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Assay Detail

CHEMBL3242033

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

Binding
Antagonist activity at full-length RORgamma (unknown origin) expressed in 293T cells after 24 hrs by luciferase reporter gene assay
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type 293T
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Discovery of 2-oxo-1,2-dihydrobenzo[cd]indole-6-sulfonamide derivatives as new RORγ inhibitors using virtual screening, synthesis and biological evaluation.
Zhang Y, Xue X, Jin X, Song Y, Li J, Luo X, Song M, Yan W, Song H, Xu Y.
Eur J Med Chem (2014) 78 : 431 -441
PubMed 24704616 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.32 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3234259 1 7.70
CHEMBL3234255 1 7.40
CHEMBL3234251 1 7.30
CHEMBL1494527 1 7.10
CHEMBL3234252 1 7.05
CHEMBL3234256 1 7.05
CHEMBL3234030 1 6.82
CHEMBL3234246 1 6.82
CHEMBL3234248 1 6.75
CHEMBL3234247 1 6.70
CHEMBL3234241 1 6.54
CHEMBL3234262 1 6.39
CHEMBL3234240 1 6.39
CHEMBL2137199 1 6.38
CHEMBL3234034 1 6.26
CHEMBL3234253 1 6.23
CHEMBL169 URSOLIC ACID 2.0 1 5.97
CHEMBL3234263 1 5.97
CHEMBL3234025 1 5.87
CHEMBL3234249 1 5.47
CHEMBL62136 T091317 1 5.46
CHEMBL3234285 1 5.29
CHEMBL3234024 1 5.12
CHEMBL3234257 1 5.00
CHEMBL3234027 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3234259 IC50 = 20.0 nM 7.70
CHEMBL3234255 IC50 = 40.0 nM 7.40
CHEMBL3234251 IC50 = 50.0 nM 7.30
CHEMBL1494527 IC50 = 80.0 nM 7.10
CHEMBL3234252 IC50 = 90.0 nM 7.05
CHEMBL3234256 IC50 = 90.0 nM 7.05
CHEMBL3234030 IC50 = 150.0 nM 6.82
CHEMBL3234246 IC50 = 150.0 nM 6.82
CHEMBL3234248 IC50 = 180.0 nM 6.75
CHEMBL3234247 IC50 = 200.0 nM 6.70
CHEMBL3234241 IC50 = 290.0 nM 6.54
CHEMBL3234262 IC50 = 410.0 nM 6.39
CHEMBL3234240 IC50 = 410.0 nM 6.39
CHEMBL2137199 IC50 = 420.0 nM 6.38
CHEMBL3234034 IC50 = 550.0 nM 6.26
CHEMBL3234253 IC50 = 590.0 nM 6.23
CHEMBL169 URSOLIC ACID IC50 = 1060.0 nM 5.97
CHEMBL3234263 IC50 = 1080.0 nM 5.97
CHEMBL3234025 IC50 = 1350.0 nM 5.87
CHEMBL3234249 IC50 = 3390.0 nM 5.47
CHEMBL62136 T091317 IC50 = 3500.0 nM 5.46
CHEMBL3234285 IC50 = 5150.0 nM 5.29
CHEMBL3234024 IC50 = 7560.0 nM 5.12
CHEMBL3234257 IC50 = 9980.0 nM 5.00
CHEMBL3234027 IC50 = 12760.0 nM 4.89