BMS-817399 [Ligand Id: 9497] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL3334824 (Bms-817399, BMS-817399)
  • CCR1/C-C chemokine receptor type 1 in Human [ChEMBL: CHEMBL2413] [GtoPdb: 58] [UniProtKB: P32246]
  • CCR1/C-C chemokine receptor type 1 in Mouse [ChEMBL: CHEMBL3872] [GtoPdb: 58] [UniProtKB: P51675]
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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]
ChEMBL Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of LKN1-mediated CD11b upregulation preincubated for 1 hr B 7.38 pIC50 42 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human whole blood assessed as blocked of MIP-1alpha-mediated CD11b upregulation preincubated for 1 hr B 7.6 pIC50 25 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of LKN1-induced chemotaxis after 60 mins B 7.79 pIC50 16.2 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MPIF1-induced chemotaxis after 60 mins B 7.84 pIC50 14.3 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MCP3-induced chemotaxis after 60 mins B 8.03 pIC50 9.3 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC1-induced chemotaxis after 60 mins B 8.12 pIC50 7.5 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha induced chemotaxis after 60 mins B 8.22 pIC50 6 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of MIP-1alpha-induced chemotaxis after 60 mins B 8.26 pIC50 5.5 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Displacement of [125I]hMIP-1alpha from CCR1 in human PBMC B 8.38 pIC50 4.2 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of RANTES-induced chemotaxis after 60 mins B 8.48 pIC50 3.3 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
ChEMBL Antagonist activity at CCR1 receptor in human THP1 cells assessed as inhibition of HCC4-induced chemotaxis after 60 mins B 8.49 pIC50 3.2 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
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 8.52 pIC50 3 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 8.82 pIC50 1.5 nM IC50 Bioorg Med Chem Lett (2019) 29: 435-440 [PMID:30455146]
GtoPdb Displacement of [125I]MIP-1α from CCR1 in human THP-1 cells. - 9 pIC50 1 nM IC50 J Med Chem (2014) 57: 7550-64 [PMID:25101488]
ChEMBL Displacement of [125I]MIP-1alpha from CCR1 in human THP1 cells B 9 pIC50 1 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
CCR1/C-C chemokine receptor type 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3872] [GtoPdb: 58] [UniProtKB: P51675]
ChEMBL Displacement of [125I]hMIP-1alpha from mouse CCR1 B 4.3 pIC50 >50000 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
Chemokine (C-C motif) receptor 1 in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3334417] [UniProtKB: Q2V0Q7]
ChEMBL Displacement of [125I]hMIP-1alpha from dog PBMC CCR1 B 6.2 pIC50 635 nM IC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]
Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469]
ChEMBL Transactivation of human full-length PXR transfected in human HepG2 cells after 24 hrs by luciferase reporter gene assay B 4.6 pEC50 >25000 nM EC50 J Med Chem (2014) 57: 7550-7564 [PMID:25101488]

ChEMBL data shown on this page come from version 32:

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]