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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 |
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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: 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 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]