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Assay Detail

CHEMBL5368326

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

Binding
Agonist activity at PXR (unknown origin) by cellular reporter assay
11
Total Activities
11
Compounds Tested
2
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

GNE-235: A Lead Compound Selective for the Second Bromodomain of PBRM1.
Cochran AG, Flynn M.
J Med Chem (2023) 66 : 13116 -13134
PubMed 37702400 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.72 6.85
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5409404 1 6.85
CHEMBL5406315 1 6.70
CHEMBL5401472 1 6.07
CHEMBL5415396 1 5.38
CHEMBL5428009 1 5.32
CHEMBL5441040 1 5.06
CHEMBL5426305 1 4.66
CHEMBL5421138 1 -
CHEMBL5431005 1 -
CHEMBL3752911 1 -
CHEMBL5207330 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5409404 EC50 = 140.0 nM 6.85
CHEMBL5406315 EC50 = 200.0 nM 6.70
CHEMBL5401472 EC50 = 850.0 nM 6.07
CHEMBL5415396 EC50 = 4200.0 nM 5.38
CHEMBL5428009 EC50 = 4800.0 nM 5.32
CHEMBL5441040 EC50 = 8700.0 nM 5.06
CHEMBL5426305 EC50 = 22000.0 nM 4.66
CHEMBL5421138 EC50 > 50000.0 nM -
CHEMBL5431005 EC50 > 50000.0 nM -
CHEMBL3752911 EC50 > 20000.0 nM -
CHEMBL5207330 Activity - -