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Assay Detail

CHEMBL1743533

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ADMET
Mechanism based inhibition of human cytochrome P450 1A2 measured by phenacetin O-deethylation (POD)
6
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Cytochrome P450 1A2 (CHEMBL3356)
Type SINGLE PROTEIN
Organism Homo sapiens

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 3 4.10 4.18
Kinact 3 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1743359 2 4.18
CHEMBL1164975 2 4.01
CHEMBL93 ZILEUTON 4.0 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1743359 Ki = 66000.0 nM 4.18
CHEMBL1164975 Ki = 98200.0 nM 4.01
CHEMBL93 ZILEUTON Ki = 117000.0 nM -
CHEMBL93 ZILEUTON Kinact = 0.035 min-1 -
CHEMBL1743359 Kinact = 0.012 min-1 -
CHEMBL1164975 Kinact = 0.037 min-1 -