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Assay Detail

CHEMBL647916

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

ADMET
Inhibition of Aryl hydrocarbon hydroxylase in phenobarbitone-treated rats
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cytochrome P450 1A1 (CHEMBL2922)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Inhibitors of hepatic mixed-function oxidases. 4. Effects of benzimidazole and related compounds on aryl hydrocarbon hydroxylase activity from phenobarbitone and 3-methylcholanthrene induced rats.
Little PJ, Ryan AJ.
J Med Chem (1982) 25 : 622 -626
PubMed 7097715 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 4.38 4.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158007 1 4.75
CHEMBL347036 PROADIFEN HYDROCHLORIDE -1.0 1 4.66
CHEMBL345675 1 4.62
CHEMBL14145 1 4.48
CHEMBL155867 1 4.09
CHEMBL156313 1 4.08
CHEMBL351132 DIMEDAZOL 1 4.01
CHEMBL306226 BENZIMIDAZOLE -1.0 1 -
CHEMBL156439 1 -
CHEMBL309135 1 -
CHEMBL348508 1 -
CHEMBL156134 1 -
CHEMBL351569 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158007 IC50 = 18000.0 nM 4.75
CHEMBL347036 PROADIFEN HYDROCHLORIDE IC50 = 22000.0 nM 4.66
CHEMBL345675 IC50 = 24000.0 nM 4.62
CHEMBL14145 IC50 = 33000.0 nM 4.48
CHEMBL155867 IC50 = 82000.0 nM 4.09
CHEMBL156313 IC50 = 84000.0 nM 4.08
CHEMBL351132 DIMEDAZOL IC50 = 97000.0 nM 4.01
CHEMBL306226 BENZIMIDAZOLE IC50 = 1100000.0 nM -
CHEMBL156439 IC50 = 110000.0 nM -
CHEMBL309135 IC50 = 670000.0 nM -
CHEMBL348508 IC50 = 480000.0 nM -
CHEMBL156134 IC50 = 170000.0 nM -
CHEMBL351569 IC50 = 630000.0 nM -