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Assay Detail

CHEMBL995591

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

Functional
Agonist activity at human PXR
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

4-Methyl-5-phenyl triazoles as selective inhibitors of 11beta-hydroxysteroid dehydrogenase type I.
Zhu Y, Olson SH, Hermanowski-Vosatka A, Mundt S, Shah K, Springer M, Thieringer R, Wright S, Xiao J, Zokian H, Balkovec JM.
Bioorg Med Chem Lett (2008) 18 : 3405 -3411
PubMed 18440811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 5.44 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL496307 1 6.16
CHEMBL522572 1 5.89
CHEMBL496495 1 5.77
CHEMBL494638 1 5.77
CHEMBL497121 1 5.62
CHEMBL496714 1 5.50
CHEMBL522701 1 5.44
CHEMBL522066 1 5.11
CHEMBL497554 1 5.10
CHEMBL523414 1 4.92
CHEMBL521536 1 4.60
CHEMBL495889 1 -
CHEMBL497122 1 -
CHEMBL497555 1 -
CHEMBL525360 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL496307 EC50 = 700.0 nM 6.16
CHEMBL522572 EC50 = 1300.0 nM 5.89
CHEMBL496495 EC50 = 1700.0 nM 5.77
CHEMBL494638 EC50 = 1700.0 nM 5.77
CHEMBL497121 EC50 = 2400.0 nM 5.62
CHEMBL496714 EC50 = 3200.0 nM 5.50
CHEMBL522701 EC50 = 3600.0 nM 5.44
CHEMBL522066 EC50 = 7700.0 nM 5.11
CHEMBL497554 EC50 = 7900.0 nM 5.10
CHEMBL523414 EC50 = 12000.0 nM 4.92
CHEMBL521536 EC50 = 25000.0 nM 4.60
CHEMBL495889 EC50 > 25000.0 nM -
CHEMBL497122 EC50 > 25000.0 nM -
CHEMBL497555 EC50 > 25000.0 nM -
CHEMBL525360 EC50 > 25000.0 nM -