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Assay Detail

CHEMBL3607384

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

Binding
Inverse agonist activity at RORgammat in mouse Th17 cells assessed as inhibition of IL-17 production after 3 days by ELISA
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type Th17
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Nuclear receptor ROR-gamma (CHEMBL1293231)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of N-(4-aryl-5-aryloxy-thiazol-2-yl)-amides as potent RORγt inverse agonists.
Wang Y, Yang T, Liu Q, Ma Y, Yang L, Zhou L, Xiang Z, Cheng Z, Lu S, Orband-Miller LA, Zhang W, Wu Q, Zhang K, Li Y, Xiang JN, Elliott JD, Leung S, Ren F, Lin X.
Bioorg Med Chem (2015) 23 : 5293 -5302
PubMed 26277758 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.10 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3314014 1 6.80
CHEMBL3605083 1 6.60
CHEMBL3605090 1 6.60
CHEMBL3605092 1 6.40
CHEMBL3605085 1 6.20
CHEMBL3605082 1 6.00
CHEMBL3605081 1 5.80
CHEMBL3605084 1 5.80
CHEMBL3605088 1 5.80
CHEMBL3605089 1 5.70
CHEMBL3605087 1 5.40
CHEMBL3605086 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3314014 IC50 = 158.49 nM 6.80
CHEMBL3605083 IC50 = 251.19 nM 6.60
CHEMBL3605090 IC50 = 251.19 nM 6.60
CHEMBL3605092 IC50 = 398.11 nM 6.40
CHEMBL3605085 IC50 = 630.96 nM 6.20
CHEMBL3605082 IC50 = 1000.0 nM 6.00
CHEMBL3605081 IC50 = 1584.89 nM 5.80
CHEMBL3605084 IC50 = 1584.89 nM 5.80
CHEMBL3605088 IC50 = 1584.89 nM 5.80
CHEMBL3605089 IC50 = 1995.26 nM 5.70
CHEMBL3605087 IC50 = 3981.07 nM 5.40
CHEMBL3605086 IC50 > 10000.0 nM -