VU0255035 [Ligand Id: 3274] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1628667 |
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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 | - | - | 7.8 | pKi | 14.87 | nM | Ki | Mol Pharmacol (2009) 76: 356-68 [PMID:19407080] |
| ChEMBL | Antagonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence assay | F | 6.16 | pIC50 | 690 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1044-1048 [PMID:22197142] |
| ChEMBL | Antagonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence analysis | F | 6.16 | pIC50 | 690 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 5035-5040 [PMID:22749871] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL276] [GtoPdb: 13] [UniProtKB: P08482] | ||||||||
| ChEMBL | Antagonist activity at rat muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by fluorescence assay | F | 6.62 | pIC50 | 240 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 1044-1048 [PMID:22197142] |
| M2 receptor in Human [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| GtoPdb | - | - | 6.2 | pKi | - | - | - | Mol Pharmacol (2009) 76: 356-68 [PMID:19407080] |
| M3 receptor in Human [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| GtoPdb | - | - | 6.1 | pKi | - | - | - | Mol Pharmacol (2009) 76: 356-68 [PMID:19407080] |
| M4 receptor in Human [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| GtoPdb | - | - | 5.9 | pKi | - | - | - | Mol Pharmacol (2009) 76: 356-68 [PMID:19407080] |
| M5 receptor in Human [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| GtoPdb | - | - | 5.6 | pKi | - | - | - | Mol Pharmacol (2009) 76: 356-68 [PMID:19407080] |
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]
