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Assay Detail

CHEMBL996935

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

Binding
Inhibition of CYP26A1 in human MCF7 cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type MCF7
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Novel azolyl-(phenylmethyl)]aryl/heteroarylamines: potent CYP26 inhibitors and enhancers of all-trans retinoic acid activity in neuroblastoma cells.
Gomaa MS, Armstrong JL, Bobillon B, Veal GJ, Brancale A, Redfern CP, Simons C.
Bioorg Med Chem (2008) 16 : 8301 -8313
PubMed 18722776 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.65 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL224305 1 8.30
CHEMBL518482 1 6.30
CHEMBL518642 1 6.05
CHEMBL517904 1 6.00
CHEMBL460780 1 5.82
CHEMBL462468 1 5.60
CHEMBL360771 1 5.48
CHEMBL517109 1 5.35
CHEMBL450523 1 5.30
CHEMBL459925 1 5.30
CHEMBL460357 1 5.16
CHEMBL389433 LIAROZOLE 2.0 1 5.16
CHEMBL460130 1 4.82
CHEMBL449460 1 4.46
CHEMBL461860 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL224305 IC50 = 5.0 nM 8.30
CHEMBL518482 IC50 = 500.0 nM 6.30
CHEMBL518642 IC50 = 900.0 nM 6.05
CHEMBL517904 IC50 = 1000.0 nM 6.00
CHEMBL460780 IC50 = 1500.0 nM 5.82
CHEMBL462468 IC50 = 2500.0 nM 5.60
CHEMBL360771 IC50 = 3300.0 nM 5.48
CHEMBL517109 IC50 = 4500.0 nM 5.35
CHEMBL450523 IC50 = 5000.0 nM 5.30
CHEMBL459925 IC50 = 5000.0 nM 5.30
CHEMBL460357 IC50 = 7000.0 nM 5.16
CHEMBL389433 LIAROZOLE IC50 = 7000.0 nM 5.16
CHEMBL460130 IC50 = 15000.0 nM 4.82
CHEMBL449460 IC50 = 35000.0 nM 4.46
CHEMBL461860 IC50 > 50000.0 nM -