cevimeline [Ligand Id: 9658] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL168815 (Cevimeline)
  • 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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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 muscarinic M1 receptor transfected in CHO cells after 120 mins by scintillation counting analysis B 5.31 pKi 4897.79 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 3255-3259 [PMID:24980056]
GtoPdb Displacement of [3H]QNB from cloned receptor. - 5.31 pKi 4850 nM Ki J Pharmacol Exp Ther (1997) 283: 1059-68 [PMID:9399977]
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 receptor transfected in CHO cells after 120 mins by scintillation counting analysis B 6.07 pKi 851.14 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 3255-3259 [PMID:24980056]
GtoPdb Displacement of [3H]QNB from cloned receptor. - 6.07 pKi 854 nM Ki J Pharmacol Exp Ther (1997) 283: 1059-68 [PMID:9399977]
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 muscarinic M3 receptor transfected in CHO cells after 120 mins by scintillation counting analysis B 5.59 pKi 2570.4 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 3255-3259 [PMID:24980056]
GtoPdb Displacement of [3H]QNB from cloned receptor. - 5.59 pKi 2575 nM Ki J Pharmacol Exp Ther (1997) 283: 1059-68 [PMID:9399977]
M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173]
GtoPdb Displacement of [3H]QNB from cloned receptor. - 5.99 pKi 1012 nM Ki J Pharmacol Exp Ther (1997) 283: 1059-68 [PMID:9399977]
ChEMBL Displacement of [3H]NMS from human muscarinic M4 receptor transfected in CHO cells after 120 mins by scintillation counting analysis B 5.99 pKi 1023.29 nM Ki Bioorg. Med. Chem. Lett. (2014) 24: 3255-3259 [PMID:24980056]

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]