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Compound Detail

CHEMBL122532

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COc1cc(/C=C\c2cccs2)cc(OC)c1

Basic Information

ChEMBL ID CHEMBL122532
Phase Preclinical
Structure Type MOL
InChI Key URRYDXXEGGXDQJ-WAYWQWQTSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

246.3
MW (Da)
3.94
ALogP
3
HBA
0
HBD
18.5
PSA (Ų)
0.81
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H14O2S
MW 246.33
Aromatic Rings 2
Heavy Atoms 17
NP-Likeness -1.01

Activity Summary

IC50 3 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 1B1
CHEMBL4878
IC50 8.7 8.7 2.0 1
Cytochrome P450 1A2
CHEMBL3356
IC50 7.96 7.96 11.0 1
Cytochrome P450 1A1
CHEMBL2231
IC50 7.21 7.21 61.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 1B1 IC50 = 2.0 nM 8.7 Inhibition of CYP1B1 17544277
Cytochrome P450 1A2 IC50 = 11.0 nM 7.96 Inhibition of CYP1A2 17544277
Cytochrome P450 1A1 IC50 = 61.0 nM 7.21 Inhibition of CYP1A1 17544277

Literature References

PubMed DOI Target Context # Activities
14552759 10.1016/j.bmcl.2003.08.013 RAW264.7 1
17544277 10.1016/j.bmc.2007.05.046 Cytochrome P450 1B1 1
17544277 10.1016/j.bmc.2007.05.046 Cytochrome P450 1A1 1
17544277 10.1016/j.bmc.2007.05.046 Cytochrome P450 1A2 1

Data from ChEMBL 36 via Core Engine