scopolamine [Ligand Id: 330] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL569713 (Isoptpo Hyoscine, Scopolamine, Transderm scop) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Displacement of [3H]NMS from human M1 muscarinic receptor expressed in CHO-K1 cells | B | 8.12 | pKi | 7.5 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| GtoPdb | - | - | 9 | pKi | - | - | - |
AAPS PharmSci (2001) 3: E30 [PMID:12049493]; Eur J Pharmacol (2016) 782: 70-6 [PMID:27085897] |
| ChEMBL | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay | B | 8.36 | pIC50 | 4.37 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based beta-arrestin engagement assay | B | 8.48 | pIC50 | 3.31 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Antagonist activity at human M1 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay | B | 8.76 | pIC50 | 1.74 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| Muscarinic acetylcholine receptor M1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2672] [UniProtKB: Q8WMX0] | ||||||||
| ChEMBL | Binding affinity towards Muscarinic acetylcholine receptor M1 was determined in calf brain membrane | B | 9.39 | pKi | 0.41 | nM | Ki | J Med Chem (1997) 40: 117-124 [PMID:9016336] |
| 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 | 9.12 | pKd | 0.75 | nM | Kd | J Med Chem (1990) 33: 2108-2113 [PMID:2374141] |
| ChEMBL | Binding affinity towards rat Muscarinic acetylcholine receptor M1 was determined | B | 9.28 | pKi | 0.53 | nM | Ki | J Med Chem (1997) 40: 117-124 [PMID:9016336] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 Y104A mutant expressed in Flp-In-CHO cells by liquid scintillation counting | B | 7.54 | pKi | 28.84 | nM | Ki | J Med Chem (2014) 57: 6739-6750 [PMID:25051097] |
| ChEMBL | Displacement of [3H]NMS from human M2 muscarinic receptor expressed in CHO-K1 cells | B | 8.02 | pKi | 9.5 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 Y177Q/T423H mutant expressed in Flp-In-CHO cells by liquid scintillation counting | B | 8.45 | pKi | 3.55 | nM | Ki | J Med Chem (2014) 57: 6739-6750 [PMID:25051097] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 Y177Q mutant expressed in Flp-In-CHO cells by liquid scintillation counting | B | 8.48 | pKi | 3.31 | nM | Ki | J Med Chem (2014) 57: 6739-6750 [PMID:25051097] |
| ChEMBL | Displacement of [3H]-NMS from human muscarinic M2 W422A mutant expressed in Flp-In-CHO cells by liquid scintillation counting | B | 8.48 | pKi | 3.31 | nM | Ki | J Med Chem (2014) 57: 6739-6750 [PMID:25051097] |
| ChEMBL | Displacement of [3H]-NMS from wild-type human muscarinic M2 receptor expressed in Flp-In-CHO cells by liquid scintillation counting | B | 8.52 | pKi | 3.02 | nM | Ki | J Med Chem (2014) 57: 6739-6750 [PMID:25051097] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - |
AAPS PharmSci (2001) 3: E30 [PMID:12049493]; J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
| 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 | 8.52 | pKd | 3 | nM | Kd | J Med Chem (1990) 33: 2108-2113 [PMID:2374141] |
| ChEMBL | Binding affinity towards rat Muscarinic acetylcholine receptor M2 was determined | B | 8.34 | pKi | 4.57 | nM | Ki | J Med Chem (1997) 40: 117-124 [PMID:9016336] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| ChEMBL | Displacement of [3H]NMS from human M3 muscarinic receptor expressed in CHO-K1 cells | B | 8.19 | pKi | 6.5 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| GtoPdb | - | - | 9.4 | pKi | - | - | - |
AAPS PharmSci (2001) 3: E30 [PMID:12049493]; J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
| 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 | 9.19 | pKd | 0.65 | nM | Kd | J Med Chem (1990) 33: 2108-2113 [PMID:2374141] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| ChEMBL | Displacement of [3H]NMS from human M4 muscarinic receptor expressed in CHO-K1 cells | B | 7.43 | pKi | 36.9 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| GtoPdb | - | - | 9.5 | pKi | - | - | - |
AAPS PharmSci (2001) 3: E30 [PMID:12049493]; J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
| ChEMBL | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein engagement assay | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by BRET based Gq protein activation assay | B | 8.42 | pIC50 | 3.8 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| ChEMBL | Antagonist activity at human M4 receptor expressed in HEK293T cells assessed as inhibition of carbachol-induced response by beta-arrestin engagement assay | B | 8.89 | pIC50 | 1.29 | nM | IC50 | J Med Chem (2014) 57: 9065-9077 [PMID:25275964] |
| 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 M5 muscarinic receptor expressed in CHO-K1 cells | B | 7.75 | pKi | 17.6 | nM | Ki | J Med Chem (2013) 56: 1693-1703 [PMID:23379472] |
| GtoPdb | - | - | 8.7 | pKi | - | - | - | J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
| ChEMBL | Displacement of [3H]-NMS from wild-type human muscarinic M5 receptor expressed in CHO-K1 cells by liquid scintillation counting | B | 8.89 | pKi | 1.29 | nM | Ki | J Med Chem (2014) 57: 6739-6750 [PMID:25051097] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
