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ChEMBL ligand: CHEMBL1101 (Akineton, Akineton-, Biperiden, Biperidenum, KL 373, NSC-759145) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
GtoPdb | - | - | 9.32 | pKd | 0.48 | nM | Kd | J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
ChEMBL | Displacement of [3H] N-methylscopolamine from human muscarinic M1 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis | B | 8.63 | pKi | 2.36 | nM | Ki | Bioorg Med Chem (2013) 21: 2651-2662 [PMID:23523385] |
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
GtoPdb | - | - | 8.2 | pKd | 6.3 | nM | Kd | J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
ChEMBL | Displacement of [3H] N-methylscopolamine from human muscarinic M2 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis | B | 7.86 | pKi | 13.7 | nM | Ki | Bioorg Med Chem (2013) 21: 2651-2662 [PMID:23523385] |
M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
GtoPdb | - | - | 8.41 | pKd | 3.9 | nM | Kd | J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
ChEMBL | Displacement of [3H] N-methylscopolamine from human muscarinic M3 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis | B | 8.23 | pKi | 5.95 | nM | Ki | Bioorg Med Chem (2013) 21: 2651-2662 [PMID:23523385] |
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
GtoPdb | - | - | 8.62 | pKd | 2.4 | nM | Kd | J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
ChEMBL | Displacement of [3H] N-methylscopolamine from human muscarinic M4 receptor expressed in CHOK1 cells after 30 mins by scintillation counting analysis | B | 7.49 | pKi | 32.1 | nM | Ki | Bioorg Med Chem (2013) 21: 2651-2662 [PMID:23523385] |
M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
GtoPdb | - | - | 8.2 | pKd | 6.3 | nM | Kd | J Pharmacol Exp Ther (1992) 260: 576-80 [PMID:1346637] |
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]