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Assay Detail

CHEMBL4733550

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

ADMET
Inhibition of recombinant human CYP1A2 using 7-ethoxyresorufin as substrate after 50 mins in presence of NADP+ by EROD assay
47
Total Activities
47
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 heterocycle-containing α-naphthoflavone derivatives as water-soluble, highly potent and selective CYP1B1 inhibitors.
Dong J,Huang G,Cui Q,Meng Q,Li S,Cui J
Eur J Med Chem (2021) 209 : 112895 -112895
PubMed 33069055 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 47 6.74 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283196 ALPHA-NAPHTHOFLAVONE 1 7.75
CHEMBL4781932 1 7.54
CHEMBL4746097 1 7.39
CHEMBL4744690 1 7.17
CHEMBL4755282 1 6.97
CHEMBL4745341 1 6.97
CHEMBL4781895 1 6.93
CHEMBL4759778 1 6.85
CHEMBL4750507 1 6.83
CHEMBL4791264 1 6.79
CHEMBL4744264 1 6.70
CHEMBL4798651 1 6.68
CHEMBL4759410 1 6.46
CHEMBL4799346 1 6.29
CHEMBL4753119 1 6.21
CHEMBL4741985 1 6.20
CHEMBL4799247 1 6.17
CHEMBL4750829 1 6.13
CHEMBL4754216 1 6.01
CHEMBL4740802 1 -
CHEMBL4746873 1 -
CHEMBL4761904 1 -
CHEMBL4745897 1 -
CHEMBL4798694 1 -
CHEMBL4740805 1 -
CHEMBL4782753 1 -
CHEMBL4749123 1 -
CHEMBL4799305 1 -
CHEMBL4798948 1 -
CHEMBL4792471 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283196 ALPHA-NAPHTHOFLAVONE IC50 = 18.0 nM 7.75
CHEMBL4781932 IC50 = 29.2 nM 7.54
CHEMBL4746097 IC50 = 40.4 nM 7.39
CHEMBL4744690 IC50 = 67.2 nM 7.17
CHEMBL4755282 IC50 = 107.6 nM 6.97
CHEMBL4745341 IC50 = 108.0 nM 6.97
CHEMBL4781895 IC50 = 117.3 nM 6.93
CHEMBL4759778 IC50 = 140.6 nM 6.85
CHEMBL4750507 IC50 = 148.2 nM 6.83
CHEMBL4791264 IC50 = 160.7 nM 6.79
CHEMBL4744264 IC50 = 199.8 nM 6.70
CHEMBL4798651 IC50 = 208.5 nM 6.68
CHEMBL4759410 IC50 = 348.6 nM 6.46
CHEMBL4799346 IC50 = 518.0 nM 6.29
CHEMBL4753119 IC50 = 622.8 nM 6.21
CHEMBL4741985 IC50 = 628.5 nM 6.20
CHEMBL4799247 IC50 = 668.4 nM 6.17
CHEMBL4750829 IC50 = 742.0 nM 6.13
CHEMBL4754216 IC50 = 965.5 nM 6.01
CHEMBL4740715 IC50 > 1000.0 nM -
CHEMBL4758643 IC50 > 1000.0 nM -
CHEMBL4781446 IC50 > 1000.0 nM -
CHEMBL4763388 IC50 > 1000.0 nM -
CHEMBL4749988 IC50 > 1000.0 nM -
CHEMBL4747913 IC50 > 1000.0 nM -
CHEMBL4753083 IC50 > 1000.0 nM -
CHEMBL4746672 IC50 > 1000.0 nM -
CHEMBL4742050 IC50 > 1000.0 nM -
CHEMBL4753629 IC50 > 1000.0 nM -
CHEMBL4759437 IC50 > 1000.0 nM -
CHEMBL4745122 IC50 > 1000.0 nM -
CHEMBL4746733 IC50 > 1000.0 nM -
CHEMBL4760296 IC50 > 1000.0 nM -
CHEMBL4740535 IC50 > 1000.0 nM -
CHEMBL4778382 IC50 > 1000.0 nM -
CHEMBL4795310 IC50 > 1000.0 nM -
CHEMBL4792471 IC50 > 1000.0 nM -
CHEMBL4798948 IC50 > 1000.0 nM -
CHEMBL4799305 IC50 > 1000.0 nM -
CHEMBL4749123 IC50 > 1000.0 nM -
CHEMBL4782753 IC50 > 1000.0 nM -
CHEMBL4740805 IC50 > 1000.0 nM -
CHEMBL4798694 IC50 > 1000.0 nM -
CHEMBL4745897 IC50 > 1000.0 nM -
CHEMBL4761904 IC50 > 1000.0 nM -
CHEMBL4746873 IC50 > 1000.0 nM -
CHEMBL4740802 IC50 > 1000.0 nM -