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Assay Detail

CHEMBL3369173

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Agonist activity at RoRc-LBD (unknown origin) expressed in HEK293 cells assessed as transcriptional activity by GAL4 reporter assay
16
Total Activities
16
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor ROR-gamma (CHEMBL1741186)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Modulators of the nuclear receptor retinoic acid receptor-related orphan receptor-γ (RORγ or RORc).
Fauber BP, Magnuson S.
J Med Chem (2014) 57 : 5871 -5892
PubMed 24502334 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 13 7.49 9.00
IC50 3 4.82 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3314002 1 9.00
CHEMBL3314001 1 8.00
CHEMBL3313999 1 7.89
CHEMBL3314000 1 7.80
CHEMBL3313998 1 7.40
CHEMBL2137199 1 6.50
CHEMBL3218917 1 5.82
CHEMBL3314005 1 4.82
CHEMBL3314004 1 4.82
CHEMBL3314003 1 4.82
CHEMBL3313997 1 -
CHEMBL3313996 1 -
CHEMBL3313995 1 -
CHEMBL3355081 1 -
CHEMBL3313993 1 -
CHEMBL3313992 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3314002 EC50 = 1.0 nM 9.00
CHEMBL3314001 EC50 = 10.0 nM 8.00
CHEMBL3313999 EC50 = 13.0 nM 7.89
CHEMBL3314000 EC50 = 16.0 nM 7.80
CHEMBL3313998 EC50 = 40.0 nM 7.40
CHEMBL2137199 EC50 = 320.0 nM 6.50
CHEMBL3218917 EC50 = 1500.0 nM 5.82
CHEMBL3314005 IC50 = 15000.0 nM 4.82
CHEMBL3314004 IC50 = 15000.0 nM 4.82
CHEMBL3314003 IC50 = 15000.0 nM 4.82
CHEMBL3313997 EC50 < 500.0 nM -
CHEMBL3313996 EC50 < 500.0 nM -
CHEMBL3313995 EC50 < 500.0 nM -
CHEMBL3355081 EC50 < 500.0 nM -
CHEMBL3313993 EC50 < 500.0 nM -
CHEMBL3313992 EC50 < 500.0 nM -