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Assay Detail

CHEMBL4820816

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 CD3/CD28/IL-1/IL-23-induced IL-17A production measured after 24 hrs by AlphaLISA assay
2
Total Activities
2
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

Tricyclic-Carbocyclic RORγt Inverse Agonists-Discovery of BMS-986313.
Yang MG, Beaudoin-Bertrand M, Xiao Z, Marcoux D, Weigelt CA, Yip S, Wu DR, Ruzanov M, Sack JS, Wang J, Yarde M, Li S, Shuster DJ, Xie JH, Sherry T, Obermeier MT, Fura A, Stefanski K, Cornelius G, Khandelwal P, Karmakar A, Basha M, Babu V, Gupta AK, Mathur A, Salter-Cid L, Denton R, Zhao Q, Dhar TGM.
J Med Chem (2021) 64 : 2714 -2724
PubMed 33591748 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 8.27 8.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761772 1 8.57
CHEMBL4871326 1 7.96

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761772 EC50 = 2.7 nM 8.57
CHEMBL4871326 EC50 = 11.0 nM 7.96