BMS309403 [Ligand Id: 6735] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL247920 (BMS-309403) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
| ChEMBL | Agonist activity at FXR-LBD (unknown origin) using fluorescein-coactivator peptide incubated for 3 hrs by TR-FRET assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| ChEMBL | Agonist activity at FXR (unknown origin) expressed in human HepG2 cells co-transfected with human RXR assessed as luciferase activity incubated for 24 hrs by cell-based luciferase assay | B | 8 | pEC50 | >10 | nM | EC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| 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 | Binding affinity to human FABP4 expressed in Escherichia coli assessed as degree of fluorescent shift by temperature-dependent fluorescence thermal shift assay | B | 8.4 | pKd | 4 | nM | Kd | Eur J Med Chem (2017) 138: 854-873 [PMID:28738306] |
| ChEMBL | Displacement of 1,8-ANS from FABP4 (unknown origin) assessed as inhibition constant by fluorescence based analysis | B | 6.44 | pKi | 360 | nM | Ki | Eur J Med Chem (2023) 253: 115319-115319 [PMID:37037141] |
| 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 | Binding affinity to FABP4 (unknown origin) assessed as inhibition constant | B | 6.8 | pKi | 160 | nM | Ki | Eur J Med Chem (2017) 138: 854-873 [PMID:28738306] |
| 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 assessed as inhibition constant by fluorescent displacement assay | B | 8.7 | pKi | <2 | nM | Ki | Eur J Med Chem (2017) 138: 854-873 [PMID:28738306] |
| ChEMBL | Displacement of BODIPY 500/510 C4 from human FABP4 expressed in Escherichia coli incubated for 30 mins by FP assay | B | 4.6 | pIC50 | >25000 | nM | IC50 | Eur J Med Chem (2017) 138: 854-873 [PMID:28738306] |
| ChEMBL | Inhibition of FABP4 (unknown origin) | B | 6.15 | pIC50 | 710 | nM | IC50 | Eur J Med Chem (2017) 138: 854-873 [PMID:28738306] |
| ChEMBL | Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP4 (unknown origin) incubated for 3 mins by fluorescence based assay | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| 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 1/Fatty acid-binding protein, liver in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5421] [GtoPdb: 2531] [UniProtKB: P07148] | ||||||||
| ChEMBL | Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP1 (unknown origin) incubated for 3 mins by fluorescence based assay | B | 5.4 | pIC50 | 4000 | nM | IC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| fatty acid binding protein 3/Fatty acid binding protein muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3344] [GtoPdb: 2533] [UniProtKB: P05413] | ||||||||
| ChEMBL | Binding affinity to human FABP3 expressed in Escherichia coli assessed as degree of fluorescent shift by temperature-dependent fluorescence thermal shift assay | B | 4.6 | pKd | >25000 | nM | Kd | Eur J Med Chem (2017) 138: 854-873 [PMID:28738306] |
| ChEMBL | Displacement of 1,8-ANS from FABP3 (unknown origin) assessed as inhibition constant by fluorescence based analysis | B | 4.52 | pKi | 30280 | nM | Ki | Eur J Med Chem (2023) 253: 115319-115319 [PMID:37037141] |
| 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 | Displacement of 8-anilino-1-naphthalene-sulfonic acid from FABP3 (unknown origin) incubated for 3 mins by fluorescence based assay | B | 4.85 | pIC50 | 14200 | nM | IC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| ChEMBL | Displacement of BODIPY 500/510 C4 from human FABP3 expressed in Escherichia coli incubated for 30 mins by FP assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Eur J Med Chem (2017) 138: 854-873 [PMID:28738306] |
| Liver X receptor-α/LXR-alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2808] [GtoPdb: 602] [UniProtKB: Q13133] | ||||||||
| ChEMBL | Inhibition of Gal-DBD and NHRLBD fused LXRalpha (unknown origin) transfected in African green monkey CV-1 cells by luciferase assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| Liver X receptor-β/LXR-beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4093] [GtoPdb: 601] [UniProtKB: P55055] | ||||||||
| ChEMBL | Inhibition of Gal-DBD and NHRLBD fused LXRbeta (unknown origin) transfected in African green monkey CV-1 cells by luciferase assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Inhibition of pBIND-PPARalpha (unknown origin) transfected in HepG2 cells incubated for 18 hrs in presence of GW0742 by dual luciferase reporter assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Inhibition of PPARgamma (unknown origin) transfected in HEK293 cells incubated for 18 hrs in presence of rosiglitazone by dual luciferase reporter assay | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
| Thyroid hormone receptor-β/Thyroid hormone receptor beta-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1947] [GtoPdb: 589] [UniProtKB: P10828] | ||||||||
| ChEMBL | Activation of pGAL4 fused THRbeta LBD (unknown origin) transfected in HEK293 cells cotransfected with pG5-Luc and pRL-TK incubated for 24 hrs by Renilla/Firefly based dual-glo luciferase assay | B | 5 | pEC50 | >10000 | nM | EC50 | J Med Chem (2023) 66: 6082-6104 [PMID:37079895] |
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]
