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Assay Detail

CHEMBL3097485

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

Binding
Inverse agonist activity at GAL4-fused human RORa expressed in HEK293T cells assessed as suppression of basal transcriptional activity after 20 hrs by dual-glo luciferase reporter gene assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Nuclear receptor ROR-alpha (CHEMBL5868)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-based design of substituted hexafluoroisopropanol-arylsulfonamides as modulators of RORc.
Fauber BP, de Leon Boenig G, Burton B, Eidenschenk C, Everett C, Gobbi A, Hymowitz SG, Johnson AR, Liimatta M, Lockey P, Norman M, Ouyang W, René O, Wong H.
Bioorg Med Chem Lett (2013) 23 : 6604 -6609
PubMed 24239186 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.25 5.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2326845 1 5.30
CHEMBL62136 T091317 1 5.30
CHEMBL3094369 1 5.22
CHEMBL3094367 1 5.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2326845 EC50 = 5000.0 nM 5.30
CHEMBL62136 T091317 EC50 = 5000.0 nM 5.30
CHEMBL3094369 EC50 = 6000.0 nM 5.22
CHEMBL3094367 EC50 = 7000.0 nM 5.16