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 | Inhibition of human wild type CCR1 | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2017) 60: 4735-4779 [PMID:28165741] |
| ChEMBL | Inhibition of human recombinant CCR1 | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2017) 60: 4735-4779 [PMID:28165741] |
| 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] |
| C-C chemokine receptor type 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5499] [UniProtKB: A6I4C9] | ||||||||
| ChEMBL | Binding affinity at rat CCR1 | B | 7.23 | pIC50 | 59 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 3367-3372 [PMID:17446072] |
| GPR35/G-protein coupled receptor 35 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293267] [GtoPdb: 102] [UniProtKB: Q9HC97] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR35 | F | 5.97 | pIC50 | 1069.98 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| FPR3/N-formyl peptide receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5646] [GtoPdb: 224] [UniProtKB: P25089] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: FPR3 | F | 5.42 | pIC50 | 3835.13 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
| GPR65/Psychosine receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3714081] [GtoPdb: 113] [UniProtKB: Q8IYL9] | ||||||||
| ChEMBL | GPCR PRESTO-Tango dose-response in antagonist mode with target: GPR65 | F | 5.62 | pIC50 | 2373.76 | nM | IC50 | EUbOPEN Chemogenomics Library - GPCR Dose-Respose |
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]
