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Assay Detail

CHEMBL975042

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

Binding
Protection of human pregnane X receptor against proteolytic digestion in presence of trypsin
4
Total Activities
4
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

N-1H-benzimidazol-5-ylbenzenesulfonamide derivatives as potent hPXR agonists.
Benod C, Subra G, Nahoum V, Mallavialle A, Guichou JF, Milhau J, Roblés S, Bourguet W, Pascussi JM, Balaguer P, Chavanieu A.
Bioorg Med Chem (2008) 16 : 3537 -3549
PubMed 18304819 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 7.27 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL463678 1 8.10
CHEMBL464497 1 8.09
CHEMBL513946 1 6.80
CHEMBL457271 1 6.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL463678 EC50 = 8.04 nM 8.10
CHEMBL464497 EC50 = 8.05 nM 8.09
CHEMBL513946 EC50 = 157.0 nM 6.80
CHEMBL457271 EC50 = 809.0 nM 6.09