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 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]
