biperiden [Ligand Id: 7128] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1101 (Biperiden, Akineton, KL 373)
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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  • M3 receptor/Muscarinic acetylcholine receptor M3 in Human [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309]
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  • M4 receptor/Muscarinic acetylcholine receptor M4 in Human [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
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  • M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912]
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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]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]