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Assay Detail

CHEMBL5325805

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

ADMET
Inhibition of CYP1B1 (unknown origin) expressed in HEK293-T-REx cells co-expressing POR incubated for 1 hr by resorufin dye based plate reader analysis
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Homo sapiens
Cell Type HEK293-T-REx
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Cytochrome P450 1B1 (CHEMBL4878)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of Cytochrome P450 1B1 Inhibitors <i>via</i> a Scaffold-Hopping Approach.
Hachey AC, Fenton AD, Heidary DK, Glazer EC.
J Med Chem (2023) 66 : 398 -412
PubMed 36520541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 7.83 10.37

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3421639 1 10.37
CHEMBL5394220 1 9.70
CHEMBL5403545 1 9.51
CHEMBL5412548 1 9.00
CHEMBL5406710 1 8.30
CHEMBL5405212 1 8.30
CHEMBL5401046 1 8.22
CHEMBL5418617 1 7.72
CHEMBL5425709 1 7.60
CHEMBL5395150 1 7.42
CHEMBL5406117 1 7.27
CHEMBL46909 1 7.18
CHEMBL5438759 1 7.00
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 6.85
CHEMBL4218514 1 6.43
CHEMBL5406218 1 6.22
CHEMBL380753 1 5.99
CHEMBL5429178 1 -
CHEMBL5396198 1 -
CHEMBL5426573 1 -
CHEMBL5406721 1 -
CHEMBL5401832 1 -
CHEMBL5406156 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3421639 IC50 = 0.043 nM 10.37
CHEMBL5394220 IC50 = 0.2 nM 9.70
CHEMBL5403545 IC50 = 0.31 nM 9.51
CHEMBL5412548 IC50 = 1.0 nM 9.00
CHEMBL5406710 IC50 = 5.0 nM 8.30
CHEMBL5405212 IC50 = 5.0 nM 8.30
CHEMBL5401046 IC50 = 6.0 nM 8.22
CHEMBL5418617 IC50 = 19.0 nM 7.72
CHEMBL5425709 IC50 = 25.0 nM 7.60
CHEMBL5395150 IC50 = 38.0 nM 7.42
CHEMBL5406117 IC50 = 54.0 nM 7.27
CHEMBL46909 IC50 = 66.0 nM 7.18
CHEMBL5438759 IC50 = 100.0 nM 7.00
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 140.0 nM 6.85
CHEMBL4218514 IC50 = 370.0 nM 6.43
CHEMBL5406218 IC50 = 600.0 nM 6.22
CHEMBL380753 IC50 = 1020.0 nM 5.99
CHEMBL5429178 IC50 > 10000.0 nM -
CHEMBL5396198 IC50 > 10000.0 nM -
CHEMBL5426573 IC50 > 10000.0 nM -
CHEMBL5406721 IC50 > 10000.0 nM -
CHEMBL5401832 IC50 > 10000.0 nM -
CHEMBL5406156 IC50 > 10000.0 nM -