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Compound Detail

CHEMBL498372

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CC(C)(C)c1cc(/C=C2\CC/C(=C\c3cc(C(C)(C)C)c(O)c(C(C)(C)C)c3)C2=O)cc(C(C)(C)C)c1O

Basic Information

ChEMBL ID CHEMBL498372
Phase Preclinical
Structure Type MOL
InChI Key AWUSJMKLSWCCKF-DFEHQXHXSA-N
2
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

516.8
MW (Da)
9.12
ALogP
3
HBA
2
HBD
57.5
PSA (Ų)
0.39
QED
2
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C35H48O3
MW 516.77
Aromatic Rings 2
Heavy Atoms 38
NP-Likeness -0.01

Activity Summary

IC50 6 meas. best 4.37

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1A2
CHEMBL3356
IC50 4.37 4.37 42800.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 4.26 4.26 55000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 1A2 IC50 = 42800.0 nM 4.37 Inhibition of human recombinant CYP1A2 18249473
Cytochrome P450 2C9 IC50 = 55000.0 nM 4.26 Inhibition of human recombinant CYP2C9 18249473

Literature References

PubMed DOI Target Context # Activities
18249473 10.1016/j.ejmech.2007.10.034 Cytochrome P450 1A2 3
18249473 10.1016/j.ejmech.2007.10.034 Cytochrome P450 2C9 3
18249473 10.1016/j.ejmech.2007.10.034 Cytochrome P450 2D6 3
18249473 10.1016/j.ejmech.2007.10.034 No relevant target 1
18249473 10.1016/j.ejmech.2007.10.034 Cytochrome P450 3A4 1
18249473 10.1016/j.ejmech.2007.10.034 Cytochrome P450 2B6 1

Data from ChEMBL 36 via Core Engine