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)
  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
  • CCR5/C-C chemokine receptor type 5 in Mouse [ChEMBL: CHEMBL3676] [GtoPdb: 62] [UniProtKB: P51682]
Created with Highcharts 10.3.3ValuesChart context menuC-C chemokine receptor type 5pKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd MousepKi MousepIC50 MousepEC50 Mouse0246810Highcharts.com
  • M1 receptor/Muscarinic acetylcholine receptor M1 in Human [ChEMBL: CHEMBL216] [GtoPdb: 13] [UniProtKB: P11229]
Created with Highcharts 10.3.3ValuesChart context menuMuscarinic acetylcholine receptor M1pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
Created with Highcharts 10.3.3ValuesChart context menuMuscarinic acetylcholine receptor M2pKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
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 35:

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]