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 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]