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Assay Detail

CHEMBL3106085

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

Binding
Inhibition of RORgammat receptor ligand binding domain in mouse spleen CD4+ T cells assessed as inhibition of IL-17 production after 3 days by ELISA
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Spleen
Cell Type T-cell
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

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
IC50 20 7.07 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3105690 1 8.00
CHEMBL3105670 1 8.00
CHEMBL3105672 1 7.90
CHEMBL3105671 1 7.80
CHEMBL3105669 1 7.60
CHEMBL3105692 1 7.60
CHEMBL3105691 1 7.60
CHEMBL3105686 1 7.30
CHEMBL3105676 1 6.90
CHEMBL3105678 1 6.80
CHEMBL3105685 1 6.70
CHEMBL3105681 1 6.70
CHEMBL3105682 1 6.60
CHEMBL3105674 1 6.50
CHEMBL3105684 1 6.50
CHEMBL3105675 1 6.40
CHEMBL3105683 1 6.20
CHEMBL3105677 1 6.10
CHEMBL3105679 1 -
CHEMBL3105680 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3105690 IC50 = 10.0 nM 8.00
CHEMBL3105670 IC50 = 10.0 nM 8.00
CHEMBL3105672 IC50 = 12.59 nM 7.90
CHEMBL3105671 IC50 = 15.85 nM 7.80
CHEMBL3105669 IC50 = 25.12 nM 7.60
CHEMBL3105692 IC50 = 25.12 nM 7.60
CHEMBL3105691 IC50 = 25.12 nM 7.60
CHEMBL3105686 IC50 = 50.12 nM 7.30
CHEMBL3105676 IC50 = 125.89 nM 6.90
CHEMBL3105678 IC50 = 158.49 nM 6.80
CHEMBL3105685 IC50 = 199.53 nM 6.70
CHEMBL3105681 IC50 = 199.53 nM 6.70
CHEMBL3105682 IC50 = 251.19 nM 6.60
CHEMBL3105674 IC50 = 316.23 nM 6.50
CHEMBL3105684 IC50 = 316.23 nM 6.50
CHEMBL3105675 IC50 = 398.11 nM 6.40
CHEMBL3105683 IC50 = 630.96 nM 6.20
CHEMBL3105677 IC50 = 794.33 nM 6.10
CHEMBL3105679 IC50 > 7943.28 nM -
CHEMBL3105680 IC50 > 10000.0 nM -