Assay Detail

CHEMBL4618964

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Binding

Inverse agonist activity at RORgammat in mouse whole blood assessed as suppression of Th17 secretion

ChEMBL ↗

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Target

Nuclear receptor ROR-gamma (CHEMBL1293231) ↗

Open DB target context

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Nuclear receptor ROR-gamma (CHEMBL1293231) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Nuclear receptor ROR-gamma

CHEMBL1293231

Anchored from Assay target.

Protein identity Nuclear receptor ROR-gamma

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

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

Target

Nuclear receptor ROR-gamma (CHEMBL1293231) ↗

Type	SINGLE PROTEIN
Organism	Mus musculus

Publication

Discovery of BMS-986251: A Clinically Viable, Potent, and Selective RORγt Inverse Agonist.

Cherney RJ, Cornelius LAM, Srivastava A, Weigelt CA, Marcoux D, Duan JJ, Shi Q, Batt DG, Liu Q, Yip S, Wu DR, Ruzanov M, Sack J, Khan J, Wang J, Yarde M, Cvijic ME, Mathur A, Li S, Shuster D, Khandelwal P, Borowski V, Xie J, Obermeier M, Fura A, Stefanski K, Cornelius G, Tino JA, Macor JE, Salter-Cid L, Denton R, Zhao Q, Carter PH, Dhar TGM.
ACS Med Chem Lett (2020) 11 : 1221 -1227
PubMed 32551004 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
EC50	1	7.96	7.96

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4634542	BMS-986251	1.0	1	7.96

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4634542	BMS-986251	EC50	=	11.0	nM	7.96