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Assay Detail

CHEMBL666150

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

ADMET
Ratio for inhibition of Cytochrome P450 1A1 to that of Cytochrome P450 1A2
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

ADMET (CHEMBL612558)
Type ADMET

Publication

Effect of structural modification on the inhibitory selectivity of rutaecarpine derivatives on human CYP1A1, CYP1A2, and CYP1B1.
Don MJ, Lewis DF, Wang SY, Tsai MW, Ueng YF.
Bioorg Med Chem Lett (2003) 13 : 2535 -2538
PubMed 12852960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 8.21 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86022 1 9.30
CHEMBL85826 1 9.22
CHEMBL312149 1 9.00
CHEMBL413956 1 9.00
CHEMBL486598 EVODIAMINE 1 8.70
CHEMBL81923 DEHYDROEVODIAMINE 1 8.52
CHEMBL312848 1 8.30
CHEMBL314445 1 7.96
CHEMBL312248 1 7.96
CHEMBL85139 RUTAECARPINE 1 7.89
CHEMBL85960 1 7.80
CHEMBL86078 1 7.52
CHEMBL85740 1 7.48
CHEMBL314132 1 7.35
CHEMBL85106 1 7.19
CHEMBL315422 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86022 IC50 = 0.5 nM 9.30
CHEMBL85826 IC50 = 0.6 nM 9.22
CHEMBL312149 IC50 = 1.0 nM 9.00
CHEMBL413956 IC50 = 1.0 nM 9.00
CHEMBL486598 EVODIAMINE IC50 = 2.0 nM 8.70
CHEMBL81923 DEHYDROEVODIAMINE IC50 = 3.0 nM 8.52
CHEMBL312848 IC50 = 5.0 nM 8.30
CHEMBL314445 IC50 = 11.0 nM 7.96
CHEMBL312248 IC50 = 11.0 nM 7.96
CHEMBL85139 RUTAECARPINE IC50 = 13.0 nM 7.89
CHEMBL85960 IC50 = 16.0 nM 7.80
CHEMBL86078 IC50 = 30.0 nM 7.52
CHEMBL85740 IC50 = 33.0 nM 7.48
CHEMBL314132 IC50 = 45.0 nM 7.35
CHEMBL85106 IC50 = 64.0 nM 7.19
CHEMBL315422 IC50 < 0.003 nM -