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Compound Detail

CHEMBL1209130

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COc1ccc(C2CC(c3ccccc3)=NN2C(C)=O)cc1

Basic Information

ChEMBL ID CHEMBL1209130
Phase Preclinical
Structure Type MOL
InChI Key ZPDSCMQRJLPXDN-UHFFFAOYSA-N
5
Targets
7
Activities
2
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

294.4
MW (Da)
3.39
ALogP
3
HBA
0
HBD
41.9
PSA (Ų)
0.87
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H18N2O2
MW 294.35
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -1.08

Activity Summary

IC50 5 meas. best 5.12
Ki 2 meas.

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
PC-3
CHEMBL390
IC50 5.12 5.12 7670.0 1
IMR-32
CHEMBL614585
IC50 5.01 5.01 9730.0 1
HEp-2
CHEMBL614735
IC50 4.97 4.97 10680.0 1
OVCAR
CHEMBL614212
IC50 4.86 4.86 13760.0 1
Xanthine dehydrogenase/oxidase
CHEMBL3649
IC50 4.12 4.12 76200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24913985 10.1016/j.bmc.2014.05.037 Cathepsin B 2
24913985 10.1016/j.bmc.2014.05.037 Cathepsin H 2
20594840 10.1016/j.bmcl.2010.05.105 Bacillus subtilis 1
20594840 10.1016/j.bmcl.2010.05.105 Staphylococcus aureus 1
20594840 10.1016/j.bmcl.2010.05.105 Enterococcus faecalis 1
20594840 10.1016/j.bmcl.2010.05.105 Pseudomonas aeruginosa 1
20594840 10.1016/j.bmcl.2010.05.105 Escherichia coli 1
20594840 10.1016/j.bmcl.2010.05.105 Enterobacter cloacae 1
21353569 10.1016/j.bmc.2011.01.058 Xanthine dehydrogenase/oxidase 1
- 10.1007/s00044-011-9824-9 HEp-2 1
- 10.1007/s00044-011-9824-9 IMR-32 1
- 10.1007/s00044-011-9824-9 OVCAR 1
- 10.1007/s00044-011-9824-9 PC-3 1

Data from ChEMBL 36 via Core Engine