pioglitazone [Ligand Id: 2694] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL595 (Actos, AD-4833, Duetact, Glustin, Pioglitazona, 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] |
| ChEMBL | Inhibition of recombinant human MAO-B | B | 6.53 | pIC50 | 298 | nM | IC50 | Bioorg Med Chem Lett (2022) 76: 128994-128994 [PMID:36162779] |
| 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 | 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 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 | 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 | Binding affinity to PPARgamma (unknown origin) assessed as inhibition constant by Cheng-Prusoff equation analysis | B | 6.22 | pKi | 600 | nM | Ki | J Nat Prod (2022) 85: 2804-2816 [PMID:36475432] |
| 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 | Displacement of fluormone pan-PPARgreen from GST-tagged human PPARgamma ligand binding domain by LanthaScreen TR-FRET competitive binding assay | B | 6.52 | pKi | 300 | nM | Ki | J Nat Prod (2023) 86: 138-148 [PMID:36529937] |
| ChEMBL | Binding affinity to PPARgamma (unknown origin) by TR-FRET-based competitive binding assay | B | 6.52 | pKi | 300 | nM | Ki | ACS Med Chem Lett (2023) 14: 425-431 [PMID:37077388] |
| ChEMBL | Binding affinity to PPARgamma (unknown origin) assessed as inhibition constant by TR-FRET based LanthaScreen competitive binding assay | B | 6.82 | pKi | 150 | nM | Ki | J Med Chem (2023) 66: 4961-4978 [PMID:36967575] |
| 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 | Agonist activity at PPARgamma LBD (unknown origin) assessed as increase in recruitment of coactivator RAP250 to PPARgamma LBD by TR-FRET-based nuclear receptor coactivator assay | B | 4.75 | pEC50 | 17700 | nM | EC50 | ACS Med Chem Lett (2023) 14: 425-431 [PMID:37077388] |
| ChEMBL | Partial agonist activity at PPARgamma (unknown origin) assessed as increase in fluorescein labeled PRIP/RAP250 coactivator peptide requirement by Lanthascreen TR-FRET assay | B | 5.17 | pEC50 | 6700 | nM | EC50 | J Nat Prod (2022) 85: 2804-2816 [PMID:36475432] |
| ChEMBL | Agonist activity at GST-tagged PPAR-gamma ligand binding domain (unknown origin) assessed as recruitment of fluorescein-labeled SRC3 coactivator peptide by LanthaScreen TR-FRET Coactivator assay | B | 5.46 | pEC50 | 3500 | nM | EC50 | J Nat Prod (2023) 86: 138-148 [PMID:36529937] |
| ChEMBL | Agonist activity at GST-tagged PPAR-gamma ligand binding domain (unknown origin) assessed as recruitment of fluorescein-labeled SRC1 coactivator peptide by LanthaScreen TR-FRET Coactivator assay | B | 5.48 | pEC50 | 3300 | nM | EC50 | J Nat Prod (2023) 86: 138-148 [PMID:36529937] |
| 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 | J Med Chem (2011) 54: 4219-4233 [PMID:21557540] |
| 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 | 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 | 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 GST-tagged PPAR-gamma ligand binding domain (unknown origin) assessed as recruitment of fluorescein-labeled PRIP/RAP250 coactivator peptide by LanthaScreen TR-FRET Coactivator assay | B | 6.05 | pEC50 | 900 | nM | EC50 | J Nat Prod (2023) 86: 138-148 [PMID:36529937] |
| 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 | 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 | 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 | 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 PPAR-gamma in human BMMSC cells assessed as induction of adiponectin production in presence of IDX adipogenic induction medium and measured on day 5 by ELISA | B | 6.41 | pEC50 | 390 | nM | EC50 | Eur J Med Chem (2020) 187: 111969-111969 [PMID:31865018] |
| 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 | Agonist activity at PPARgamma in human BMMSC cells assessed as promotion of adiponectin secretion by measuring increase in adiponectin level in presence of IDX medium by ELISA | B | 6.7 | pEC50 | 200 | nM | EC50 | J Nat Prod (2023) 86: 138-148 [PMID:36529937] |
| 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 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]
