BX 471 [Ligand Id: 767] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL232656 (BX-471, BX-741) |
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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 | Binding affinity to human CCR1 by radioligand binding assay | B | 9 | pKd | 1 | nM | Kd | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| GtoPdb | - | - | 9 | pKi | 1 | nM | Ki | J Biol Chem (2000) 275: 19000-8 [PMID:10748002] |
| ChEMBL | Binding affinity to CCR1 | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| ChEMBL | Binding Affinity at CCL3 | B | 7.51 | pIC50 | 31 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3109-3112 [PMID:17383873] |
| ChEMBL | Antagonist activity against human CCR1 receptor expressed in THP1 cells assessed as inhibition of chemotaxis | F | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3367-3372 [PMID:17446072] |
| ChEMBL | Antagonist activity at human CCR1 expressed in THP1 cells assessed as effect on MIP-1-alpha-induced calcium flux by FLIPR | F | 7.74 | pIC50 | 18 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3367-3372 [PMID:17446072] |
| ChEMBL | Displacement of [125I]MIP-1-alpha from human recombinant CCR1 expressed in HEK293 cells | B | 8.26 | pIC50 | 5.5 | nM | IC50 | J Med Chem (2009) 52: 1295-1301 [PMID:19183043] |
| ChEMBL | Antagonist activity at human CCR1 in THP1 cells assessed as inhibition of MIP-1-alpha-induced chemotaxis after 3 hrs | F | 8.82 | pIC50 | 1.5 | nM | IC50 | J Med Chem (2009) 52: 1295-1301 [PMID:19183043] |
| 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 | 8.89 | pIC50 | 1.3 | 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 | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 435-440 [PMID:30455146] |
| CCR1/C-C chemokine receptor type 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3872] [GtoPdb: 58] [UniProtKB: P51675] | ||||||||
| ChEMBL | Binding affinity to mouse CCR1 by radioligand binding assay | B | 6.7 | pKd | 200 | nM | Kd | J Med Chem (2012) 55: 9363-9392 [PMID:22931505] |
| ChEMBL | Binding affinity at mouse CCR1 | B | 6.21 | pIC50 | 615 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3367-3372 [PMID:17446072] |
| CCR1/C-C chemokine receptor type 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5499] [GtoPdb: 58] [UniProtKB: Q9JLY8] | ||||||||
| ChEMBL | Binding affinity at rat CCR1 | B | 7.23 | pIC50 | 59 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3367-3372 [PMID:17446072] |
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]
