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Assay Detail

CHEMBL1925454

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

ADMET
Inhibition of human B-lymphoblastoid cell microsomal CYP1A2 assessed as 7-ethoxyresorufin O-deethylation preincubated for 5 mins with substrate
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of orteronel (TAK-700), a naphthylmethylimidazole derivative, as a highly selective 17,20-lyase inhibitor with potential utility in the treatment of prostate cancer.
Kaku T, Hitaka T, Ojida A, Matsunaga N, Adachi M, Tanaka T, Hara T, Yamaoka M, Kusaka M, Okuda T, Asahi S, Furuya S, Tasaka A.
Bioorg Med Chem (2011) 19 : 6383 -6399
PubMed 21978946 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 4.55 4.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1921976 ORTERONEL 3.0 1 4.55

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1921976 ORTERONEL IC50 = 28000.0 nM 4.55