BMS-817399 [Ligand Id: 9497] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3334824 (Bms-817399, BMS-817399) |
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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 33:
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]
