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Assay Detail

CHEMBL3385309

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

Binding
Inverse agonist activity at RORgammaT (unknown origin) by M1H assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.
Gege C, Schlüter T, Hoffmann T.
Bioorg Med Chem Lett (2014) 24 : 5265 -5267
PubMed 25305688 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.23 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3105681 1 8.10
CHEMBL3105674 1 7.80
CHEMBL38 TRETINOIN 4.0 1 6.70
CHEMBL62136 T091317 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3105681 IC50 = 7.943 nM 8.10
CHEMBL3105674 IC50 = 15.85 nM 7.80
CHEMBL38 TRETINOIN IC50 = 199.53 nM 6.70
CHEMBL62136 T091317 IC50 = 501.19 nM 6.30