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Assay Detail

CHEMBL4701583

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

Binding
Inverse agonist activity of PXR (unknown origin)
1
Total Activities
1
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 subfamily 1 group I member 2 (CHEMBL3401)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Tricyclic sulfones as potent, selective and efficacious RORγt inverse agonists - Exploring C6 and C8 SAR using late-stage functionalization.
Shi Q,Xiao Z,Yang MG,Marcoux D,Cherney RJ,Yip S,Li P,Wu DR,Weigelt CA,Sack J,Khan J,Ruzanov M,Wang J,Yarde M,Ellen Cvijic M,Li S,Shuster DJ,Xie J,Sherry T,Obermeier M,Fura A,Stefanski K,Cornelius G,Chacko S,Shu YZ,Khandelwal P,Hynes J,Tino JA,Salter-Cid L,Denton R,Zhao Q,Dhar TGM
Bioorg Med Chem Lett (2020) 30 : 127521 -127521
PubMed 32882417 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 5.04 5.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4763134 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4763134 EC50 = 9200.0 nM 5.04