vicriviroc [Ligand Id: 807] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL82301 (MK-7690, SCH-351125, SCH-417690 FREE BASE, SCH-D, Vicriviroc) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681] | ||||||||
| ChEMBL | Antagonistic activity against C-C chemokine receptor type 5 | F | 8.6 | pKi | 2.5 | nM | Ki | J Med Chem (2004) 47: 2405-2408 [PMID:15115380] |
| ChEMBL | Inhibition of [125I]RANTES binding to CCR5 receptor. | B | 8.68 | pKi | 2.1 | nM | Ki | Bioorg Med Chem Lett (2003) 13: 709-712 [PMID:12639564] |
| GtoPdb | - | - | 9.1 | pKi | - | - | - | Antimicrob Agents Chemother (2005) 49: 4911-9 [PMID:16304152] |
| ChEMBL | Displacement of [125I]MIP-1beta from CCR5 in IL-10-stimulated human monocytes | B | 8.52 | pIC50 | 3 | nM | IC50 | ACS Med Chem Lett (2010) 1: 483-487 [PMID:24900235] |
| ChEMBL | Antagonist activity at CCR5 in IL-10 stimulated human PBMC cells assessed as MIP-1beta induced chemotaxis | F | 8.92 | pIC50 | 1.2 | nM | IC50 | ACS Med Chem Lett (2010) 1: 483-487 [PMID:24900235] |
| ChEMBL | Binding affinity to CCR5 | B | 9.35 | pIC50 | 0.45 | nM | IC50 | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| CCR5/C-C chemokine receptor type 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3676] [GtoPdb: 62] [UniProtKB: P51682] | ||||||||
| ChEMBL | Displacement of [125I]-RANTES from CCR5 in mouse NIH/3T3 cells after 1 hr | B | 9.04 | pIC50 | 0.91 | nM | IC50 | Eur J Med Chem (2018) 147: 115-129 [PMID:29425816] |
| M1 receptor/Muscarinic acetylcholine receptor M1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229] | ||||||||
| ChEMBL | Antagonistic activity against muscarinic M1 receptor | F | 5 | pKi | >10000 | nM | Ki | J Med Chem (2004) 47: 2405-2408 [PMID:15115380] |
| M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172] | ||||||||
| ChEMBL | Antagonistic activity against Muscarinic acetylcholine receptor M2 | F | 5 | pKi | >10000 | nM | Ki | J Med Chem (2004) 47: 2405-2408 [PMID:15115380] |
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]
