisoxetine radioligand
- ChEMBL_142960 (CHEMBL750812) Inhibition of [3H]nisoxetine binding to the norepinephrine transporter in rat midbrain.
- ChEMBL_142969 (CHEMBL751449) Displacement of [3H]nisoxetine from norepinephrine transporter (NET) in rat brain membranes
- ChEMBL_143128 (CHEMBL744172) Inhibition of [3H]NE binding to norepinephrine transporter of rat brain synaptosomes
- ChEMBL_143134 (CHEMBL744178) Compound was tested for inhibiting reuptake of [3H]- NE by norepinephrine transporter
- ChEMBL_143135 (CHEMBL744179) Norepinephrine transporter activity was determined by inhibition of monoamine [3H]-NE reuptake
- ChEMBL_144983 (CHEMBL754325) Ability to inhibit [3H]NE reuptake at norepinephrine transporter from rat brain
- ChEMBL_144986 (CHEMBL754328) Binding affinity towards norepinephrine transporter using [3H]nisoxetine as radioligand was determined
- ChEMBL_1452255 (CHEMBL3366167) Displacement of [3H]Nisoxetine from human Norepinephrine transporter by liquid scintillation counting
- ChEMBL_193312 (CHEMBL806826) Inhibitory activity against norepinephrine (NE) uptake in rat whole brain synaptosome preparation
- ChEMBL_302942 (CHEMBL841777) In vitro binding affinity against norepinephrine transporter using [3H]-nisoxetine as radioligand
- ChEMBL_303224 (CHEMBL827189) Inhibition of [3H]nisoxetine binding to rat norepinephrine transporter at 10 uM
- ChEMBL_303548 (CHEMBL839753) Displacement of [3H]nisoxetine from norepinephrine transporter (NET) of rat cerebral cortex
- ChEMBL_303591 (CHEMBL829602) Displacement of [3H]-nisoxetine from norepinephrine transporter of rat cerebral corticex homogenate
- ChEMBL_306091 (CHEMBL830866) Inhibition of [3H]nisoxetine binding to norepinephrine transporter of rat cerebral cortex
- ChEMBL_334929 (CHEMBL859244) Inhibition of [3H] norepinephrine uptake into human NET expressed in HEK293 cells
- ChEMBL_499923 (CHEMBL979833) Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells
- ChEMBL_500244 (CHEMBL966882) Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells
- ChEMBL_541290 (CHEMBL1031549) Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK cells
- ChEMBL_558178 (CHEMBL962312) Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells
- ChEMBL_595700 (CHEMBL1041763) Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells
- ChEMBL_598114 (CHEMBL1038296) Inhibition of norepinephrine reuptake at human NET expressed in MDCK-Net6 cells
- ChEMBL_610770 (CHEMBL1064405) Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells
- ChEMBL_611007 (CHEMBL1072383) Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells
- ChEMBL_617684 (CHEMBL1101480) Inhibition of norepinephrine uptake at human NET expressed in MDCK-Net6 cells
- ChEBML_143133 Binding affinity towards norepinephrine transporter by displacement of [3H]nisoxetine radioligand from rat brain
- ChEBML_145001 Compound was tested for inhibition of [3H]NE binding to norepinephrine transporter HEK cells
- ChEMBL_129897 (CHEMBL740142) In vitro inhibition of accumulation of (-)-[3H]Norepinephrine (NA) in mouse brain slices
- ChEMBL_140880 (CHEMBL752511) Inhibition of [3H]NE reuptake by human norepinephrine transporter expressed in HEK293 cells
- ChEMBL_142628 (CHEMBL746896) Concentration causing 50% Inhibition of binding of [3H]- nisoxatine to Norepinephrine transporter (NET).
- ChEMBL_142631 (CHEMBL746899) Inhibition of binding of [3H]nisoxetine to (NET) norepinephrine transporter in rat striatum
- ChEMBL_142639 (CHEMBL746907) Inhibition of [3H]NE uptake by Norepinephrine transporter of rat occipital cortex synaptosomes
- ChEMBL_142640 (CHEMBL746908) Inhibition of [3H]NE uptake by Norepinephrine transporter of rat occipital cortex synaptosomes
- ChEMBL_142779 (CHEMBL750499) Compound was tested for its ability to displace [3H]citalopram from norepinephrine transporter
- ChEMBL_142783 (CHEMBL752158) Inhibition of [3H]nisoxetine binding to norepinephrine transporter (NET) of rat cortical homogenates
- ChEMBL_142784 (CHEMBL752159) Binding affinity against norepinephrine cloned human transporter using 40-80 pM [125I]RTI
- ChEMBL_142942 (CHEMBL872842) Affinity at norepinephrine transporter (NET) in rat striatum, using [3H]- nisoxatine as radioligand
- ChEMBL_142947 (CHEMBL750799) Binding affinity towards Norepinephrine transporter was determined using NE[3H]Nisoxetine as radioligand
- ChEMBL_142951 (CHEMBL750803) Inhibition of norepinephrine Transporter Affinity against rat whole brain using [3H]nisoxetine radioligand
- ChEMBL_143109 (CHEMBL872668) Binding affinity for norepinephrine transporter in rat brain using [3H]-nisoxatine as radioligand
- ChEMBL_144975 (CHEMBL753707) Binding affinity towards norepinephrine transporter in rat striatum using [3H]nisoxetine as radioligand
- ChEMBL_144977 (CHEMBL753709) Binding affinity at the norepinephrine transporter in rat striatum by [3H]nisoxetine displacement.
- ChEMBL_144987 (CHEMBL754231) Inhibition of [3H]-NE reuptake at Norepinephrine transporter in rat parietal/occipital cortex
- ChEMBL_144988 (CHEMBL754232) Ability to displace [3H]-nisoxatine radioligand for the Norepinephrine transporter in rat brain
- ChEMBL_145004 (CHEMBL756266) Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells
- ChEMBL_1558447 (CHEMBL3773323) Inhibition of recombinant human norepinephrine transporter assessed as reduction in [3H]-NA reuptake
- ChEMBL_1559990 (CHEMBL3777268) Displacement of [3H]nisoxentine from human recombinant norepinephrine transporter expressed in CHO cells
- ChEMBL_197580 (CHEMBL803007) Binding affinity against human cloned norepinephrine transporter using 40-80 pM [125I]RTI.
- ChEMBL_306359 (CHEMBL828236) Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK293 cells
- ChEMBL_487421 (CHEMBL1020015) Displacement of [3H]nisoxetine from human norepinephrine transporter expressed in MDCK-Net6 cells
- ChEMBL_62322 (CHEMBL674261) Displacement of [125I]RTI-55 from human Norepinephrine transporter expressed in HEK cells
- ChEBML_142788 Tested for inhibitory activity against bovine adrenal norepinephrine N-methyl-transferase using phenylethanolamine as substrate
- ChEBML_142939 Binding affinity to Norepinephrine transporter using [3H]-nisoxatine as radioligand in stably transfected NIH3T3 cells
- ChEBML_143123 Inhibition of [3H]NE uptake at Norepinephrine transporter in rat parietal/occipital cortex was determined
- ChEBML_143125 Inhibition of norepinephrine transporter by inhibition of [3H]NE uptake into rat nerve endings (synaptosomes)
- ChEBML_144989 Compound was tested for the inhibition of norepinephrine [3H]NE reuptake into rat cortical membranes
- ChEMBL_142624 (CHEMBL882167) 50% Inhibition against Norepinephrine transporter in rat cerebral cortex by displacing [3H]nisoxetine radioligand
- ChEMBL_142630 (CHEMBL746898) Inhibition of binding of [3H]- nisoxatine to Norepinephrine transporter (NET) of rat cerebral cortex.
- ChEMBL_142632 (CHEMBL746900) The binding affinity at the Norepinephrine transporter reuptake sites determined using competition binding assay
- ChEMBL_142935 (CHEMBL750364) Inhibition of [125I]RTI-55 binding to norepinephrine transporter (NET) expressed in HEK cells
- ChEMBL_143133 (CHEMBL744177) Binding affinity towards norepinephrine transporter by displacement of [3H]nisoxetine radioligand from rat brain
- ChEMBL_143140 (CHEMBL744184) Compound was evaluated for binding to Norepinephrine Transporter (NET) using [3H]desmethylimipramine as radioligand
- ChEMBL_145001 (CHEMBL756263) Compound was tested for inhibition of [3H]NE binding to norepinephrine transporter HEK cells
- ChEMBL_2068294 (CHEMBL4723547) Displacement of [3H]nisoxetine from norepinephrine transporter (unknown origin) by liquid scintillation counting method
- ChEMBL_302666 (CHEMBL839954) Inhibitory constant for [3H]NE reuptake at norepinephrine transporter of rat parietal-occipital cortex
- ChEMBL_303505 (CHEMBL839977) In vitro displacement of [3H]nisoxetine from human norepinephrine transporter expressed in HEK293 cells
- ChEMBL_699309 (CHEMBL1647129) Inhibition of [3H]norepinephrine reuptake at NET in rat brain synaptosome by scintillation counting
- ChEMBL_741840 (CHEMBL1769985) Inhibition of human NET in HEK293 cells assessed as inhibition of [3H]norepinephrine uptake
- ChEMBL_974162 (CHEMBL2411004) Displacement of [3H]-norepinephrine from human NET expressed in CHO cells by TopCounting analysis
- ChEBML_1711465 Displacement of [3H]nisoxetine from recombinant human norepinephrine transporter after 120 mins by scintillation counting analysis
- ChEMBL_140881 (CHEMBL752512) Binding affinity at the norepinephrine transporter was measured using [125I]RTI-55 as a radioligand
- ChEMBL_142613 (CHEMBL751151) Compound was tested for inhibition of [125I]-RTI-55 binding to norepinephrine transporter HEK cells
- ChEMBL_142614 (CHEMBL751152) Inhibition of [125I]- RTI -55 binding at the Norepinephrine transporter sites on HEK-hNET cells
- ChEMBL_142940 (CHEMBL750369) In vitro binding affinity against monoamine transporter NET (norepinephrine transporter) in LLC-PK1 cell membranes.
- ChEMBL_143121 (CHEMBL748003) In vitro binding affinity towards Norepinephrine transporter rat cerebral cortical homogenates by [3H]nisoxetine displacement.
- ChEMBL_143123 (CHEMBL748005) Inhibition of [3H]NE uptake at Norepinephrine transporter in rat parietal/occipital cortex was determined
- ChEMBL_1442873 (CHEMBL3377151) Induction of NET-mediated norepinephrine release in rat brain synaptosomes by [3H]NE release assay
- ChEMBL_1442878 (CHEMBL3377156) Inhibition of NET-mediated norepinephrine release in rat brain synaptosomes by [3H]NE release assay
- ChEMBL_144974 (CHEMBL753706) Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats
- ChEMBL_144984 (CHEMBL754326) Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats
- ChEMBL_1654664 (CHEMBL4004030) Inhibition of NET (unknown origin) expressed in HEK293 cells assessed as reduction in norepinephrine reuptake
- ChEMBL_302728 (CHEMBL838676) Inhibitory constant against reuptake of [3H]NE at norepinephrine transporter of rat parietal-occipital cortex
- ChEMBL_303772 (CHEMBL830129) In vitro inhibition of [3H]nisoxetine binding to norepinephrine transporter expressed in human kidney cells
- ChEMBL_699305 (CHEMBL1647125) Inhibition of [3H]norepinephrine reuptake at human NET expressed in MDCK cells by scintillation counting
- ChEMBL_769841 (CHEMBL1831835) Inhibition of human NET expressed in MDCK-Net6 cells assessed as inhibition of norepinephrine uptake
- ChEBML_142806 Equilibrium dissociation constant (KD) for Competitive binding between [3H]- nisoxatine and the compound at human Norepinephrine transporter
- ChEBML_142934 Binding affinity to norepinephrine (NE) transporter in membranes of cells selectively expressing the human genes for NET
- ChEMBL_1456969 (CHEMBL3368420) Inhibition of [3H]-NE uptake in human norepinephrine transporter expressed in HEK293 cells by scintillation counting
- ChEMBL_1745411 (CHEMBL4179921) Displacement of [3H]nisoxetine from recombinant human norepinephrine transporter after 120 min by scintillation counting method
- ChEMBL_1864054 (CHEMBL4365029) Displacement of [3H]nisoxetine from recombinant human norepinephrine transporter after 120 mins by scintillation counting analysis
- ChEMBL_583225 (CHEMBL1055024) Inhibition of [3H]norepinephrine uptake at human NET expressed in MDCK-Net6 cells by scintillation counting
- ChEMBL_726960 (CHEMBL1686749) Inhibition of [3H]norepinephrine reuptake at human recombinant NET expressed in HEK293 cells by scintillation counting
- ChEMBL_792745 (CHEMBL1930660) Inhibition of [3H]norepinephrine reuptake at human NET cloned in rat brain synaptosome by scintillation counting
- ChEMBL_806517 (CHEMBL1959650) Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells after 120 mins
- ChEMBL_142645 (CHEMBL747096) Tested for the binding affinity towards Norepinephrine transporter in rat cerebral cortex by displacing [3H]nisoxetine radioligand
- ChEMBL_142794 (CHEMBL752762) Compound was evaluated for inhibition of [3H]NE uptake in HEK-hNET cells expressing Human norepinephrine transporter
- ChEMBL_142954 (CHEMBL750806) In vitro inhibitory activity against radioligand [3H]-nisoxatine binding to norepinephrine transporter (NET) in rat cortical tissue
- ChEMBL_143106 (CHEMBL749356) Affinity for the displacement of [3H]paroxetine binding to norepinephrine transporter (NET) in rat frontal cortex membranes
- ChEMBL_1505018 (CHEMBL3595873) Inhibition of human NET expressed in CHOK1 cells incubated for 45 mins by [3H]-norepinephrine uptake assay
- ChEMBL_33178 (CHEMBL642052) In vitro ability to inhibit norepinephrine binding to alpha-2 adrenergic receptor of guinea pig vas deferens
- ChEBML_142946 Binding affinity was evaluated by measuring inhibiting the binding of [3H]nisoxetine to Norepinephrine transporter in rat brain tissue
- ChEMBL_142636 (CHEMBL746904) Inhibition of high affinity uptake of [3H]NE by norepinephrine transporter in nerve endings obtained from rat brain.
- ChEMBL_142637 (CHEMBL746905) Binding affinity for Norepinephrine transporter is assessed from the ability to displace [3H]nisoxetine from rat frontal cortex
- ChEMBL_142804 (CHEMBL751377) The compound was tested in vitro for binding affinity for the norepinephrine transporter (NET) using competitive binding assay.
- ChEMBL_142944 (CHEMBL750796) Binding affinity at the Norepinephrine transporter in rat frontal cortex by inhibition of 0.5 nM [3H]nisoxetine binding
- ChEMBL_1456596 (CHEMBL3369978) Inhibition of [3H]norepinephrine reuptake at human NET expressed in CHO cells after 45 mins by scintillation counting
- ChEMBL_1929929 (CHEMBL4433105) Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by liquid scintillation counting method
- ChEMBL_641577 (CHEMBL1176114) Inhibition of [3H]norepinephrine reuptake at human NET expressed in HEK293 cells after 90 mins by scintillation counting
- ChEBML_143114 Compound has been evaluated for its affinity towards Norepinephrine transporter by displacing the radio isotope [3H]nisoxetine from rat forebrain
- ChEMBL_142635 (CHEMBL746903) Ability to inhibit high affinity reuptake of [3H]-NE (Norepinephrine transporter) into nerve ending synaptosomes prepared from brain regions
- ChEMBL_142946 (CHEMBL750798) Binding affinity was evaluated by measuring inhibiting the binding of [3H]nisoxetine to Norepinephrine transporter in rat brain tissue
- ChEMBL_143105 (CHEMBL749355) Ability to inhibit high affinity uptake of [3H]NE at Norepinephrine transporter (NET) using rat brain parietal/occipital cortex
- ChEMBL_144969 (CHEMBL753702) In vitro binding affinity against human norepinephrine transporter in human embryonic kidney cell line by using [3H]-nisoxatine radioligand
- ChEMBL_144972 (CHEMBL753705) In vitro competitive binding versus [3H]- nisoxatine in murine kidney cells transfected with cDNA for human norepinephrine transporter (NET)
- ChEMBL_144973 (CHEMBL873910) In vitro competitive binding versus [3H]- nisoxatine in murine kidney cells transfected with cDNA for human norepinephrine transporter (NET)
- ChEMBL_1455467 (CHEMBL3363899) Inhibition of norepinephrine reuptake at human NET expressed in HEK293 cells after 15 mins by fluorescence neurotransmitter transporter assay
- ChEMBL_1651928 (CHEMBL4001183) Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells after 120 mins by scintillation counting
- ChEMBL_1657815 (CHEMBL4007285) Inhibition of [3H]-5-norepinephrine reuptake in human NET expressed in HEK293 cells by microbeta liquid scintillation counting method
- ChEMBL_490890 (CHEMBL989166) Displacement of [125I]PIC from human imidazoline receptor 1 in human platelets analyzed under norepinephrine mask of alpha 2AR
- ChEMBL_493240 (CHEMBL948470) Displacement of Levo[ring-2,5,6-3H]norepinephrine from human cloned NET expressed in HEK293 cells by microplate scintillation counter
- ChEMBL_493243 (CHEMBL948473) Displacement of Levo[ring-2,5,6-3H]norepinephrine from rat synaptosomal NET expressed in HEK293 cells by microplate scintillation counter
- ChEMBL_142619 (CHEMBL751157) In vitro binding affinity in LLC-PK1 cells by Norepinephrine transporter binding assay by using [125I]-IPT as a radioligand
- ChEMBL_142972 (CHEMBL752042) Ability to inhibit high affinity uptake of norepinephrine transporter into the nerve endings of rat synaptosomes using [3H]NE radioligand
- ChEMBL_144968 (CHEMBL755086) In vitro binding affinity against human norepinephrine transporter in human embryonic kidney cell line using [125I]RTI-55 as radioligand
- ChEMBL_144970 (CHEMBL753703) In vitro binding affinity against human norepinephrine transporter in human embryonic kidney cell line by using [125I]-RTI-55 radioligand
- ChEMBL_303717 (CHEMBL829052) Inhibition of high affinity uptake by the norepinephrine transporter from rat synaptosomal nerve endings by using [3H]NE as radioligand
- ChEMBL_33177 (CHEMBL642051) Alpha-2-adrenolytic activity was assessed in vitro from the ability to inhibit norepinephrine binding to guinea pig vas deferens
- ChEMBL_687286 (CHEMBL1291962) Displacement of [3H]nisoxetine from norepinephrine transporter in Sprague-Dawley rat frontal cortex after 1 hr by liquid scintillation counting
- ChEBML_143120 In vitro binding affinity of compound for Norepinephrine (NE) transporter with [3H]- nisoxatine as radioligand in corpus striatum tissue from rat forebrain
- ChEMBL_1356559 (CHEMBL3286058) Inhibition of [3H]norepinephrine uptake at NET expressed in rat hypothalamic homogenate containing synaptosomes after 5 mins by scintillation counting analysis
- ChEMBL_142793 (CHEMBL872959) Compound was evaluated for binding affinity using [125I]RTI-55 as a radioligand in HEK-hNET cells expressing human norepinephrine transporter
- ChEMBL_1513492 (CHEMBL3611848) Antagonist activity at human alpha1B adrenoceptor assessed as inhibition of norepinephrine-induced increase of intracellular calcium level by cell based assay
- ChEMBL_1633616 (CHEMBL3876408) Displacement of [3H]nisoxetine from human recombinant norepinephrine transporter expressed in CHO cells measured after 120 mins by scintillation counting method
- ChEBML_144978 Evaluated for ability to inhibit high affinity uptake of [3H]-NE using rat nerve endings obtained from brain regions enriched in Norepinephrine transporter
- ChEMBL_142607 (CHEMBL751146) Ability to displace [125I]- RTI-55 binding at the Norepinephrine transporter site on HEK cells expressing cDNA for the human transporter (hNET)
- ChEMBL_142936 (CHEMBL750365) Compound was tested for its affinity by the inhibition of [125I]RTI-55 binding at norepinephrine transporter (NET) transfected in HEK cells
- ChEMBL_142971 (CHEMBL752041) Ability to inhibit high affinity uptake of norepinephrine transporter into the nerve endings of rat synaptosomes using [3H]NE as a radioligand
- ChEMBL_1617625 (CHEMBL3859694) Antagonist activity at alpha1A adrenoceptor in Sprague-Dawley rat urethra assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
- ChEMBL_1617626 (CHEMBL3859695) Antagonist activity at alpha1B adrenoceptor in Sprague-Dawley rat aorta assessed as inhibition of norepinephrine-induced smooth muscle contraction after 20 mins
- ChEMBL_1803914 (CHEMBL4276206) Inhibition of [3H]norepinephrine uptake at human NET expressed in HEK293 cells after 15 to 20 mins by microbeta scintillation counting method
- ChEMBL_144978 (CHEMBL753710) Evaluated for ability to inhibit high affinity uptake of [3H]-NE using rat nerve endings obtained from brain regions enriched in Norepinephrine transporter
- ChEMBL_1586596 (CHEMBL3821817) Inhibition of human NET expressed in CHO cells assessed as [3H]-Norepinephrine reuptake incubated for 45 mins measured after 30 mins by topcount method
- ChEMBL_2062317 (CHEMBL4717570) Inhibition of human NET expressed in CHO-K1 cells assessed as inhibition of [3H]-norepinephrine reuptake measured after 45 mins by Microscintillation counting analysis
- ChEMBL_753884 (CHEMBL1798146) Antagonist activity at human adrenergic alpha1A receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
- Norepinephrine, Transporter NET (h) Assay Type: BindingSpecies: HumanOrigin: Recombinant/CHO cellsLigand: [3H]-NisoxetineLigand [M]: 1.00E-09Kd (Binding Affinity): 3.00E-09Bmax: 10 pmol/mg proteinMethod: RadioactivityMeasurement: DPM
- ChEMBL_144979 (CHEMBL754321) Evaluated for its ability to inhibit high affinity uptake of [3H]NE using rat nerve endings obtained from brain regions enriched in norepinephrine transporter (NET)
- Functional Uptake Assay (hNET) Inhibition of human norepinephrine reuptake transporter was assayed using the recombinant human norepinephrine transporter expressed in either HEK293 or MDCK cells using a published method (Galli A et al., J. Exp. Biol. 198: 2197-2212, 1995). The cells were plated before the assay. Test compound and/or vehicle was preincubated with cells in modified HEPES buffer pH 7.1 or pH 7.4 for 20 minutes at 18 to 25° C. Following the preincubation, 25 nM [3H]norepinephrine was added for an additional timed incubation period (10 to 20 minutes). After the cells were washed to remove [3H]norepinephrine not internalized, the cells were lysed, and the amount of tritium in the cell lysate was measured using a liquid scintillation counter to determine [3H]norepinephrine uptake. Non-specific binding of tritium was measured in a control reaction containing 10 uM imipramine (or 10 uM nisoxetine), and was subtracted from the counts for assays to correct for non-specific binding of tritium.
- Functional Uptake Assay (rNET) Quantification of norepinephrine uptake was performed using synaptosomes isolated in a 0.32 M sucrose buffer from a male Wistar rat hypothalamus. The uptake of radiolabelled norepinephrine by synaptosomes (100 ug of proteins/point) was allowed by incubating them for 20 minutes at 37° C. in presence of test compounds and [3H]-norepinephrine (0.1 uCi/point). The experiment was performed in a deep well. Synaptosomes and [3H]-norepinephrine were prepared in a Krebs buffer pH 7.4 containing 25 mM NaHCO3, 11 mM glucose and 50 uM ascorbic acid. This incubation buffer was oxygenated for 5 minutes before incubation. Basal control was incubated for 20 minutes at 4° C. in order to avoid any uptake. Following this incubation, the uptake was stopped by filtration through a unifilter 96-wells GFB Packard plate washed with Krebs buffer containing 25 mM NaHCO3 in order to eliminate the free [3H]-norepinephrine.
- ChEMBL_1777922 (CHEMBL4234914) Inhibition of voltage-dependent L-type calcium channel in Wistar rat 3rd-order mesenteric artery assessed as reduction in norepinephrine-induced vessel contraction by myographic method
- ChEMBL_753885 (CHEMBL1798147) Antagonist activity against human cloned adrenergic Alpha-1B receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
- ChEMBL_753973 (CHEMBL1798356) Antagonist activity against human cloned adrenergic Alpha-1D receptor expressed in HEK293 cells assessed as inhibition of norepinephrine-induced [3H]inositol phosphate hydrolysis by scintillation counting
- ChEMBL_1661733 (CHEMBL4011345) Inhibition of recombinant human NET expressed in HEK293 cell membranes assessed as reduction in [3H]-norepinephrine uptake incubated for 22 mins by micro beta scintillation counting analysis
- ChEMBL_2110695 (CHEMBL4819545) Agonist activity at beta2 adrenoceptor (unknown origin) expressed in sf9 cells assessed as reversal of norepinephrine inhibition of [3H]DHAP binding to beta2 adrenoceptor by radioligand binding assay
- ChEMBL_1824642 (CHEMBL4324406) Inhibition of human N-terminal His6 tagged PNMT using norepinephrine as substrate preincubated for 10 mins in presence of AdoMet followed by substrate addition by fluorescence based SAHH enzyme coupled assay
- ChEMBL_1742585 (CHEMBL4158335) Inhibition of c-terminal hexa-His tagged human MB-COMT expressed in HEK293 cell membrane homogenate using norepinephrine as substrate after 1 hr in presence of SAM by MTase glo methyltransferase assay
- ChEMBL_1742588 (CHEMBL4158338) Inhibition of c-terminal hexa-His tagged rat MB-COMT expressed in HEK293 cell membrane homogenate using norepinephrine as substrate after 1 hr in presence of SAM by MTase glo methyltransferase assay
- Radioligand Binding Assay (Ki) and Norepinephrine Uptake Assay (IC50) Compounds were evaluated the inhibition of [3H] nisoxetine binding to MDCK-Net6 cells, stably transfected with the human norepinephrine transporter (hNET). Data from wells containing 1 uM desipramine were used to define non-specific hNET binding. Total radioligand bound is defined by addition of binding buffer alone in the presence of [3H]nisoxetine (Perkin-Elmer). The radioligand binding reaction was initiated by addition of [3H]nisoxetine, and incubated for 2 h at 37 deg C. The KD value estimated for [3H]nisoxetine was 10 nM using intact whole cells. The inhibition constant (Ki) was calculated by the Cheng and Prusoff equation. IC50 Values were obtained from inhibition of norepinephrine uptake in MDCK-Net6 cells, stably transfected with the human NET.
- Norepinephrine Transporter Binding Assay Human Norepinephrine Transporter (NET) Binding (Antagonist Radioligand) was determined at Panlabs Cerep (assay #204410). Human norepinephrine transporters expressed in dog kidney MDCK cells were used in modified Tris-HCl buffer pH 7.4. A 40 μg‡ aliquot was incubated with 0.2 nM [125I]RTI-55 for 3 hours at 4° C. Non-specific binding was estimated in the presence of 10 μml desipramine. Membranes were filtered and washed, and the filters were then counted to determine [125I]RTI-55 specifically bound. Compounds were assayed using an 8-point titration, with a starting concentration of 10 μM and one-half log serial dilutions. ‡Note: Membrane protein may change from lot to lot, the concentration used is adjusted if necessary. IC50 values were determined by a non-linear, least squares regression analysis using MathIQ™ (IDBusiness Solutions Ltd., UK).
- Binding Assay NE transporter binding assay for evaluating binding of the compound to the norepinephrine transporter was carried out using human recombinant norepinephrine transporter membrane (PerkinElmer Life and Analytical Sciences, USA) expressed in MDCK cells and radioisotope [3H]Nisoxetine (PerkinElmer).That is, the test drug, 6 nM [3H]Nisoxetine, norepinephrine transporter membrane (11 ug/well), 120 mM NaCl and 50 mM Tris-HCl buffer (pH 7.4) containing 5 mM KCl were added to obtain a reaction mixture with a final volume of 0.25 ml. After incubation for 60 minutes at 4° C., the mixture was quickly passed through a Filtermat A glass fiber filter pre-soaked with 0.5% (w/v) PEI (polyethyleneimine) using Inotech Harvester (Inotech) to terminate the reaction. After washing with cold washing buffer (50 mM Tris-HCl, pH 7.4, 0.9% NaCl) solution, the filter was covered with MeltiLex and sealed in a sample bag. After drying in an oven, radioactivity was counted using MicroBeta Plus (Wallac).
- Norepinephrine transporter (NET) Uptake Inhibition ASsay Compound activity was assessed using a convenient in vitro assay. Briefly, HEK cells expressing recombinant NET were plated at 50,000 cells/well on a 96 well plate pre-coated with Matrigel one day prior to the experiment. Culture medium (DMEM/FBS) was removed and 30 μl of assay buffer (Tris-HCl 50 mM, EDTA 4 mM, BDA 0.1%) with the desired concentration of test compound was added. The plate was incubated at 37° C. for 15 minutes. Assay buffer (30 μl) containing the same concentration of compound diluted in [3H]-Norepinephrine uptake buffer (final concentration 20 nM) was added to each well and the plate was incubated at 37° C. for 5 minutes. The reaction mixture was removed, and the cells were washed with 100 μl ice-cold assay buffer twice. Lysis buffer (50 μl) was added to the cells followed by a 5 minute incubation with gentle shaking at room temperature. The lysate was transferred to a 96 well isoplate. Optiphase supermix (100 μl) was added to each well with complete mixing. Radioactivity was counted with Microbeta Counter and reported as CPM. Desipramine was used as a control to measure non-specific uptake and for data normalization. Percent inhibition of [3H]-Norepinephrine uptake calculations: 100×(1−(CPMtest sample−CPMnon-specific uptake)/(CPMMAX−CPMMIN)).
- Radioligand Binding Assay The compounds were evaluated using well established radioligand binding assays protocols (Galli, A. et al., J. Exp. Biol. 1995, 198, 2197-2212; Giros, B. et al., Trends Pharmcol. Sci. 1993, 14, 43-49; Gu, H. et al., J. Biol. Chem. 1994, 269(10), 7124-7130; Shearman, L. P. et al, Am. J. Physiol., 1998, 275(6 Pt 1), C1621-1629; Wolf, W. A. et al., J. Biol. Chem. 1992, 267(29), 20820-20825). The human recombinant transporter proteins dopamine (DAT), norepinephrine (NET) and serotonin (SERT) were selected for the in vitro assays.
- Radioligand Binding Assay (Ki) Compounds were evaluated the inhibition of [3H] nisoxetine binding to MDCK-Net6 cells, stably transfected with the human norepinephrine transporter (hNET). Data from wells containing 1 uM desipramine were used to define non-specific hNET binding. Total radioligand bound is defined by addition of binding buffer alone in the presence of [3H]nisoxetine (Perkin-Elmer). The radioligand binding reaction was initiated by addition of [3H]nisoxetine, and incubated for 2 h at 37 deg C. The KD value estimated for [3H]nisoxetine was 10 nM using intact whole cells. The inhibition constant (Ki) was calculated by the Cheng and Prusoff equation.
- Binding Assay NET: Human norepinephrine transporter (NET) enriched membranes (5 μg) were incubated with 5 nM of radiolabeled [3H]-Nisoxetin in assay buffer containing 50 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, pH 7.4.NSB (non specific binding) was measured by adding 1 μM. After 60 min incubation at 4° C., binding reaction was terminated by filtering through Multiscreen GF/C (Millipore) presoaked in 0.5% polyethyleneimine in Vacuum Manifold Station, followed by 3 washes with ice-cold filtration buffer containing 50 mM Tris-HCl, 0.9% NaCl, pH 7.4.Filter plates were dried at 60° C. for 1 hour and 30 μl of scintillation cocktail were added to each well before radioactivity reading.
- Radioligand Binding Assay The compounds were evaluated using well established radioligand binding assays protocols (Galli, A. et al., J. Exp. Biol. 1995, 198, 2197-2212; Giros, B. et al., Trends Pharmcol. Sci. 1993, 14, 43-49; Gu, H. et al., J. Biol. Chem. 1994, 269(10), 7124-7130; Shearman, L. P. et al, Am. J. Physiol., 1998, 275 (6 Pt 1), C1621-1629; Wolf, W. A. et al., J. Biol. Chem. 1992, 267(29), 20820-20825). The human recombinant transporter proteins dopamine (DAT), norepinephrine (NET) and serotonin (SERT) were selected for the in vitro assays. The radioligand binding assays were carried out at 11 different test concentrations 0.1 nm to 1 μM.
- Uptake Assay Protocol NET: This protocol was designed to measure inhibition of uptake by the human norepinephrine transporter. The reagents were human NET (HEK293F) cells, desipramine (Sigma), nomifensine, neurotransmitter transporter uptake assay kit (Molecular Devices), freestyle 293 expression medium (Invitrogen), 10× Hank's Balanced Salt Solution (HBSS; Invitrogen), 1 M HEPES (Mediatech), Biocoat poly-D-lysine 96-well, black, clear plates (Becton, Dickinson), and 500 μL polypropylene U-bottom 96-well plates (Fisher). The Assay Buffer (AB) was 1×HBSS and 0.02 M HEPES.The HEK293F cells were transfected with the human norepinephrine transporter and frozen in 1 mL aliquots at about 1E+07 cells/mL. On the day of the experiment, the cells were removed from −80° C. or liquid nitrogen and thawed in a room temperature water bath. The cells were dilute to about 1-2E+06 with Freestyle medium. A 1 mL sample (1:2 dilution) was prepared, and the cells were counted. The cells were spun at 1100 rpm for 5 minutes, and the medium was aspirated off. The cells were resuspend in medium at 1.5E+06 cells/mL for about 60,000 cells per well. 40 μL of cells were dispensed per well in the Biocoat plates. The plates were spun at 1100 rpm for 1 minute to improve homogeneity of the cell layer and were incubated at 37° C. for a minimum of 3 hours.
- Binding Assay Human norepinephrine transporter (NET) enriched membranes (5 μg) were incubated with 5 nM of radiolabeled [3H]-Nisoxetin in assay buffer containing 50 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, pH 7.4.NSB (non specific binding) was measured by adding 10 μM desipramine. The binding of the test compound was measured in five different concentrations. After 60 min incubation at 4° C., binding reaction was terminated by filtering through Multiscreen GF/C (Millipore) presoaked in 0.5% polyethyleneimine in Vacuum Manifold Station, followed by 3 washes with ice-cold filtration buffer containing 50 mM Tris-HCl, 0.9% NaCl, pH 7.4.Filter plates were dried at 60° C. for 1 hour and 30 μl of scintillation cocktail were added to each well before radioactivity reading.
- Binding Assay Human norepinephrine transporter (NET) enriched membranes (5 μg) were incubated with 5 nM of radiolabeled [3H]-Nisoxetin in assay buffer containing 50 mM Tris-HCl, 120 mM NaCl, 5 mM KCl, pH 7.4.NSB (non specific binding) was measured by adding desipramine 10 μM. The binding of the test compound was measured at five different concentrations. After 60 min incubation at 4° C., binding reaction was terminated by filtering through Multiscreen GF/C (Millipore) presoaked in 0.5% polyethyleneimine in Vacuum Manifold Station, followed by 3 washes with ice-cold filtration buffer containing 50 mM Tris-HCl, 0.9% NaCl, pH 7.4.Filter plates were dried at 60° C. for 1 h and 30 μl of scintillation cocktail were added to each well before radioactivity reading.
- In Vitro Pharmacology Assay The monoamine transporters inhibitory activities of selected cycloalkylmethylamines of Formula (I) are reported herein. The compounds were evaluated using well established radioligand binding assays protocols (Galli, A. et al., J. Exp. Biol. 1995, 198, 2197-2212; Giros, B. et al., Trends Pharmcol. Sci. 1993, 14, 43-49; Gu, H. et al., J. Biol. Chem. 1994, 269(10), 7124-7130; Shearman, L. P. et al, Am. J. Physiol., 1998, 275(6 Pt 1), C1621-1629; Wolf, W. A. et al., J. Biol. Chem. 1992, 267(29), 20820-20825). The human recombinant transporter proteins dopamine (DAT), norepinephrine (NET) and serotonin (SERT) were selected for the in vitro assays. The radioligand binding assays were carried out at 11 different test concentrations 0.1 nM to 1 μM.
- Radioligand Binding Assay The monoamine transporters inhibitory activities of selected compounds cycloalkylmethylamine derivatives comprising Formula (I) are reported herein. The compounds were evaluated using well established radioligand binding assays protocols (Galli, A. et al., J. Exp. Biol. 1995, 198, 2197-2212; Giros, B. et al., Trends Pharmcol. Sci. 1993, 14, 43-49; Gu, H. et al., J. Biol. Chem. 1994, 269(10), 7124-7130; Shearman, L. P. et al, Am. J. Physiol., 1998, 275(6 Pt 1), C1621-1629; Wolf, W. A. et al., J. Biol. Chem. 1992, 267(29), 20820-20825). The human recombinant transporter proteins dopamine (DAT), norepinephrine (NET) and serotonin (SERT) were selected for the in vitro assays. The radioligand binding assays were carried out at 11 different test concentrations 0.1 nm to 1 μM.
- Norepinephrine Transporter Binding Assay Norepinephrine Transporter Binding Assay. Brains from male Sprague-Dawley rats weighing 200-225 g (Taconic Labs, Germantown, N.Y.) were removed, frontal cortex dissected and rapidly frozen. Membranes were prepared by homogenizing tissues in 20 volumes (w/v) of 50 mM Tris containing 120 mM NaCl and 5 mM KCl, (pH 7.4 at 25° C.), using a Brinkman Polytron and centrifuged at 50,000×g for 10 min at 4° C. The resulting pellet was resuspended in buffer, recentrifuged and resuspended in buffer to a concentration of 80 mg/mL. Ligand binding experiments were conducted in assay tubes containing 0.5 mL buffer for 60 min at 0-4° C. Each tube contained 0.5 nM [3H]Nisoxetine (PerkinElmer Life Sciences, Boston, Mass.) and 8 mg frontal cortex tissue (original wet weight). Nonspecific binding was determined using 1 mM desipramine. Incubations were terminated by rapid filtration through Whatman GF/B filters, presoaked in 0.05% polyethylenimine, using a Brandel R48 filtering manifold (Brandel Instruments Gaithersburg, Md.). The filters were washed twice with 3 mL cold buffer and transferred to scintillation vials. Beckman Ready Value (3.0 mL) was added and the vials were counted using a Beckman 6000 liquid scintillation counter (Beckman Coulter Instruments, Fullerton, Calif.). Each compound was tested with concentrations ranging from 0.01 nM to 100 mM for competition against binding of [3H]Nisoxetine, in at least three independent experiments, each performed in triplicate. Data were analyzed by using GraphPad Prism software (San Diego, Calif.) [11; Zou et. al. J. Med. Chem. 2006, 49, 6391-6399]. The results of the in vitro assays, grouped by functionality into the amides and amines are presented in Tables 1 and 2, respectively. All compounds were tested as racemic mixtures.
- Radioligand Binding Assay (Ki) and Inhibition of Substrate Uptake (EC50/IC50) Binding affinity of each compound was measured by assessing the potency of inhibition of binding of radiolabeled RTI-55. Membranes were preincubated with compound before the addition of [125I]RTI-55. The reaction was terminated by filtration through Whatman GF/C filters using a 96-well Tomtech cell harvester (Tomtech, Orange, CT). Scintillation fluid was added to each filter spot and radioactivity remaining on the filter was determined using a Wallace beta-plate reader. IC50 values were converted to Ki values using the Cheng-Prusoff equation. Specific binding was defined as the difference in binding observed in the presence and absence of 5 uM mazindol (HEK-hDAT and -NET) or 5 uM imipramine (HEK-hSERT). EC50/IC50 values were obtained from inhibition of the reuptake of [3H] dopamine for DAT, [3H] serotonin for SERT, or [3H] norepinephrine for NET.
- Norepinephrine Transporter Binding Assay Brains from male Sprague-Dawley rats weighing 200-225 g (Taconic Labs, Germantown, N.Y.) were removed, frontal cortex dissected and rapidly frozen. Membranes were prepared by homogenizing tissues in 20 volumes (w/v) of 50 mM Tris containing 120 mM NaCl and 5 mM KCl, (pH 7.4 at 25° C.), using a Brinkman Polytron and centrifuged at 50,000xg for 10 min at 4° C. The resulting pellet was resuspended in buffer, recentrifuged and resuspended in buffer to a concentration of 80 mg/mL. Ligand binding experiments were conducted in assay tubes containing 0.5 mL buffer for 60 min at 0-4° C. Each tube contained 0.5 nM [3H]Nisoxetine (PerkinElmer Life Sciences, Boston, Mass.) and 8 mg frontal cortex tissue (original wet weight). Nonspecific binding was determined using 1 mM desipramine. Incubations were terminated by rapid filtration through Whatman GF/B filters, presoaked in 0.05% polyethylenimine, using a Brandel R48 filtering manifold (Brandel Instruments Gaithersburg, Md.). The filters were washed twice with 3 mL cold buffer and transferred to scintillation vials. Beckman Ready Value (3.0 mL) was added and the vials were counted using a Beckman 6000 liquid scintillation counter (Beckman Coulter Instruments, Fullerton, Calif.).
- Binding Assay Norepinephrine Transporter Binding Assay. Brains from male Sprague-Dawley rats weighing 200-225 g (Taconic Labs, Germantown, N.Y.) were removed, frontal cortex dissected and rapidly frozen. Membranes were prepared by homogenizing tissues in 20 volumes (w/v) of 50 mM Tris containing 120 mM NaCl and 5 mM KCl, (pH 7.4 at 25° C.), using a Brinkman Polytron and centrifuged at 50,000×g for 10 min at 4° C. The resulting pellet was resuspended in buffer, recentrifuged and resuspended in buffer to a concentration of 80 mg/mL. Ligand binding experiments were conducted in assay tubes containing 0.5 mL buffer for 60 min at 0-4° C. Each tube contained 0.5 nM [3H]Nisoxetine (PerkinElmer Life Sciences, Boston, Mass.) and 8 mg frontal cortex tissue (original wet weight). Nonspecific binding was determined using 1 mM desipramine. Incubations were terminated by rapid filtration through Whatman GF/B filters, presoaked in 0.05% polyethylenimine, using a Brandel R48 filtering manifold (Brandel Instruments Gaithersburg, Md.). The filters were washed twice with 3 mL cold buffer and transferred to scintillation vials. Beckman Ready Value (3.0 mL) was added and the vials were counted using a Beckman 6000 liquid scintillation counter (Beckman Coulter Instruments, Fullerton, Calif.). Each compound was tested with concentrations ranging from 0.01 nM to 100 mM for competition against binding of [3H]Nisoxetine, in at least three independent experiments, each performed in triplicate.
- Norepinephrine Transporter Binding Assay 1. Each tube receives the following components: 25 ul drug or vehicle 25 ul [3H]-Nisoxetine 200 ul tissue suspension. 2. Initiate binding reaction with the addition of tissue, and incubate at room temperature for 1 hour. 3. Terminate binding reaction by rapid filtration of tube contents onto 0.1% PEI treated GF/C filters (TopCount). 4. Rinse the assay tubes once with ice cold 50 mM NaCl, then rapidly rinse the filters with 6×1 ml/tube of the same wash buffer. 5. Radioactivity trapped onto the filters is assessed using liquid scintillation spectrophotometer after soaking the filters for at least 1 hour in scintillation cocktail. Materials and Reagents 1. The receptor source is human recombinant/CHO. 2. [3H]-Nisoxetine, diluted to a concentration of 10 nM in assay buffer, is used as the radioligand. Thus, the final ligand concentration is 1 nM. 3. Non specific binding is defined as that remaining in the presence of 1×10−6M desipramine (MW=302.8) (Make fresh: in bag with dessicating rocks 1, dissolves in water 1E-3). 4. The reference compound for the assay is desipramine. Desimpramine is run at following final concentrations: 1×10−10, 2×10−10, 5×10−10, 1×10−9, 2×10−9, 5×10−9, 1×10−8, 2×10−8, 5×10−8, 1×10−7, 2×10−7, 5×10−7M 5. The positive control is any of the above run at the final concentrations of: 1×10−9, 5×10−9, 2×10−8 M. 6. The Kd for the receptor is 3 nM. Buffers MW (g/mole) g/1 L Incubation Buffer: 50 mM Tris, pH 7.4 121 6.06 5 mM KCl 74.6 0.38 120 mM NaCl 58.4 7.02 Wash Buffer: 50 mM NaCl 58.4 3.0