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Compound Detail

CHEMBL497783

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O=C(/C=C/c1cccc(Cl)c1)/C=C/c1cccc(Cl)c1

Basic Information

ChEMBL ID CHEMBL497783
Phase Preclinical
Structure Type MOL
InChI Key AGUILNAYEDJFSM-FIFLTTCUSA-N
2
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

303.2
MW (Da)
5.29
ALogP
1
HBA
0
HBD
17.1
PSA (Ų)
0.70
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H12Cl2O
MW 303.19
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness -0.23

Activity Summary

IC50 4 meas. best 5.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1A2
CHEMBL3356
IC50 5.47 5.47 3400.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 4.67 4.67 21300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 1A2 IC50 = 3400.0 nM 5.47 Inhibition of human recombinant CYP1A2 18249473
Cytochrome P450 2C9 IC50 = 21300.0 nM 4.67 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 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 2D6 1
18249473 10.1016/j.ejmech.2007.10.034 Cytochrome P450 2B6 1
29223100 10.1016/j.ejmech.2017.11.048 Nuclear factor erythroid 2-related factor 2 1
29223100 10.1016/j.ejmech.2017.11.048 Luciferin 4-monooxygenase 1

Data from ChEMBL 36 via Core Engine