GW7647 [Ligand Id: 2674] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL21241 (GW7647) |
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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 | 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 | 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 | 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 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 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 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]
