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ChEMBL ligand: CHEMBL1101 (Akineton, Akineton-, Biperiden, Biperidene, Biperideno, 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 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]