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Compound Detail

CHEMBL330398

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COc1cccc2c1NC(=O)Cc1c-2[nH]c2ccc(Br)cc12

Basic Information

ChEMBL ID CHEMBL330398
Phase Preclinical
Structure Type MOL
InChI Key IZRNPQQLTKFPRZ-UHFFFAOYSA-N
1
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

357.2
MW (Da)
4.10
ALogP
2
HBA
2
HBD
54.1
PSA (Ų)
0.69
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H13BrN2O2
MW 357.21
Aromatic Rings 3
Heavy Atoms 22

Activity Summary

IC50 6 meas. best 4.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 4.8 4.8 15995.6 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10425100 10.1021/jm9900570 Tumor Cell line 2
10425100 10.1021/jm9900570 Cyclin-dependent kinase 1 1
10425100 10.1021/jm9900570 HCT-116 1
14695817 10.1021/jm0308904 Cyclin-dependent kinase 1/cyclin B 1
14695817 10.1021/jm0308904 Cyclin-dependent kinase 5/CDK5 activator 1 1
14695817 10.1021/jm0308904 Glycogen synthase kinase-3 beta 1
19906467 10.1016/j.ejmech.2009.10.018 Cyclin-dependent kinase 1/cyclin B 1
19906467 10.1016/j.ejmech.2009.10.018 Glycogen synthase kinase-3 beta 1
19906467 10.1016/j.ejmech.2009.10.018 Malate dehydrogenase, mitochondrial 1

Data from ChEMBL 36 via Core Engine