atropine [Ligand Id: 320] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL517712 (Atroject, Atropen, Atrophate, Atropine, Atropine (autoinjector), Atropinum, Dl-hyoscyamine, Isopto Atropine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3198] [GtoPdb: 2465] [UniProtKB: P21836] | ||||||||
| ChEMBL | Compound was evaluated for the binding affinity by displacing [3H]methylscopolamine [3H]NMS from mouse cerebral cortex tissue. | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (1992) 35: 1102-1108 [PMID:1552502] |
| ChEMBL | Compound was evaluated for the binding affinity by displacing [3H]oxotremorine from mouse cerebral cortex tissue. | B | 9.46 | pKi | 0.35 | nM | Ki | J Med Chem (1992) 35: 1102-1108 [PMID:1552502] |
| α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] | ||||||||
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 6.18 | pKi | 666 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin) | B | 5.87 | pIC50 | 1354 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Binding affinity towards muscarinic m1 receptor | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (1994) 37: 2285-2291 [PMID:8057277] |
| ChEMBL | Competitive inhibition of EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells after 4 hrs by FRET assay in presence of para-LRB-AC42 | B | 8.92 | pKi | 1.2 | nM | Ki | J Med Chem (2012) 55: 2125-2143 [PMID:22329602] |
| ChEMBL | Displacement of [3H] N-methylscopolamine from human muscarinic M1 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis | B | 9.04 | pKi | 0.92 | nM | Ki | Bioorg Med Chem (2013) 21: 2651-2662 [PMID:23523385] |
| ChEMBL | Displacement of [3H]NMS from EGFP-fused human M1 receptor N-terminal truncated at 17 residues expressed in HEK293 cells after 22 hrs by liquid scintillation counting | B | 9.24 | pKi | 0.58 | nM | Ki | J Med Chem (2012) 55: 2125-2143 [PMID:22329602] |
| ChEMBL | Displacement of [3H]NMS from human M1 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method | B | 9.36 | pKi | 0.44 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 471-476 [PMID:30554957] |
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.44 | pKi | 0.37 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Inhibition of [3H]QNB binding to CHO cells bearing transfected muscarinic acetylcholine receptor M3 | B | 9.48 | pKi | 0.33 | nM | Ki | J Med Chem (1991) 34: 1436-1440 [PMID:2016720] |
| ChEMBL | Displacement of [3H]pirenzepine from muscarinic M1 receptor | B | 9.52 | pKi | 0.3 | nM | Ki | J Nat Prod (1993) 56: 441-455 [PMID:8496700] |
| GtoPdb | - | - | 9.6 | pKi | - | - | - |
EMBO J (1987) 6: 3923-9 [PMID:3443095]; Mol Pharmacol (1998) 53: 1120-30 [PMID:9614217]; AAPS PharmSci (2001) 3: E30 [PMID:12049493]; Mol Pharmacol (2006) 69: 1641-51 [PMID:16439611]; J Pharmacol Exp Ther (2001) 297: 790-7 [PMID:11303071]; J Recept Signal Transduct Res (1997) 17: 177-84 [PMID:9029489] |
| ChEMBL | Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M1 | B | 9.6 | pKi | 0.25 | nM | Ki | J Med Chem (2002) 45: 984-987 [PMID:11831911] |
| ChEMBL | DRUGMATRIX: Muscarinic M1 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.82 | pIC50 | 1.52 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Muscarinic acetylcholine receptor M1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2672] [UniProtKB: Q8WMX0] | ||||||||
| ChEMBL | Inhibition of [3H]NMS binding to cerebral cortex membranes which contain predominantly the Muscarinic acetylcholine receptor M1 subtypes | B | 8.62 | pKi | 2.4 | nM | Ki | J Med Chem (1989) 32: 1522-1528 [PMID:2738887] |
| ChEMBL | Binding affinity against Muscarinic acetylcholine receptor M1 by displacement of [3H]pirenzepine in bovine striatum | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (1988) 31: 1463-1466 [PMID:3385735] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | In vitro receptor binding against Muscarinic acetylcholine receptor M1 in rat cerebral cortex was determined using [3H]pirenzepine | B | 8.89 | pKd | 1.3 | nM | Kd | J Med Chem (1990) 33: 2108-2113 [PMID:2374141] |
| ChEMBL | Displacement of [3H]NMS from rat muscarinic M1 receptor expressed in CHO cells after 3 hrs | B | 8.85 | pKi | 1.4 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
| ChEMBL | Displacement of [3H]NMS from rat muscarinic M1 receptor expressed in CHO cells after 3 hrs | B | 8.86 | pKi | 1.38 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 223-227 [PMID:23200253] |
| ChEMBL | Displacement of [3H]NMS from rat recombinant muscarinic M1 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting | B | 9.1 | pKi | 0.79 | nM | Ki | Nat Chem Biol (2008) 4: 42-50 [PMID:18059262] |
| ChEMBL | Evaluated for the phosphatidyl inositol turnover at Muscarinic acetylcholine receptor M1 in rat cortex | F | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (1988) 31: 1463-1466 [PMID:3385735] |
| ChEMBL | Ability to displace [3H]pirenzepine (PZ) from M1 receptor in rat cortex homogenate | B | 9.59 | pKi | 0.26 | nM | Ki | J Med Chem (1993) 36: 848-854 [PMID:8464039] |
| ChEMBL | Displacement of [3H]pirenzepine from muscarinic acetylcholine receptor M1 in rat cortex homogenates | B | 9.59 | pKi | 0.26 | nM | Ki | J Med Chem (1991) 34: 2984-2989 [PMID:1920350] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229]; Life Sci (1992) 51: 955-71 [PMID:1325587]; Mol Pharmacol (1989) 35: 469-76 [PMID:2704370] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Antimuscarinic activity on the acetylcholine-induced inhibition of contraction of guinea pig ileum which has M2 muscarinic receptor subtype. | F | 8.7 | pKd | 2 | nM | Kd | J Med Chem (1989) 32: 1522-1528 [PMID:2738887] |
| ChEMBL | Antagonist potency against muscarinic receptors was assed by antagonism of carbachol induced inhibition of electrically stimulated guinea pig atria | F | 8.87 | pKd | 1.35 | nM | Kd | J Med Chem (1989) 32: 79-84 [PMID:2909747] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(4-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)piperazin-1-yl)ethyl)amino)hexyl)indolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Tris(hydrotrifluoroacetate fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 7.73 | pKi | 18.62 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of [3H]UR-AP060 from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cell homogenate after 3 hrs by liquid scintillation counting assay | B | 7.77 | pKi | 16.98 | nM | Ki | J Med Chem (2017) 60: 3314-3334 [PMID:28388054] |
| ChEMBL | Displacement of [3H]NMS from human muscarinic acetylcholine receptor M2 expressed in CHOK1 cells | B | 7.8 | pKi | 15.85 | nM | Ki | J Med Chem (2017) 60: 3314-3334 [PMID:28388054] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-1-(6-((3,5-Bis((2-(3-(1-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)-1H-imidazol-4-yl)propanamido)ethyl)carbamoyl)benzyl)amino)-6-oxohexyl)-3,3-dimethyl-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Tris(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 8.15 | pKi | 7.08 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(4-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)piperazin-1-yl)ethyl)amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Bis(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 8.31 | pKi | 4.9 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(3-(1-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)-1H-imidazol-4-yl)propanamido)ethyl)-amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonateHydrotrifluoroacetate fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 8.5 | pKi | 3.16 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of 4-(2-((1E,3E)-5-((E)-3,3-Dimethyl-1-(6-oxo-6-((2-(4-(4-(1-(2-oxo-2-(11-oxo-10,11-dihydro-5H-dibenzo[b,e][1,4]diazepin-5-yl)ethyl)piperidin-4-yl)butyl)piperazin-1-yl)ethyl)amino)hexyl)-5-sulfoindolin-2-ylidene)penta-1,3-dien-1-yl)-3,3-dimethyl-3H-indol-1-ium-1-yl)butane-1-sulfonate Bis(hydrotrifluoroacetate) fluorescent tracer from human muscarinic M2 receptor expressed in CHO-K9 cells by FACSCalibur flow cytometry | B | 8.6 | pKi | 2.51 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of [3H]-AFDX-384 from human muscarinic M2 receptor expressed in CHO-K1 cells | B | 8.72 | pKi | 1.9 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| ChEMBL | Binding affinity (Ki) against binding of [3H]NMS to membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M2 | B | 8.82 | pKi | 1.5 | nM | Ki | J Med Chem (2002) 45: 984-987 [PMID:11831911] |
| ChEMBL | Displacement of [3H] N-methylscopolamine from human muscarinic M2 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis | B | 8.84 | pKi | 1.44 | nM | Ki | Bioorg Med Chem (2013) 21: 2651-2662 [PMID:23523385] |
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.88 | pKi | 1.33 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Binding affinity towards muscarinic m2 receptor | B | 9 | pKi | 1 | nM | Ki | J Med Chem (1994) 37: 2285-2291 [PMID:8057277] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 receptor expressed in CHO-K9 cells measured after 60 mins by Hoechst H33342 dye based confocal plate reader assay | B | 9.04 | pKi | 0.91 | nM | Ki | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | Displacement of [3H]NMS from human M2 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 471-476 [PMID:30554957] |
| ChEMBL | Displacement of [3H]UNSW-MK259 from human muscarinic acetylcholine receptor M2 expressed in CHOK9 cells after 3 hrs by liquid scintillation counting assay | B | 9.09 | pKi | 0.81 | nM | Ki | J Med Chem (2017) 60: 3314-3334 [PMID:28388054] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - |
EMBO J (1987) 6: 3923-9 [PMID:3443095]; AAPS PharmSci (2001) 3: E30 [PMID:12049493]; J Pharmacol Exp Ther (2001) 297: 790-7 [PMID:11303071]; Eur J Pharmacol (2016) 782: 70-6 [PMID:27085897] |
| ChEMBL | muscarinic acetylcholine receptor M1 | B | 9.46 | pKi | 0.34 | nM | Ki | J Med Chem (1991) 34: 1436-1440 [PMID:2016720] |
| ChEMBL | Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation pre-incubated for 30 mins followed by carbachol addition and measured after 1 hr by HTRF assay | F | 8.09 | pIC50 | 8.13 | nM | IC50 | J Med Chem (2019) 62: 5358-5369 [PMID:31074983] |
| ChEMBL | Antagonist activity at human muscarinic M2 receptor expressed in HEK293 cells co-expressing HA-Galphaq/i5 assessed as inhibition of carbachol-induced IP1 accumulation at 37 degree C pre-incubated for 30 mins followed by carbachol addition and measured after 60 mins by HTRF assay | F | 8.09 | pIC50 | 8.13 | nM | IC50 | J Med Chem (2020) 63: 4133-4154 [PMID:32233403] |
| ChEMBL | DRUGMATRIX: Muscarinic M2 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.43 | pIC50 | 3.73 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3197] [GtoPdb: 14] [UniProtKB: Q9ERZ4] | ||||||||
| ChEMBL | Ability to displace [3H]methylscopolamine ([3H]NMS) from mouse cerebral cortex | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (1992) 35: 3141-3147 [PMID:1507203] |
| ChEMBL | Ability to displace [3H]oxotremorine ([3H]-OXO-M) from mouse cerebral cortex | B | 9.46 | pKi | 0.35 | nM | Ki | J Med Chem (1992) 35: 3141-3147 [PMID:1507203] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL309] [GtoPdb: 14] [UniProtKB: P10980] | ||||||||
| ChEMBL | In vitro receptor binding against Muscarinic acetylcholine receptor M2 in rat heart was determined using [3H]pirenzepine | B | 8.57 | pKd | 2.7 | nM | Kd | J Med Chem (1990) 33: 2108-2113 [PMID:2374141] |
| ChEMBL | Evaluated for the inhibition of adenylate cyclase at M2 receptor in rat heart | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (1988) 31: 1463-1466 [PMID:3385735] |
| ChEMBL | Inhibition of carbachol-induced release of alpha-amylase from pancreatic acinar cells from that of rat ileum contained the M2 receptor subtypes | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (1989) 32: 1522-1528 [PMID:2738887] |
| ChEMBL | Displacement of [3H]NMS from rat recombinant muscarinic M2 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting | B | 8.84 | pKi | 1.45 | nM | Ki | Nat Chem Biol (2008) 4: 42-50 [PMID:18059262] |
| GtoPdb | - | - | 9.1 | pKi | - | - | - |
Life Sci (1992) 51: 955-71 [PMID:1325587]; J Pharmacol Exp Ther (1998) 284: 500-7 [PMID:9454790] |
| ChEMBL | Ability to displace [3H](-)-quinuclidinyl benzilate(QNB) from M2 receptor in rat heart homogenate | B | 9.12 | pKi | 0.76 | nM | Ki | J Med Chem (1993) 36: 848-854 [PMID:8464039] |
| ChEMBL | Displacement of [3H](-)-quinuclidinyl benzilate(QNB) from muscarinic (M2) receptor in rat heart homogenates | B | 9.12 | pKi | 0.76 | nM | Ki | J Med Chem (1991) 34: 2984-2989 [PMID:1920350] |
| ChEMBL | Binding affinity against Muscarinic acetylcholine receptor M2 by displacement of [3H]QNB in rat myocardium | B | 9.15 | pKi | 0.7 | nM | Ki | J Med Chem (1988) 31: 1463-1466 [PMID:3385735] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis | B | 8.66 | pKi | 2.18 | nM | Ki | Bioorg Med Chem (2013) 21: 2651-2662 [PMID:23523385] |
| ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M3 receptor expressed in BHK-21 cells | B | 9.05 | pKi | 0.9 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| ChEMBL | Displacement of [3H]NMS from human M3 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method | B | 9.28 | pKi | 0.53 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 471-476 [PMID:30554957] |
| ChEMBL | Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M3 | B | 9.3 | pKi | 0.5 | nM | Ki | J Med Chem (2002) 45: 984-987 [PMID:11831911] |
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.36 | pKi | 0.44 | nM | Ki | DrugMatrix in vitro pharmacology data |
| GtoPdb | - | - | 9.8 | pKi | - | - | - |
EMBO J (1987) 6: 3923-9 [PMID:3443095]; AAPS PharmSci (2001) 3: E30 [PMID:12049493]; J Pharmacol Exp Ther (2001) 297: 790-7 [PMID:11303071]; Eur J Pharmacol (2016) 782: 70-6 [PMID:27085897] |
| ChEMBL | DRUGMATRIX: Muscarinic M3 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 8.68 | pIC50 | 2.07 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL320] [GtoPdb: 15] [UniProtKB: P08483] | ||||||||
| ChEMBL | In vitro receptor binding against Muscarinic acetylcholine receptor M3 in rat submandibular gland was determined using [3H]pirenzepine | B | 9.2 | pKd | 0.63 | nM | Kd | J Med Chem (1990) 33: 2108-2113 [PMID:2374141] |
| ChEMBL | Displacement of [3H]NMS from rat recombinant muscarinic M3 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting | B | 9.1 | pKi | 0.8 | nM | Ki | Nat Chem Biol (2008) 4: 42-50 [PMID:18059262] |
| GtoPdb | - | - | 9.3 | pKi | - | - | - |
J Pharmacol Exp Ther (2002) 303: 29-35 [PMID:12235229]; Life Sci (1992) 51: 955-71 [PMID:1325587] |
| ChEMBL | Ability to displace [3H]N-methylscopolamine (NMS) from M3 receptor in rat submaxillary gland homogenate | B | 9.92 | pKi | 0.12 | nM | Ki | J Med Chem (1993) 36: 848-854 [PMID:8464039] |
| Muscarinic acetylcholine receptor M3 in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5498] [UniProtKB: Q8VH26] | ||||||||
| ChEMBL | Antagonist potency against carbachol induced contractions of isolated guinea pig ileum Muscarinic acetylcholine receptor | F | 8.83 | pKd | 1.48 | nM | Kd | J Med Chem (1989) 32: 79-84 [PMID:2909747] |
| ChEMBL | Antagonist potency at muscarinic M3 receptor in guinea-pig ileum assessed as inhibition of carbachol-induced contractions after 15 mins | F | 8.99 | pKd | 1.02 | nM | Kd | Bioorg Med Chem (2018) 26: 2573-2585 [PMID:29681486] |
| ChEMBL | Antagonist activity at muscarinic M3 receptor in guinea-pig ileum assessed as inhibition of carbachol-induced contractions after 15 mins | B | 8.99 | pKd | 1.02 | nM | Kd | Bioorg Med Chem (2019) 27: 1254-1262 [PMID:30792106] |
| ChEMBL | Antagonism to the H1 receptor of guinea pig ileum was determined | F | 9.11 | pKd | 0.78 | nM | Kd | Bioorg Med Chem Lett (1995) 5: 667-672 |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M4 receptor expressed in BHK-21 cells | B | 8.52 | pKi | 3 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| ChEMBL | Displacement of [3H]-NMS from recombinant human M4 receptor expressed in CHO cell membranes | B | 8.8 | pKi | 1.6 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 2479-2483 [PMID:28427812] |
| ChEMBL | Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis | B | 8.86 | pKi | 1.39 | nM | Ki | Bioorg Med Chem (2013) 21: 2651-2662 [PMID:23523385] |
| ChEMBL | Displacement of [3H]NMS from human recombinant muscarinic M4 receptor expressed in CHO cell membranes | B | 9.19 | pKi | 0.64 | nM | Ki | Bioorg Med Chem Lett (2017) 27: 3576-3581 [PMID:28633897] |
| ChEMBL | Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M4 | B | 9.47 | pKi | 0.34 | nM | Ki | J Med Chem (2002) 45: 984-987 [PMID:11831911] |
| GtoPdb | - | - | 9.5 | pKi | - | - | - |
EMBO J (1987) 6: 3923-9 [PMID:3443095]; AAPS PharmSci (2001) 3: E30 [PMID:12049493]; J Pharmacol Exp Ther (2001) 297: 790-7 [PMID:11303071]; Eur J Pharmacol (2016) 782: 70-6 [PMID:27085897] |
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.98 | pKi | 0.1 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Muscarinic M4 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.13 | pIC50 | 0.74 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL317] [GtoPdb: 16] [UniProtKB: P08485] | ||||||||
| ChEMBL | Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting | B | 9.28 | pKi | 0.52 | nM | Ki | Nat Chem Biol (2008) 4: 42-50 [PMID:18059262] |
| ChEMBL | Displacement of [3H]NMS from rat recombinant muscarinic M4 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting | B | 9.28 | pKi | 0.52 | nM | Ki | Nat Chem Biol (2008) 4: 42-50 [PMID:18059262] |
| GtoPdb | - | - | 9.7 | pKi | - | - | - | Life Sci (1992) 51: 955-71 [PMID:1325587] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| ChEMBL | Displacement of [3H]NMS from human muscarinic acetylcholine receptor subtype 5 expressed in CHO cell membranes by scintillation counting method | B | 8.83 | pKi | 1.47 | nM | Ki | J Med Chem (2014) 57: 7804-7810 [PMID:25147929] |
| ChEMBL | Displacement of [3H]-4-DAMP from human muscarinic M5 receptor expressed in BHK-21 cells | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2010) 53: 6386-6397 [PMID:20684563] |
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.18 | pKi | 0.66 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | Displacement of [3H]NMS from human M5 AChR expressed in CHO cell membranes after 1 to 2 hrs by liquid scintillation spectrometry method | B | 9.22 | pKi | 0.6 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 471-476 [PMID:30554957] |
| ChEMBL | Binding affinity (Ki) against binding of [3H]NMS using membranes from CHO cells expressing cloned human Muscarinic acetylcholine receptor M5 | B | 9.27 | pKi | 0.54 | nM | Ki | J Med Chem (2002) 45: 984-987 [PMID:11831911] |
| GtoPdb | - | - | 9.3 | pKi | - | - | - |
J Pharmacol Exp Ther (2001) 297: 790-7 [PMID:11303071]; Eur J Pharmacol (2016) 782: 70-6 [PMID:27085897]; Life Sci (1999) 64: 2351-8 [PMID:10374898] |
| ChEMBL | Displacement of [3H]QNB from muscarinic acetylcholine M5 receptor after 1.5 hrs by scintillation counting | B | 9.4 | pKi | 0.4 | nM | Ki | Bioorg Med Chem (2011) 19: 5756-5762 [PMID:21907583] |
| ChEMBL | Activation of human muscarinic M5 receptor expressed in CHO cells coexpressing Gq protein assessed as increase in acetylcholine potency at 30 uM by calcium mobilization-based ACh concentration-response curve assay relative to control | F | 9.68 | pKi | 0.21 | nM | Ki | J Med Chem (2009) 52: 3445-3448 [PMID:19438238] |
| ChEMBL | DRUGMATRIX: Muscarinic M5 radioligand binding (ligand: [3H] N-Methylscopolamine) | B | 9.04 | pIC50 | 0.92 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL277] [GtoPdb: 17] [UniProtKB: P08911] | ||||||||
| ChEMBL | Displacement of [3H]NMS from rat recombinant muscarinic M5 receptor expressed in CHO cells after 2 hrs by microplate scintillation counting | B | 9.07 | pKi | 0.86 | nM | Ki | Nat Chem Biol (2008) 4: 42-50 [PMID:18059262] |
| GtoPdb | - | - | 9.4 | pKi | - | - | - | Life Sci (1992) 51: 955-71 [PMID:1325587] |
| Nicotinic acetylcholine receptor alpha 5 subunit in Musca domestica (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2366408] [UniProtKB: A9XFY4] | ||||||||
| ChEMBL | Displacement of [3H]alpha-bungarotoxin from nAChR in Musca domestica (house fly) head membrane after 60 min by scintillation counting | B | 4.49 | pKi | 32500 | nM | Ki | J Pestic Sci (1992) 17: 231-236 |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity towards 5-hydroxytryptamine 1A receptor by the displacement of [125I]trans-8-OH-PIPAT in membrane homogenates of hippocampal tissue of rat brain | B | 4.7 | pKi | >20000 | nM | Ki | J Med Chem (1993) 36: 3161-3165 [PMID:8230102] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 6.28 | pKi | 530 | nM | Ki | DrugMatrix in vitro pharmacology data |
| ChEMBL | DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine) | B | 5.99 | pIC50 | 1012 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Organic cation transporter 1/Solute carrier family 22 member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5685] [GtoPdb: 1019] [UniProtKB: O15245] | ||||||||
| ChEMBL | Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy | B | 4.91 | pIC50 | 12200 | nM | IC50 | J Med Chem (2008) 51: 5932-5942 [PMID:18788725] |
| α2A-adrenoceptor in Human [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | - | - | 4.85 | pKi | 14000 | nM | Ki | Invest Ophthalmol Vis Sci (2018) 59: 2778-2791 [PMID:29860464] |
| Glycine Receptor (All subtypes) in Human [GtoPdb: 428] | ||||||||
| GtoPdb | - | - | 3.6 | pIC50 | - | - | - |
J Neurochem (1999) 73: 802-6 [PMID:10428078]; J Neurochem (2007) 100: 758-69 [PMID:17181559] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
