ML381 [Ligand Id: 8591] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3185781 |
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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 | - | - | 5 | pKi | >10000 | nM | Ki | ChemMedChem (2014) 9: 1677-82 [PMID:24692176] |
| ChEMBL | Antagonist activity at human muscarinic M1 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by by Fluo-4AM staining based fluorescence assay | F | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2022) 65: 6273-6286 [PMID:35417155] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| GtoPdb | - | - | 4.52 | pKi | >30000 | nM | Ki | ChemMedChem (2014) 9: 1677-82 [PMID:24692176] |
| ChEMBL | Antagonist activity at human muscarinic M2 receptor expressed in CHO cells co-expressing Gqi5 assessed as intracellular calcium mobilization by calcium mobilization assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2022) 65: 6273-6286 [PMID:35417155] |
| M3 receptor/Muscarinic acetylcholine receptor M3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL245] [GtoPdb: 15] [UniProtKB: P20309] | ||||||||
| GtoPdb | - | - | 4.52 | pKi | >30000 | nM | Ki | ChemMedChem (2014) 9: 1677-82 [PMID:24692176] |
| ChEMBL | Antagonist activity at human muscarinic M3 receptor expressed in CHO cells co-expressing Gqi5 assessed as intracellular calcium mobilization by calcium mobilization assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2022) 65: 6273-6286 [PMID:35417155] |
| M4 receptor/Muscarinic acetylcholine receptor M4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1821] [GtoPdb: 16] [UniProtKB: P08173] | ||||||||
| GtoPdb | - | - | 4.52 | pKi | <30000 | nM | Ki | ChemMedChem (2014) 9: 1677-82 [PMID:24692176] |
| ChEMBL | Antagonist activity at human muscarinic M4 receptor expressed in CHO cells co-expressing Gqi5 assessed as intracellular calcium mobilization by calcium mobilization assay | F | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2022) 65: 6273-6286 [PMID:35417155] |
| M5 receptor/Muscarinic acetylcholine receptor M5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2035] [GtoPdb: 17] [UniProtKB: P08912] | ||||||||
| GtoPdb | - | - | 6.3 | pKi | - | - | - | ChemMedChem (2014) 9: 1677-82 [PMID:24692176] |
| ChEMBL | Antagonist activity at human muscarinic M5 receptor expressed in CHO cells assessed as inhibition of acetylcholine-induced calcium mobilization by Fluo-4AM staining based fluorescence assay | F | 6.35 | pIC50 | 450 | nM | IC50 | J Med Chem (2022) 65: 6273-6286 [PMID:35417155] |
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]
