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	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	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	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-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 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 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]
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]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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 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]