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 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]
