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: O94782Q8TAF3]
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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 based LanthaScreen competitive binding assay B 8 pKi 10 nM Ki ACS Med Chem Lett (2022) 13: 1131-1136 [PMID:35859875]
ChEMBL Binding affinity to PPARalpha (unknown origin) assessed as inhibition constant by Cheng-Prusoff equation analysis B 8.15 pKi 7 nM Ki J Nat Prod (2022) 85: 2804-2816 [PMID:36475432]
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 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 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 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 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 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 Partial agonist activity at PPARalpha (unknown origin) assessed as increase in PRIP/RAP250 coactivator peptide requirement by Lanthascreen TR-FRET assay B 7.7 pEC50 20 nM EC50 J Nat Prod (2022) 85: 2804-2816 [PMID:36475432]
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 pBIND tagged human PPARalpha expressed in human HepG2 cells incubated for 18 hrs by dual luciferase reporter assay B 8.05 pEC50 9 nM EC50 Bioorg Med Chem (2022) 56: 116615-116615 [PMID:35051813]
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 PPARalpha measured by dual luciferase reporter gene assay B 8.15 pEC50 7 nM EC50 Eur J Med Chem (2022) 229: 114061-114061 [PMID:34954593]
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 expressed in HEK293 cells by luciferase/beta-galactosidase reporter gene assay B 8.19 pEC50 6.5 nM EC50 J Med Chem (2022) 65: 1961-1978 [PMID:35089724]
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 human PPARalpha incubated for 22 to 24 hrs by luciferase assay B 8.24 pEC50 5.7 nM EC50 ACS Med Chem Lett (2023) 14: 766-776 [PMID:37312852]
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 PPARalpha (unknown origin) by Alpha Screen assay B 8.52 pEC50 3 nM EC50 Medchemcomm (2019) 10: 1412-1419 [PMID:31673308]
ChEMBL Agonist activity at human PPAR-alpha B 8.52 pEC50 3 nM EC50 J Med Chem (2016) 59: 9201-9214 [PMID:27652492]
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 PPARalpha (unknown origin) B 8.85 pEC50 1.4 nM EC50 J Med Chem (2022) 65: 2571-2592 [PMID:35060744]
ChEMBL Agonist activity at human PPAR-alpha expressed in CHO-K1 cells by PathHunter assay B 9 pEC50 1 nM EC50 J Med Chem (2022) 65: 9974-10000 [PMID:35797110]
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: O94782Q8TAF3]
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 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]