BMS309403 [Ligand Id: 6735] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL247920 (BMS-309403)
  • fatty acid binding protein 4/Fatty acid binding protein adipocyte in Human [ChEMBL: CHEMBL2083] [GtoPdb: 2534] [UniProtKB: P15090]
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  • fatty acid binding protein 4/Fatty acid-binding protein, adipocyte in Rat [ChEMBL: CHEMBL2021755] [GtoPdb: 2534] [UniProtKB: P70623]
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  • fatty acid binding protein 5/Fatty acid binding protein epidermal in Human [ChEMBL: CHEMBL3674] [GtoPdb: 2535] [UniProtKB: Q01469]
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  • fatty acid binding protein 3/Fatty acid binding protein muscle in Human [ChEMBL: CHEMBL3344] [GtoPdb: 2533] [UniProtKB: P05413]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
fatty acid binding protein 4/Fatty acid binding protein adipocyte in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2083] [GtoPdb: 2534] [UniProtKB: P15090]
ChEMBL Direct binding to His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by isothermal titration calorimetry B 5.69 pKd 2050 nM Kd Bioorg Med Chem (2016) 24: 4310-4317 [PMID:27460668]
ChEMBL Binding affinity at recombinant human 6His-tagged FABP4 expressed in Escherichia coli BL21 DE3 by isothermal titration calorimetry B 6.6 pKd 252.7 nM Kd J Med Chem (2020) 63: 4090-4106 [PMID:32202425]
ChEMBL Displacement of 1,8-ANS from recombinant human 6His-tagged FABP4 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay B 6.6 pKi 253.4 nM Ki J Med Chem (2020) 63: 4090-4106 [PMID:32202425]
ChEMBL Displacement of 1,8-ANS from His6-tagged FABP4 (unknown origin) expressed in Escherichia coli BL21(DE3) cells by fluorescence assay B 6.66 pKi 220 nM Ki Bioorg Med Chem (2016) 24: 4310-4317 [PMID:27460668]
ChEMBL Binding affinity to His-tagged human recombinant FABP4 expressed in Escherichia coli BL21 (DE3) by fluorescence assay B 6.8 pKi 160 nM Ki ACS Med Chem Lett (2016) 7: 435-439 [PMID:27096055]
ChEMBL Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human a-FABP by fluorescence spectrophotometry B 7.82 pKi 15 nM Ki Bioorg Med Chem Lett (2011) 21: 2949-2952 [PMID:21481589]
ChEMBL Displacement of [3H]2,3-bis[(2,4-dichlorobenzyl)oxy]benzoic acid from aFABP B 8.13 pKi 7.4 nM Ki Bioorg Med Chem Lett (2007) 17: 3511-3515 [PMID:17502136]
ChEMBL Displacement of 1,8-ANS from aFABP by fluorescence based-assay B 8.7 pKi <2 nM Ki Bioorg Med Chem Lett (2007) 17: 3511-3515 [PMID:17502136]
ChEMBL Inhibition of human FABP4 by 8-anilino-1-naphthalenesulfonic acid based fluorescence displacement assay B 6.66 pIC50 221 nM IC50 Bioorg Med Chem Lett (2013) 23: 1662-1666 [PMID:23395658]
fatty acid binding protein 4/Fatty acid-binding protein, adipocyte in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2021755] [GtoPdb: 2534] [UniProtKB: P70623]
ChEMBL Inhibition of rat ap2 by fluorescent 1,8-anilino-8-naphthalene sulfonate assay B 7.54 pKi 29 nM Ki Eur J Med Chem (2012) 52: 70-81 [PMID:22483089]
fatty acid binding protein 5/Fatty acid binding protein epidermal in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3674] [GtoPdb: 2535] [UniProtKB: Q01469]
ChEMBL Displacement of 1,8-ANS from recombinant human 6His-tagged FABP5 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay B 5.03 pKi 9240 nM Ki J Med Chem (2020) 63: 4090-4106 [PMID:32202425]
ChEMBL Displacement of 1,8-ANS from eFABP by fluorescence based-assay B 6.46 pKi 350 nM Ki Bioorg Med Chem Lett (2007) 17: 3511-3515 [PMID:17502136]
fatty acid binding protein 3/Fatty acid binding protein muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3344] [GtoPdb: 2533] [UniProtKB: P05413]
ChEMBL Displacement of 1,8-ANS from recombinant human 6His-tagged FABP3 expressed in Escherichia coli BL21 DE3 incubated for 15 mins followed by 1,8-ANS addition and measured after 3 mins by fluorescence based assay B 5.13 pKi 7450 nM Ki J Med Chem (2020) 63: 4090-4106 [PMID:32202425]
ChEMBL Displacement of fluorescent 1-anilinonapthalene 8-sulfonic acid from human h-FABP by fluorescence spectrophotometry B 5.46 pKi 3470 nM Ki Bioorg Med Chem Lett (2011) 21: 2949-2952 [PMID:21481589]
ChEMBL Displacement of 1,8-ANS from mFABP by fluorescence based-assay B 6.6 pKi 250 nM Ki Bioorg Med Chem Lett (2007) 17: 3511-3515 [PMID:17502136]
ChEMBL Inhibition of human FABP3 by 8-anilino-1-naphthalenesulfonic acid based fluorescence displacement assay B 4.83 pIC50 14700 nM IC50 Bioorg Med Chem Lett (2013) 23: 1662-1666 [PMID:23395658]

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]