GW7647 [Ligand Id: 2674] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL21241 (GW7647)
  • Farnesoid X receptor/Bile acid receptor FXR in Human [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1]
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  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
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  • Pre-mRNA-splicing factor 19 in Saccharomyces cerevisiae S288c [ChEMBL: CHEMBL5058] [UniProtKB: P32523]
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  • ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1 in Human [ChEMBL: CHEMBL1795087] [GtoPdb: 2428] [UniProtKB: O94782]
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  • ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782, Q8TAF3]
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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 Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay B 5.31 pIC50 4910 nM IC50 Bioorg. Med. Chem. (2013) 21: 4266-4278 [PMID:23688559]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Binding affinity to PPARalpha LBD (unknown origin) by surface plasmon resonance assay B 4.02 pKd 96400 nM Kd Bioorg. Med. Chem. Lett. (2014) 24: 2957-2962 [PMID:24821375]
ChEMBL Binding affinity to human PPAR-alpha LBD assessed as recruitment of fluorescein-labeled coactivator peptide by surface plasmon resonance method B 7.49 pKd 32.4 nM Kd Bioorg. Med. Chem. Lett. (2014) 24: 3168-3174 [PMID:24856059]
ChEMBL Binding affinity to human PPARalpha (unknown origin) by competitive TR-FRET assay B 9 pKd 1 nM Kd J. Med. Chem. (2013) 56: 1535-1543 [PMID:23286787]
ChEMBL Binding affinity to PPARalpha (unknown origin) by TR-FRET assay B 8.92 pKi 1.2 nM Ki Bioorg Med Chem (2019) 27: 2948-2958 [PMID:31128991]
ChEMBL Displacement of Fluormone-Pan-PPAR Green from human GST-tagged PPARalpha LBD by TR-FRET assay B 10.27 pKi 0.05 nM Ki J Med Chem (2017) 60: 7459-7475 [PMID:28799755]
ChEMBL Agonist activity at PPARalpha-LBD expressed in HEK293 cells co-expressing GAL4-DBD after 16 to 19 hrs by beta lactamase reporter gene assay F 9.34 pIC50 0.46 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 6233-6236 [PMID:22939697]
ChEMBL Agonist activity at PPARalpha LBD (unknown origin) assessed as induction of PGC1alpha co-activator activity by TR-FRET analysis B 4.73 pEC50 18600 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 2957-2962 [PMID:24821375]
ChEMBL Agonist activity at human Gal4 fused PPARalpha LBD expressed in COS-7 cells incubated for 24 hrs by firefly luciferase reporter gene assay B 5.68 pEC50 2080 nM EC50 Eur J Med Chem (2021) 218: 113388-113388 [PMID:33784603]
ChEMBL Agonist activity at human PPARalpha LBD by cell based luciferase reporter gene assay F 6.4 pEC50 400 nM EC50 J. Med. Chem. (2011) 54: 788-808 [PMID:21218783]
ChEMBL Agonist activity at wild-type human PPARalpha Thr279Ala mutant expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay B 6.6 pEC50 250 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4048-4052 [PMID:25022880]
ChEMBL Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay B 6.64 pEC50 230 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 4048-4052 [PMID:25022880]
ChEMBL Transactivation of human PPARalpha LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay B 6.64 pEC50 230 nM EC50 Bioorg. Med. Chem. Lett. (2010) 20: 2469-2473 [PMID:20307981]
ChEMBL Transactivation of human GAL4-fused PPARalpha ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay B 6.7 pEC50 200 nM EC50 Bioorg. Med. Chem. Lett. (2012) 22: 7662-7666 [PMID:23102891]
ChEMBL Transactivation of human PPARalpha expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay B 6.7 pEC50 200 nM EC50 J. Med. Chem. (2016) 59: 61-81 [PMID:26595749]
ChEMBL Agonist activity at human PPARalpha expressed in HEK293 cells assessed as receptor transactivation at by luciferase reporter gene assay F 6.7 pEC50 200 nM EC50 J. Med. Chem. (2009) 52: 6224-6232 [PMID:19791744]
ChEMBL Agonist activity at PPARalpha ligand binding domain expressed in HEK293 cells co-expressing GAL4 after 18 hrs by dual-luciferase activity based transactivation assay B 6.7 pEC50 200 nM EC50 Bioorg. Med. Chem. Lett. (2011) 21: 4869-4872 [PMID:21742490]
ChEMBL Agonist activity at Gal4-fused PPARalpha expressed in HEK293 cells after 18 hrs by dual luciferase reporter gene assay F 6.7 pEC50 200 nM EC50 Eur. J. Med. Chem. (2011) 46: 5218-5224 [PMID:21889235]
ChEMBL Transactivation of PPARalpha expressed in HEK293A cells co-expressing GAL4 after 16 to 18 hrs by luciferase reporter gene assay B 6.7 pEC50 200 nM EC50 Eur. J. Med. Chem. (2012) 58: 317-322 [PMID:23137448]
ChEMBL Transactivation of GAL4-fused human PPARalpha ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay B 6.7 pEC50 200 nM EC50 J. Med. Chem. (2012) 55: 10771-10775 [PMID:23130964]
ChEMBL Agonist activity at human PPARalpha F 7.3 pEC50 50 nM EC50 J. Med. Chem. (2012) 55: 4027-4061 [PMID:22260081]
ChEMBL Agonist activity at GAL4N fused human PPARalpha LBD expressed in HEK293 cells co-expressing TK-MH100x4-Luc after 24 hrs by luciferase reporter gene assay B 7.59 pEC50 26 nM EC50 Bioorg Med Chem Lett (2017) 27: 3131-3134 [PMID:28539218]
ChEMBL Agonist activity at N-terminal Gal4 fused human PPARalpha LBD transfected in HEK293 cells after 24 hrs by luciferase reporter gene assay B 7.68 pEC50 21 nM EC50 Bioorg Med Chem (2016) 24: 5455-5461 [PMID:27622746]
ChEMBL Agonist activity at GAL4-tagged human PPARalpha ligand binding domain chimeric receptor expressed in HEK293 cells after 24 hrs by luciferase reporter gene assay B 7.68 pEC50 21 nM EC50 Bioorg Med Chem (2016) 24: 5258-5269 [PMID:27591006]
ChEMBL Agonist activity at GAL4-tagged PPARalpha ligand-binding domain (unknown origin) expressed in HEK293T cells incubated for 16 to 19 hrs by beta-lactamase reporter gene assay B 7.81 pEC50 15.4 nM EC50 Bioorg. Med. Chem. Lett. (2015) 25: 270-275 [PMID:25491112]
ChEMBL Agonist activity at PPAR-alpha (unknown origin) expressed in HEK293 cells by luciferase reporter gene assay B 7.87 pEC50 13.6 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 3168-3174 [PMID:24856059]
ChEMBL Agonist activity at human PPARalpha transfected in human HepG2 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay B 8.05 pEC50 9 nM EC50 Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359]
ChEMBL Agonist activity at PPAR-alpha (unknown origin) expressed in HEK293 cells by TR-FRET assay B 8.15 pEC50 7.1 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 3168-3174 [PMID:24856059]
ChEMBL Agonist activity at human GAL4 fused PPARalpha-LBD expressed in human HepG2 cells after 18 hrs by luciferase reporter gene assay B 8.15 pEC50 7 nM EC50 Eur J Med Chem (2018) 159: 267-276 [PMID:30296685]
ChEMBL Agonist activity at human PPARalpha transfected in human MCF7 cells after 16 hrs by luciferase reporter gene assay B 8.19 pEC50 6.5 nM EC50 J. Med. Chem. (2015) 58: 6639-6652 [PMID:26226490]
GtoPdb - - 8.2 pEC50 - - - Diabetes (1999) 48: 1415-24 [PMID:10389847];
Bioorg Med Chem Lett (2001) 11: 1225-7 [PMID:11354382]
ChEMBL In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR alpha ligand binding domain B 8.22 pEC50 6 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1225-1227 [PMID:11354382]
ChEMBL Agonist activity at PPARalpha (unknown origin) B 8.22 pEC50 6 nM EC50 Eur J Med Chem (2018) 159: 267-276 [PMID:30296685]
ChEMBL Agonist activity at GAL4-tagged PPARalpha-LBD (unknown origin) expressed in HEK293 cells assessed as induction of receptor transactivation incubated for 16 hrs by luciferase reporter gene assay B 8.27 pEC50 5.4 nM EC50 J Med Chem (2020) 63: 13124-13139 [PMID:33142057]
ChEMBL Agonist activity at PPARalpha (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay B 8.3 pEC50 5 nM EC50 ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410]
ChEMBL Agonist activity at human PPAR-alpha B 8.52 pEC50 3 nM EC50 J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
ChEMBL Agonist activity at PPARalpha (unknown origin) by Alpha Screen assay B 8.52 pEC50 3 nM EC50 MedChemComm (2019) 10: 1412-1419 [PMID:31673308]
ChEMBL Displacement of pan-PPAR fluormone from PPARalpha LBD by TR-FRET based LanthaScreen assay B 8.74 pEC50 1.8 nM EC50 J. Med. Chem. (2012) 55: 4978-4989 [PMID:22582973]
ChEMBL Agonist activity at human PPARalpha expressed in HEK293 cells by luciferase reporter gene assay B 9.05 pEC50 0.89 nM EC50 Bioorg. Med. Chem. Lett. (2014) 24: 5265-5267 [PMID:25305688]
ChEMBL Activation of PPARalpha transfected in HEK293 cells after 18 hrs by firefly luciferase reporter gene-based luminescence assay relative to control B 9.22 pEC50 0.6 nM EC50 J. Nat. Prod. (2011) 74: 1779-1786 [PMID:21800856]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Activation of murine PPAR alpha ligand binding domain B 9 pEC50 1 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1225-1227 [PMID:11354382]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR delta ligand binding domain B 5.21 pEC50 6200 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1225-1227 [PMID:11354382]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
ChEMBL Activation of murine PPAR delta ligand binding domain B 5.54 pEC50 2900 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1225-1227 [PMID:11354382]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Binding affinity to human PPARgamma (unknown origin) by competitive TR-FRET assay B 6.74 pKd 180 nM Kd J. Med. Chem. (2013) 56: 1535-1543 [PMID:23286787]
ChEMBL In vitro transcriptional activation in CV-1 cells expressing human Gal4-PPAR gamma ligand binding domain B 5.96 pEC50 1100 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1225-1227 [PMID:11354382]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238]
ChEMBL Activation of murine PPAR gamma ligand binding domain B 5.89 pEC50 1300 nM EC50 Bioorg. Med. Chem. Lett. (2001) 11: 1225-1227 [PMID:11354382]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat. Chem. Biol. (2009) 5: 765-771 [PMID:19734910]
Pre-mRNA-splicing factor 19 in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5058] [UniProtKB: P32523]
ChEMBL Agonist activity at human PPARalpha expressed in human MCF7 cells coexpressing TIF2 by luciferase reporter gene assay F 6.75 pEC50 178 nM EC50 Bioorg. Med. Chem. (2008) 16: 10098-10105 [PMID:18952442]
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795087] [GtoPdb: 2428] [UniProtKB: O94782]
ChEMBL Inhibition of USP1 (unknown origin) assessed as reduction in K63-linked diUb cleavage by gel electrophoresis based orthogonal diUb cleavage assay B 5.3 pIC50 5000 nM IC50 J. Med. Chem. (2015) 58: 1581-1595 [PMID:25364867]
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782, Q8TAF3]
ChEMBL Inhibition of human USP1/UAF1 complex using Ub-Rho as substrate by qHTS assay B 5.3 pIC50 5000 nM IC50 J Med Chem (2016) 59: 9321-9336 [PMID:27362876]

ChEMBL data shown on this page come from version 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]