ChEMBL ligand: CHEMBL3598140
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449] There should be some charts here, you may need to enable JavaScript!
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
RAR-related orphan receptor-γ/Nuclear receptor ROR-gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741186] [GtoPdb: 600] [UniProtKB: P51449]
ChEMBL	Inhibition of RORgammat (unknown origin)	B	6.37	pIC50	425	nM	IC50	Eur J Med Chem (2023) 247: 115039-115039 [PMID:36566711]
ChEMBL	Allosteric inhibition of yeast GAL4 DNA domain-fused RORgammat LBD (97 to 518 residues) (unknown origin) expressed in HEK293T cells after 20 to 22 hrs by steady-glo luciferase assay	B	6.9	pIC50	127	nM	IC50	ACS Med Chem Lett (2020) 11: 114-119 [PMID:32071676]
ChEMBL	Inhibition of RORgammat in human PBMC by IL17A assay	B	7.4	pIC50	40	nM	IC50	ACS Med Chem Lett (2020) 11: 1810-1819 [PMID:33062158]
ChEMBL	Displacement of Alexa647-labeled MRL-87 from human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) measured after 30 mins by TR-FRET assay	B	7.76	pIC50	17.3	nM	IC50	J Med Chem (2020) 63: 241-259 [PMID:31821760]
ChEMBL	Allosteric inverse agonist activity at recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment incubated for 60 mins by TR-FRET assay	B	7.77	pIC50	17	nM	IC50	ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
ChEMBL	Allosteric inverse agonist activity at C-terminal His-tagged RORgammat LBD (265 to 507 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells assessed as N-terminal biotinylated SRC1 box2 coactivator peptide recruitment by TR-FRET assay	B	7.89	pIC50	13	nM	IC50	J Med Chem (2021) 64: 9238-9258 [PMID:34008974]
ChEMBL	Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in absence of RORgamma agonist cholesterol by TR-FRET assay	B	7.9	pIC50	12.7	nM	IC50	J Med Chem (2020) 63: 241-259 [PMID:31821760]
ChEMBL	Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in presence of 0.25 uM RORgamma agonist cholesterol by TR-FRET assay	B	8.03	pIC50	9.4	nM	IC50	J Med Chem (2020) 63: 241-259 [PMID:31821760]
ChEMBL	Inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins by TR-FRET assay	B	8.11	pIC50	7.8	nM	IC50	J Med Chem (2020) 63: 241-259 [PMID:31821760]
ChEMBL	Competitive inverse agonist activity at human N-terminal His6-tagged RORgammat LBD (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as inhibition of N-terminal biotinylated co-activator SRC1 box2 peptide recruitment measured after 30 mins in presence of 1 uM RORgamma agonist cholesterol by TR-FRET assay	B	8.11	pIC50	7.8	nM	IC50	J Med Chem (2020) 63: 241-259 [PMID:31821760]
ChEMBL	Displacement of Alexa flour647-labeled MRL-871 from RORgammat LBD (265 to 507 residues) (unknown origin) expressed in Escherichia coli BL21(DE3) cells by TR-FRET assay	B	8.15	pIC50	7	nM	IC50	J Med Chem (2021) 64: 9238-9258 [PMID:34008974]
ChEMBL	Inverse agonist activity at His6-tagged human RORgammat LBD expressed in Escherichia coli BL21(DE3) assessed as decrease in SRC-1 recruitment using Biotin-SPSSHSSLTERHKILHRLLQEGSP as substrate incubated for 15 mins by TRET assay	B	8.15	pIC50	7	nM	IC50	Eur J Med Chem (2023) 247: 115039-115039 [PMID:36566711]
ChEMBL	Allosteric inverse agonist at His tagged RORgammat (unknown origin) expressed in Escherichia coli BL21(DE3) cells incubated for 2 hrs by TR-FRET assay	B	8.15	pIC50	7	nM	IC50	J Med Chem (2021) 64: 10519-10536 [PMID:34264059]
ChEMBL	Inhibition of human GAL4-fused RORgammat LBD transfected in Escherichia coli BL21(DE3) cell measured after 16 hrs by HTRF assay	B	8.21	pIC50	6.1	nM	IC50	J Med Chem (2018) 61: 10976-10995 [PMID:30010338]
ChEMBL	Inhibition of His6-tagged human RORgammat LBD expressed in Escherichia coli BL21(DE3) cells after 16 hrs by HTRF assay	B	8.22	pIC50	6	nM	IC50	ACS Med Chem Lett (2020) 11: 1810-1819 [PMID:33062158]
ChEMBL	Allosteric inverse agonist activity at 2-chloro-N-(2,6-dimethylphenyl)-5-nitrobenzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-N-(2,6-dimethylphenyl)-5-nitrobenzamide incubated for 60 mins by TR-FRET assay	B	8.26	pIC50	5.5	nM	IC50	ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
ChEMBL	Allosteric inverse agonist activity at 2-chloro-5-nitro-N-o-tolylbenzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-5-nitro-N-o-tolylbenzamide incubated for 60 mins by TR-FRET assay	B	8.26	pIC50	5.5	nM	IC50	ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
ChEMBL	Allosteric inhibition of recombinant His6-tagged RORgammat LBD (unknown origin) expressed in Escherichia coli BL21(DE3) assessed as inhibition of biotin-labelled SRC-1 peptide recruitment preincubated for 15 mins followed by biotin-labelled SRC-1 peptide addition and measured after overnight incubation by TR-FRET assay	B	8.7	pIC50	2	nM	IC50	ACS Med Chem Lett (2020) 11: 114-119 [PMID:32071676]
ChEMBL	Allosteric inverse agonist activity at 2-chloro-5-nitro-N-(2-(trifluoromethyl)phenyl)benzamide-ligated recombinant human N-terminal His6-tagged RORgammat ligand binding domain (265 to 518 residues) expressed in Escherichia coli BL21 (DE3) assessed as reduction in coactivator, N-terminal biotinylated SRC-1 box2 peptide recruitment in presence of 2-chloro-5-nitro-N-(2-(trifluoromethyl)phenyl)benzamide incubated for 60 mins by TR-FRET assay	B	8.89	pIC50	1.3	nM	IC50	ACS Med Chem Lett (2021) 12: 631-639 [PMID:33854703]
ChEMBL	Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486) expressed in bacterial expression system assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis	B	7.8	pEC50	16	nM	EC50	Bioorg Med Chem Lett (2015) 25: 2907-2912 [PMID:26048793]
ChEMBL	Inverse agonist activity at RORC (unknown origin)	B	7.8	pEC50	16	nM	EC50	Eur J Med Chem (2022) 228: 113962-113962 [PMID:34776280]
GtoPdb	Inverse agonist activity at N-terminal 6xHis-tagged human RORc ligand binding domain (241 to 486); assessed as inhibition of SRC1 co-activator peptide recruitment after 3 hrs by TR-FRET analysis	-	7.8	pEC50	16	nM	EC50	Bioorg Med Chem Lett (2015) 25: 2907-12 [PMID:26048793]
ChEMBL	Partial agonist activity at RORgammat (unknown origin) assessed as increase in FITC-labeled SRC1B2 peptide recruitment by HTRF assay	B	8.33	pEC50	4.7	nM	EC50	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
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 PPARgamma LBD (unknown origin) assessed as dissociation constant followed by heating for 3 mins by Bradford assay	B	6.6	pKd	250	nM	Kd	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
ChEMBL	Binding affinity to PPARgamma LBD (unknown origin) assessed as inhibition constant in presence of 1 uM of rosiglitazone by HTRF based competitive binding assay	B	6.64	pKi	230	nM	Ki	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
ChEMBL	Binding affinity to PPARgamma LBD (unknown origin) assessed as inhibition constant by HTRF based competitive binding assay	B	6.68	pKi	210	nM	Ki	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
ChEMBL	Binding affinity to PPARgamma LBD (unknown origin) assessed as inhibition constant in presence of 10 nM of rosiglitazone by HTRF based competitive binding assay	B	6.8	pKi	160	nM	Ki	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
ChEMBL	Inverse agonist activity at His6-tagged PPARgamma LBD (unknown origin) assessed as N-terminal biotinylated PGC1a coactivator peptide recruitment in presence of rosiglitazone by TR-FRET assay	B	5.2	pIC50	6300	nM	IC50	J Med Chem (2021) 64: 9238-9258 [PMID:34008974]
ChEMBL	Displacement of fluormone PPARgamma green from GST-tagged human PPARgamma-LBD after 2 hrs by fluorescence polarization assay	B	6.89	pIC50	130	nM	IC50	Bioorg Med Chem Lett (2015) 25: 2907-2912 [PMID:26048793]
ChEMBL	Inverse agonist activity at human PPARgamma	B	6.89	pIC50	130	nM	IC50	Eur J Med Chem (2022) 228: 113962-113962 [PMID:34776280]
ChEMBL	Binding affinity to PPARgamma LBD (unknown origin) using FITC-labeled PGC-1alpha peptide in presence of 1 uM of rosiglitazone by HTRF based competitive binding assay	B	5.04	pEC50	9100	nM	EC50	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
ChEMBL	Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in FITC-labeled PGC-1alpha coactivator peptide recruitment in presence of GW9662 by HTRF assay	B	5.89	pEC50	1300	nM	EC50	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
ChEMBL	Inverse agonist activity at His6-tagged PPARgamma LBD (unknown origin) assessed as N-terminal biotinylated PGC1a coactivator peptide recruitment by TR-FRET assay	B	6.47	pEC50	340	nM	EC50	J Med Chem (2021) 64: 9238-9258 [PMID:34008974]
ChEMBL	Binding affinity to PPARgamma LBD (unknown origin) using FITC-labeled PGC-1alpha peptide in presence of 10 nM of rosiglitazone by HTRF based competitive binding assay	B	6.64	pEC50	230	nM	EC50	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]
ChEMBL	Partial agonist activity at PPARgamma LBD (unknown origin) assessed as increase in FITC-labeled PGC-1alpha coactivator peptide recruitment by HTRF assay	B	6.77	pEC50	170	nM	EC50	Bioorg Med Chem (2022) 68: 116877-116877 [PMID:35714534]

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]