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Assay Detail

CHEMBL916378

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Functional
Inhibition of ATRA-induced CYP26 in human T47D cells assessed as ATRA metabolism using [11.12-3H]-ATRA
18
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type T47D
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 26A1 (CHEMBL5141)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel retinoic acid metabolism blocking agents endowed with multiple biological activities are efficient growth inhibitors of human breast and prostate cancer cells in vitro and a human breast tumor xenograft in nude mice.
Patel JB, Huynh CK, Handratta VD, Gediya LK, Brodie AM, Goloubeva OG, Clement OO, Nanne IP, Soprano DR, Njar VC.
J Med Chem (2004) 47 : 6716 -6729
PubMed 15615521 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 6.82 8.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL57765 1 8.20
CHEMBL223072 1 8.00
CHEMBL190837 1 7.62
CHEMBL224828 1 6.67
CHEMBL225621 2 5.22
CHEMBL431135 1 -
CHEMBL224080 1 -
CHEMBL7301 FENRETINIDE 3.0 1 -
CHEMBL157101 KETOCONAZOLE 4.0 1 -
CHEMBL225121 1 -
CHEMBL225429 1 -
CHEMBL387639 1 -
CHEMBL224995 1 -
CHEMBL388283 1 -
CHEMBL388064 1 -
CHEMBL53449 1 -
CHEMBL417769 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL57765 IC50 = 6.3 nM 8.20
CHEMBL223072 IC50 = 10.0 nM 8.00
CHEMBL190837 IC50 = 24.0 nM 7.62
CHEMBL224828 IC50 = 215.0 nM 6.67
CHEMBL225621 IC50 = 6000.0 nM 5.22
CHEMBL225621 IC50 = 6000.0 nM 5.22
CHEMBL431135 IC50 - -
CHEMBL224080 IC50 - -
CHEMBL7301 FENRETINIDE IC50 - -
CHEMBL157101 KETOCONAZOLE IC50 - -
CHEMBL225121 IC50 - -
CHEMBL225429 IC50 - -
CHEMBL387639 IC50 - -
CHEMBL224995 IC50 - -
CHEMBL388283 IC50 - -
CHEMBL388064 IC50 - -
CHEMBL53449 IC50 - -
CHEMBL417769 IC50 - -