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Assay Detail

CHEMBL3106083

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

Binding
Displacement of 25-[26,27-3H]hydroxycholesterol from RORgammat receptor ligand binding domain (unknown origin) after 60 mins
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

Discovery of novel N-(5-(arylcarbonyl)thiazol-2-yl)amides and N-(5-(arylcarbonyl)thiophen-2-yl)amides as potent RORγt inhibitors.
Wang Y, Cai W, Zhang G, Yang T, Liu Q, Cheng Y, Zhou L, Ma Y, Cheng Z, Lu S, Zhao YG, Zhang W, Xiang Z, Wang S, Yang L, Wu Q, Orband-Miller LA, Xu Y, Zhang J, Gao R, Huxdorf M, Xiang JN, Zhong Z, Elliott JD, Leung S, Lin X.
Bioorg Med Chem (2014) 22 : 692 -702
PubMed 24388993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.23 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3105692 1 7.60
CHEMBL3105671 1 7.50
CHEMBL3105681 1 7.40
CHEMBL3105815 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3105692 Ki = 25.12 nM 7.60
CHEMBL3105671 Ki = 31.62 nM 7.50
CHEMBL3105681 Ki = 39.81 nM 7.40
CHEMBL3105815 Ki = 398.11 nM 6.40