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Assay Detail

CHEMBL4334806

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

ADMET
Inhibition of recombinant human CYP1A1 expressed in supersomes using 7-ethoxyresorufin as substrate after 15 mins in presence of NADP+ by EROD assay
21
Total Activities
21
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 1A1 (CHEMBL2231)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of benzochalcone derivatives as selective CYP1B1 inhibitors and anticancer agents.
Dong J, Huang G, Zhang Q, Wang Z, Cui J, Wu Y, Meng Q, Li S.
Medchemcomm (2019) 10 : 1606 -1614
PubMed 31803401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 6.57 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4563547 1 7.29
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 7.09
CHEMBL4559128 1 6.93
CHEMBL4454231 1 6.79
CHEMBL4468505 1 6.66
CHEMBL4566759 1 6.60
CHEMBL4473797 1 6.54
CHEMBL4469707 1 6.52
CHEMBL4449722 1 6.51
CHEMBL4581268 1 6.48
CHEMBL4476356 1 6.44
CHEMBL1935214 1 6.40
CHEMBL4566283 1 6.36
CHEMBL4518018 1 6.30
CHEMBL1935213 1 6.28
CHEMBL4445947 1 6.27
CHEMBL4514655 1 6.25
CHEMBL4554686 1 -
CHEMBL17200 1 -
CHEMBL4549846 1 -
CHEMBL1935209 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4563547 IC50 = 51.8 nM 7.29
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 80.3 nM 7.09
CHEMBL4559128 IC50 = 117.1 nM 6.93
CHEMBL4454231 IC50 = 161.3 nM 6.79
CHEMBL4468505 IC50 = 220.5 nM 6.66
CHEMBL4566759 IC50 = 250.0 nM 6.60
CHEMBL4473797 IC50 = 285.8 nM 6.54
CHEMBL4469707 IC50 = 300.9 nM 6.52
CHEMBL4449722 IC50 = 306.4 nM 6.51
CHEMBL4581268 IC50 = 330.0 nM 6.48
CHEMBL4476356 IC50 = 364.7 nM 6.44
CHEMBL1935214 IC50 = 401.2 nM 6.40
CHEMBL4566283 IC50 = 434.9 nM 6.36
CHEMBL4518018 IC50 = 499.0 nM 6.30
CHEMBL1935213 IC50 = 529.0 nM 6.28
CHEMBL4445947 IC50 = 532.6 nM 6.27
CHEMBL4514655 IC50 = 556.6 nM 6.25
CHEMBL4554686 IC50 > 1000.0 nM -
CHEMBL17200 IC50 > 1000.0 nM -
CHEMBL4549846 IC50 > 1000.0 nM -
CHEMBL1935209 IC50 > 1000.0 nM -