CP-481,715 [Ligand Id: 3497] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1628706 (CP-481715)
  • CCR1/C-C chemokine receptor type 1 in Human [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
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  • CCR5/C-C chemokine receptor type 5 in Human [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
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  • M2 receptor/Muscarinic acetylcholine receptor M2 in Human [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
CCR1/C-C chemokine receptor type 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
GtoPdb - - 8 pKd 9.2 nM Kd J Biol Chem (2003) 278: 40473-80 [PMID:12909630]
ChEMBL Binding affinity to CCR1 B 7.13 pKi 74 nM Ki J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
ChEMBL Antagonist activity at recombinant CCR1 (unknown origin) expressed in non-adherent cells co-expressing Galpha16 assessed as inhibition of MIP-1 alpha-induced calcium flux by Fluo-4 NW or Calcium 4 dye based FLIPR TETRA assay F 7.23 pIC50 59 nM IC50 Bioorg Med Chem Lett (2019) 29: 435-440 [PMID:30455146]
ChEMBL Antagonist activity at CCR1 in human THP1 cells assessed as inhibition of chemotaxis after 30 mins by Celltiter-glo reagent based luminescence assay B 7.41 pIC50 39 nM IC50 Bioorg Med Chem Lett (2019) 29: 435-440 [PMID:30455146]
CCR5/C-C chemokine receptor type 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL274] [GtoPdb: 62] [UniProtKB: P51681]
ChEMBL Binding affinity to CCR5 B 7.18 pKi 66 nM Ki J Med Chem (2012) 55: 9363-9392 [PMID:22931505]
M2 receptor/Muscarinic acetylcholine receptor M2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL211] [GtoPdb: 14] [UniProtKB: P08172]
ChEMBL Binding affinity to muscarinic M2 receptor B 5.88 pKi 1323 nM Ki J Med Chem (2012) 55: 9363-9392 [PMID:22931505]

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]