ChEMBL ligand: CHEMBL3137304 (Dagrocorat, PF-00251802, PF-0251802, PF-802)
Glucocorticoid receptor in Human [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150] 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
Glucocorticoid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2034] [GtoPdb: 625] [UniProtKB: P04150]
ChEMBL	Transrepression of GR in human whole blood assessed as inhibition of LPS-induced TNF-alpha release preincubated for 45 mins followed by LPS addition after 18 hrs by AlphaLISA method	B	7.46	pIC50	35	nM	IC50	J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL	Antagonist activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of dexamethasone induced transactivation incubated for 24 hrs by beta-galactosidase reporter gene assay	B	8.05	pIC50	8.9	nM	IC50	J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL	Displacement of fluormone RED from human full length glucocorticoid receptor after 4 hrs by fluorescence polarization assay	B	8.14	pIC50	<7.2	nM	IC50	J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
GtoPdb	Measured in a glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay.	-	8.88	pIC50	1.31	nM	IC50	US8901310. Tricyclic compounds, compositions, and methods (2014)
ChEMBL	Fluorescence Polarization Ligand Binding Assay: The glucocorticoid receptor fluorescence polarization ligand binding (GRFP) assay is used to evaluate direct binding of testing compounds to full-length glucocorticoid (GR) protein. Reagents for this assay are purchased from Invitrogen in a test kit. A fluorescent labeled GR ligand is used as a fluorescent tracer and test compounds compete with the fluorescent tracer for GR binding. The change in polarization value in the presence of test compounds is due to binding of test compounds to GR and is used to determine IC50 and relative binding affinity of test compounds for GR.	B	8.88	pIC50	1.31	nM	IC50	US-8901310-B2. Tricyclic compounds, compositions, and methods (2014)
ChEMBL	Transrepression activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells assessed as inhibition of PMA-stimulated gene expression incubated for 24 hrs by beta-galactosidase reporter gene assay	B	9.16	pIC50	0.69	nM	IC50	J Med Chem (2018) 61: 1785-1799 [PMID:29424542]
ChEMBL	Transactivation activity at glucocorticoid receptor (unknown origin) expressed in human ChaGoK1 cells incubated for 24 hrs by beta-galactosidase reporter gene assay	B	8.32	pEC50	4.8	nM	EC50	J Med Chem (2018) 61: 1785-1799 [PMID:29424542]

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]