pioglitazone [Ligand Id: 2694] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL595 (Actos, AD-4833, Duetact, Glustin, Pioglitazone, U-72107, Zactos) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| aldo-keto reductase family 1 member B/Aldose reductase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2622] [GtoPdb: 2768] [UniProtKB: P07943] | ||||||||
| ChEMBL | DRUGMATRIX: Aldose Reductase enzyme inhibition (substrate: DL-Glyceraldehyde) | B | 4.88 | pIC50 | 13200 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342] | ||||||||
| ChEMBL | Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 6.52 | pIC50 | 300 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
| ABCB11/Bile salt export pump in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2073674] [GtoPdb: 778] [UniProtKB: O70127] | ||||||||
| ChEMBL | Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake | B | 5.7 | pIC50 | 2000 | nM | IC50 | Drug Metab Dispos (2012) 40: 130-138 [PMID:21965623] |
| carbonic anhydrase 2/Carbonic anhydrase II in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL205] [GtoPdb: 3092] [UniProtKB: P00918] | ||||||||
| ChEMBL | DRUGMATRIX: Carbonic Anhydrase II enzyme inhibition (substrate: 4-Nitrophenyl acetate (4-NPA)) | B | 6.94 | pIC50 | 114 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| carnitine palmitoyltransferase 1A/Carnitine O-palmitoyltransferase 1, liver isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1293194] [GtoPdb: 3249] [UniProtKB: P50416] | ||||||||
| ChEMBL | SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 1, liver isoform | B | 5 | pIC50 | >10000 | nM | IC50 | Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752). |
| carnitine palmitoyltransferase 1B/Carnitine O-palmitoyltransferase 1, muscle isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2216739] [GtoPdb: 3250] [UniProtKB: Q92523] | ||||||||
| ChEMBL | SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 1, muscle isoform | B | 4 | pIC50 | >100000 | nM | IC50 | Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752). |
| carnitine palmitoyltransferase 2/Carnitine palmitoyltransferase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3238] [GtoPdb: 3252] [UniProtKB: P23786] | ||||||||
| ChEMBL | SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 2 | B | 4 | pIC50 | >100000 | nM | IC50 | Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752). |
| carnitine palmitoyltransferase 2/Carnitine palmitoyltransferase 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4037] [GtoPdb: 3252] [UniProtKB: P18886] | ||||||||
| ChEMBL | SUPPLEMENTARY: Inhibition of Carnitine palmitoyltransferase 2 | B | 4 | pIC50 | >100000 | nM | IC50 | Roche carnitine palmitoyltransferase modulator screening data (supplementary data associated with the publication CHEMBL2216752). |
| CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] | ||||||||
| ChEMBL | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by Cheng-Prusoff analysis | B | 6.43 | pKi | 370 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671] |
| ChEMBL | Displacement of [3H]rosiglitazone from recombinant human C-terminal His-tagged MitoNEET cytosolic domain (32 to 108 residues) expressed in Escherichia coli BL21 by scintillation proximity assay | B | 5.06 | pIC50 | 8650 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5350-5353 [PMID:27687671] |
| CDGSH iron-sulfur domain-containing protein 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3308979] [UniProtKB: B0K020] | ||||||||
| ChEMBL | Displacement of [3H]rosiglitazone from rat liver mitochondrial mitoNEET by scintillation counting | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 819-823 [PMID:20064719] |
| CDGSH iron-sulfur domain-containing protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523399] [UniProtKB: Q8N5K1] | ||||||||
| ChEMBL | Binding affinity to recombinant human N-terminal His6-tagged NAF1 expressed in Escherichia coli by scintillation proximity assay | B | 5.32 | pIC50 | 4800 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 901-904 [PMID:30770154] |
| Enoyl-[acyl-carrier-protein] reductase [NADH] in Francisella tularensis subsp. tularensis (strain SCHU S4 / Schu 4) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2150835] [UniProtKB: Q5NGQ3] | ||||||||
| ChEMBL | Inhibition of C-terminal His6-tagged Francisella tularensis SCHU S4 FabI expressed in Escherichia coli BL21 (DE3) using CrCoA as substrate assessed as oxidation of NADH to NAD+ by fluorescence assay | B | 4.1 | pIC50 | 79000 | nM | IC50 | J Med Chem (2013) 56: 5275-5287 [PMID:23815100] |
| Monoamine oxidase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1951] [GtoPdb: 2489] [UniProtKB: P21397] | ||||||||
| ChEMBL | DRUGMATRIX: Monoamine Oxidase MAO-A enzyme inhibition (substrate: Kynuramine) | B | 4.46 | pIC50 | 35069 | nM | IC50 | DrugMatrix in vitro pharmacology data |
| Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
| ChEMBL | Competitive inhibition of human MAOB expressed in Pichia pastoris | B | 6.3 | pKi | 500 | nM | Ki | ACS Med Chem Lett (2012) 3: 39-42 [PMID:22282722] |
| ChEMBL | Inhibition of human recombinant microsomal MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay | B | 6.57 | pKi | 270.8 | nM | Ki | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
| ChEMBL | Inhibition of human recombinant soluble MAO-B expressed in Pichia pastoris incubated for 30 mins prior to substrate addition measured after 60 mins by MAO-Glo assay | B | 6.7 | pKi | 199.4 | nM | Ki | Bioorg Med Chem (2015) 23: 770-778 [PMID:25600407] |
| ChEMBL | Inhibition of human recombinant MAO-B after 15 mins | B | 6.53 | pIC50 | 298 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5295-5298 [PMID:20650633] |
| Monoamine oxidase B in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2993] [GtoPdb: 2490] [UniProtKB: P19643] | ||||||||
| ChEMBL | Competitive inhibition of rat MAOB expressed in Pichia pastoris | B | 5.68 | pKi | 2100 | nM | Ki | ACS Med Chem Lett (2012) 3: 39-42 [PMID:22282722] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Receptor binding affinity to human Peroxisome proliferator activated receptor alpha against [3H]-NNC 0061-4655 radioligand | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
| ChEMBL | Agonist activity at PPARalpha (unknown origin) | B | 5.17 | pEC50 | 6700 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| ChEMBL | In vitro transactivation using receptor transactivation assay against hPPAR alpha | F | 5.18 | pEC50 | 6680 | nM | EC50 | J Med Chem (2002) 45: 789-804 [PMID:11831892] |
| ChEMBL | In vitro transactivation of human Peroxisome proliferator activated receptor alpha (hPPARalpha) | B | 5.18 | pEC50 | 6680 | nM | EC50 | J Med Chem (2003) 46: 4883-4894 [PMID:14584939] |
| 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 mouse liver PPARalpha | B | 5.94 | pIC50 | 1150 | nM | IC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| 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 6His-tagged PPARgamma LBD expressed in Escherichia coli BL21(DE3) using FITC-NTKNHPMLMNLLKDNPAQD peptide by isothermal titration calorimetry | B | 6.06 | pKd | 871 | nM | Kd | J Med Chem (2019) 62: 2008-2023 [PMID:30676741] |
| ChEMBL | Binding affinity against Peroxisome proliferator activated receptor gamma (PPAR gamma) | B | 5.91 | pKi | 1230.27 | nM | Ki | Bioorg Med Chem Lett (1999) 9: 3329-3334 [PMID:10612594] |
| ChEMBL | In vitro binding to peroxisome proliferator activated receptor gamma (PPAR gamma) using [3H]-BRL 49653 as radioligand in scintillation proximity assay (SPA) | B | 5.91 | pKi | 1230.27 | nM | Ki | J Med Chem (1998) 41: 5020-5036 [PMID:9836620] |
| ChEMBL | Binding affinity to human Peroxisome proliferator activated receptor gamma using scintillation proximity assay | B | 6.2 | pKi | 630 | nM | Ki | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | Displacement of fluormone PanPPAR green tracer ligand from human 6His-tagged PPARgamma isoform 1 LBD (203 to 477 residues) expressed in Escherichia coli BL21(DE3) after 1 hr by TR-FRET assay | B | 6.38 | pKi | 420 | nM | Ki | J Med Chem (2019) 62: 2008-2023 [PMID:30676741] |
| ChEMBL | Binding affinity to PPARgamma (unknown origin) by TR-FRET assay | B | 6.47 | pKi | 340 | nM | Ki | Bioorg Med Chem (2019) 27: 2948-2958 [PMID:31128991] |
| ChEMBL | Binding affinity to PPAR-gamma (unknown origin) by TR-FRET assay | B | 7.02 | pKi | 96 | nM | Ki | J Med Chem (2020) 63: 16012-16027 [PMID:33325691] |
| ChEMBL | Binding affinity to PPARgamma (unknown origin) by TR-FRET assay | B | 7.21 | pKi | 62 | nM | Ki | J Nat Prod (2019) 82: 259-264 [PMID:30672698] |
| ChEMBL | Transrepression activity at human PPARgamma expressed in HEK293 cells assessed as inhibition of TNFalpha induced NF-kappaB promoter activity pretreated for 4 hrs followed by TNFalpha stimulation after 3 hrs by luciferase reporter gene assay | B | 4.66 | pIC50 | 22000 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 2776-2780 [PMID:28465099] |
| ChEMBL | Inhibition of fluormone binding to human PPARgamma LBD after 2 hrs by competitive fluorescence polarization assay | B | 5.1 | pIC50 | 8000 | nM | IC50 | Bioorg Med Chem Lett (2012) 22: 2954-2958 [PMID:22424975] |
| ChEMBL | Receptor binding affinity to human Peroxisome proliferator activated receptor gamma against [3H]ragalitazar radioligand | B | 5.13 | pIC50 | 7400 | nM | IC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
| ChEMBL | Competitive displacement of fluorescently labelled PPAR tracer ligand from GST-tagged human PPARgamma ligand binding domain after 1 hr in dark by TR-FRET competitive binding assay | B | 5.75 | pIC50 | 1790 | nM | IC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| ChEMBL | Displacement of FITC-NCoR1 peptide from human 6His-tagged PPARgamma isoform 1 LBD (203 to 477 residues) expressed in Escherichia coli BL21(DE3) after 1 hr by FITC/TR-FRET assay | B | 5.77 | pIC50 | 1700 | nM | IC50 | J Med Chem (2019) 62: 2008-2023 [PMID:30676741] |
| ChEMBL | Displacement of fluormone PPAR-green from N-terminal His-tagged human PPARgamma-LBD after 2 hrs by fluorescence polarization assay | B | 6.07 | pIC50 | 855 | nM | IC50 | Bioorg Med Chem (2010) 18: 8315-8323 [PMID:21030263] |
| ChEMBL | Displacement of [3H]rosiglitazone from PPAR gamma | B | 6.1 | pIC50 | 800 | nM | IC50 | Bioorg Med Chem Lett (2007) 17: 4613-4618 [PMID:17574414] |
| ChEMBL | Agonist activity at PPARgamma (unknown origin) | B | 6.14 | pIC50 | 720 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2907-2912 [PMID:26048793] |
| GtoPdb | - | - | 6.2 | pIC50 | - | - | - |
J Med Chem (1998) 41: 5020-36 [PMID:9836620]; Biochem Biophys Res Commun (2000) 278: 704-11 [PMID:11095972]; J Pharmacol Exp Ther (1998) 284: 751-9 [PMID:9454824] |
| ChEMBL | Transactivation of GAL4-fused human PPARgamma transfected in HEK293BENA cells after 24 hrs by steady glo-luciferase reporter gene assay | B | 5.69 | pEC50 | 2053 | nM | EC50 | J Med Chem (2018) 61: 10067-10083 [PMID:30351933] |
| ChEMBL | Displacement of Fluoromone from GST-tagged recombinant human PPARgamma ligand binding domain by LanthaScreen TR-FRET assay | B | 5.8 | pEC50 | 1600 | nM | EC50 | Eur J Med Chem (2016) 124: 49-62 [PMID:27560282] |
| ChEMBL | Agonist activity at human PPARgammaDEF receptor expressed in african green monkey COS7 cells transfected with pGal5-TK-pGL3/pRenilla-CMV assessed as intrinsic activity measured after 39 hrs by dual luciferase reporter assay | B | 5.8 | pEC50 | 1600 | nM | EC50 | Eur J Med Chem (2020) 195: 112258-112258 [PMID:32272420] |
| ChEMBL | Transactivation of Gal4-fused human PPARgamma transfected in COS7 cells co-transfected with pGAL5-TK-pGL3 and pRennilla-CMV incubated for 39 hrs by dual luciferase reporter assay | B | 5.85 | pEC50 | 1400 | nM | EC50 | Eur J Med Chem (2020) 185: 111748-111748 [PMID:31648125] |
| ChEMBL | Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay | B | 5.89 | pEC50 | 1280 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 767-772 [PMID:23265881] |
| ChEMBL | Partial agonist activity at human PPARgamma-LBD/Gal4 DNA binding domain by transactivation assay | B | 5.89 | pEC50 | 1280 | nM | EC50 | J Med Chem (2011) 54: 4219-4233 [PMID:21557540] |
| ChEMBL | In vitro transactivation of human Peroxisome proliferator activated receptor gamma | B | 6.01 | pEC50 | 970 | nM | EC50 | J Med Chem (2003) 46: 4883-4894 [PMID:14584939] |
| ChEMBL | Agonist activity at PPARgamma (unknown origin) | B | 6.01 | pEC50 | 970 | nM | EC50 | J Med Chem (2020) 63: 5031-5073 [PMID:31930920] |
| ChEMBL | In vitro transactivation using receptor transactivation assay against hPPAR gamma | F | 6.01 | pEC50 | 970 | nM | EC50 | J Med Chem (2002) 45: 789-804 [PMID:11831892] |
| ChEMBL | Transactivation of human GAL4-fused PPARgamma ligand binding domain transfected in HEK293 cells after 18 hrs by dual luciferase reporter gene assay | B | 6.1 | pEC50 | 800 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 7662-7666 [PMID:23102891] |
| ChEMBL | Transactivation activity at Homo sapiens (human) PPARgamma | B | 6.22 | pEC50 | 600 | nM | EC50 | Med Chem Res (2011) 20: 1005-1014 |
| ChEMBL | Activation of peroxisome proliferator activated receptor gamma measured by induction of 50% of maximum alkaline phosphatase activity, transfection assay in CV-1 cells | F | 6.23 | pEC50 | 588.84 | nM | EC50 | J Med Chem (1998) 41: 5020-5036 [PMID:9836620] |
| ChEMBL | Transcriptional activation of peroxisome proliferator activated receptor gamma | F | 6.23 | pEC50 | 588.84 | nM | EC50 | Bioorg Med Chem Lett (1999) 9: 3329-3334 [PMID:10612594] |
| ChEMBL | Agonist activity for Human PPAR gamma receptor in transcriptional activation assay | F | 6.24 | pEC50 | 580 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Maximal reporter activity against human Peroxisome proliferator activated receptor gamma Gal4 chimeric in transiently transfected CV-1 cells by functional assay. | F | 6.24 | pEC50 | 580 | nM | EC50 | Bioorg Med Chem Lett (2001) 11: 3111-3113 [PMID:11720854] |
| ChEMBL | Agonist activity at GAL4-tagged human PPARgamma ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay | B | 6.24 | pEC50 | 570 | nM | EC50 | Bioorg Med Chem (2012) 20: 2141-2151 [PMID:22341573] |
| ChEMBL | Transactivation of PPARgamma in CV1 cells | F | 6.26 | pEC50 | 550 | nM | EC50 | J Med Chem (2006) 49: 4072-4084 [PMID:16821769] |
| ChEMBL | Transactivation of GAL4-fused human PPARgamma ligand binding domain expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay | B | 6.3 | pEC50 | 500 | nM | EC50 | Eur J Med Chem (2016) 124: 49-62 [PMID:27560282] |
| ChEMBL | Partial agonist activity at human PPARgamma expressed in CHO cells co-transfected with Gal4-responsive luciferase reporter plasmid after 24 hrs by transactivation assay | F | 6.41 | pEC50 | 390 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 1978-1982 [PMID:21377875] |
| ChEMBL | Agonist activity at human PPARgamma ligand binding domain expressed in COS-1 cells co-transfected with Gal4 by luciferase reporter gene assay | B | 6.41 | pEC50 | 390 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 220-224 [PMID:21130649] |
| ChEMBL | Transactivation of Gal4 fused human PPARgamma LBD expressed in African green monkey COS7 cells after 42 hrs by dual luciferase reporter gene assay | B | 6.42 | pEC50 | 380 | nM | EC50 | Eur J Med Chem (2017) 126: 590-603 [PMID:27918994] |
| ChEMBL | Transactivation of chimeric Gal4 yeast DBD fused-PPARgamma LBD (unknown origin) expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay | B | 6.46 | pEC50 | 350 | nM | EC50 | J Med Chem (2019) 62: 2008-2023 [PMID:30676741] |
| ChEMBL | Transactivation at Gal4 fused PPARgamma LBD (unknown origin) expressed in African green monkey COS7 cells after 42 hrs by luciferase assay | B | 6.49 | pEC50 | 320 | nM | EC50 | Eur J Med Chem (2016) 124: 138-152 [PMID:27569195] |
| ChEMBL | Modulation of human PPARgamma-LBD expressed in african green monkey COS7 cells co-transfected with Gal4 assessed as activation of transactivation activity by luciferase assay | B | 6.52 | pEC50 | 300 | nM | EC50 | Bioorg Med Chem (2011) 19: 5372-5382 [PMID:21873070] |
| ChEMBL | Transactivation of human PPARgamma 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 | 6.52 | pEC50 | 300 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2469-2473 [PMID:20307981] |
| ChEMBL | Activation of human 6His-tagged PPARgamma isoform 1 LBD (203 to 477 residues) expressed in Escherichia coli BL21(DE3) assessed as increase in FITC-TRAP220 peptide recruitment after 1 hr by FITC/TR-FRET assay | B | 6.59 | pEC50 | 260 | nM | EC50 | J Med Chem (2019) 62: 2008-2023 [PMID:30676741] |
| ChEMBL | Transactivation of full length human PPARgamma2 expressed in HEK293T cells co-expressing PPRE after 18 hrs by luciferase reporter gene assay | B | 6.6 | pEC50 | 250 | nM | EC50 | J Med Chem (2019) 62: 2008-2023 [PMID:30676741] |
| ChEMBL | Agonist activity at PPARgamma in human HepG2 cells assessed as activation of PPRE incubated for 24 hrs by dual luciferase reporter gene assay | B | 6.62 | pEC50 | 240 | nM | EC50 | Bioorg Med Chem (2018) 26: 4153-4167 [PMID:30001846] |
| ChEMBL | Agonist activity at human PPARgamma expressed in HEK293 cells incubated for 18 hrs by luciferase reporter gene assay | B | 6.68 | pEC50 | 210 | nM | EC50 | J Nat Prod (2014) 77: 2513-2521 [PMID:25333853] |
| ChEMBL | Transactivation of human PPARgamma 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 PPARgamma 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 | Activation of Gal4-tagged human PPARgamma expressed in CHO cells by luciferase reporter gene assay | B | 6.85 | pEC50 | 140 | nM | EC50 | Bioorg Med Chem (2010) 18: 5885-5895 [PMID:20656494] |
| ChEMBL | Transactivation of human full length PPARgamma expressed in HEK293 cells after 18 hrs by luciferase reporter gene based luminescence assay | B | 7 | pEC50 | 100 | nM | EC50 | J Nat Prod (2018) 81: 2419-2428 [PMID:30362739] |
| ChEMBL | Transactivation of GAL4-DBD fused human PPARgamma ligand binding domain expressed in UAS-bla HEL 293H cells preincubated for 16 hrs followed by FRET substrate addition and measured after 2 hrs by TR-FRET assay | B | 7.01 | pEC50 | 98 | nM | EC50 | Bioorg Med Chem (2018) 26: 5870-5884 [PMID:30429097] |
| ChEMBL | Agonist activity at PPARgamma assessed as transcriptional activation | F | 7.06 | pEC50 | 88 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2095-2098 [PMID:20219371] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | Displacement of [3H]rosiglitazone from mouse PPARgamma receptor by scintillation proximation assay | B | 6.15 | pIC50 | 700 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 4959-4962 [PMID:18752947] |
| ChEMBL | In vitro transcriptional activation of Peroxisome proliferator activated receptor gamma (PPAR) expressed in CV-1 cells | F | 6.16 | pEC50 | 690 | nM | EC50 | J Med Chem (1996) 39: 665-668 [PMID:8576907] |
| ChEMBL | Agonist activity for murine PPAR gamma receptor in transcriptional activation assay | F | 6.26 | pEC50 | 550 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4797] [GtoPdb: 595] [UniProtKB: O88275] | ||||||||
| ChEMBL | Displacement of [3H]rosigliatzone from PPARgamma in rat adipocytes | B | 6.15 | pIC50 | 700 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3192-3195 [PMID:18482837] |
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]
