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Assay Detail

CHEMBL1908258

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

ADMET
Mechanism based inhibition of rat cytochrome P450 CYP1A2 measured by 7-methoxyresorufin O-demethylation (MROD)
8
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cytochrome P450 1A2 (CHEMBL1075125)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Cytochrome p450 enzymes mechanism based inhibitors: common sub-structures and reactivity.
Fontana E, Dansette PM, Poli SM.
Curr Drug Metab (2005) 6 : 413 -454
PubMed 16248836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.98 8.40
kinact 4 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3215311 2 8.40
CHEMBL1908227 2 7.52
CHEMBL374163 2 6.06
CHEMBL1908231 2 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3215311 Ki = 4.0 nM 8.40
CHEMBL1908227 Ki = 30.0 nM 7.52
CHEMBL374163 Ki = 870.0 nM 6.06
CHEMBL1908231 Ki = 1200.0 nM 5.92
CHEMBL374163 kinact = 0.1 min-1 -
CHEMBL1908227 kinact = 0.04 min-1 -
CHEMBL1908231 kinact = 0.3 min-1 -
CHEMBL3215311 kinact = 0.06 min-1 -