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Compound Detail

CHEMBL134501

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O=C1Cc2c([nH]c3ccc(Br)cc23)-c2cccnc2N1

Basic Information

ChEMBL ID CHEMBL134501
Phase Preclinical
Structure Type MOL
InChI Key YZVVOFLCHCBTMZ-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

328.2
MW (Da)
3.49
ALogP
2
HBA
2
HBD
57.8
PSA (Ų)
0.66
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H10BrN3O
MW 328.17
Aromatic Rings 3
Heavy Atoms 20
NP-Likeness -0.25

Activity Summary

IC50 6 meas. best 5.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 5.22 5.07 6000.0 2
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 5.22 5.22 6000.0 1
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 5.08 5.08 8400.0 2
Unchecked
CHEMBL612545
IC50 4.92 4.92 12000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33901899 10.1016/j.ejmech.2021.113445 Unchecked 2
14698171 10.1016/j.bmcl.2003.10.062 Cyclin-dependent kinase 1/cyclin B 1
14698171 10.1016/j.bmcl.2003.10.062 Cyclin-dependent kinase 5/CDK5 activator 1 1
14698171 10.1016/j.bmcl.2003.10.062 Glycogen synthase kinase-3 beta 1
14698171 10.1016/j.bmcl.2003.10.062 Unchecked 1
33901899 10.1016/j.ejmech.2021.113445 Cyclin-dependent kinase 1/cyclin B 1
33901899 10.1016/j.ejmech.2021.113445 Cyclin-dependent kinase 5/CDK5 activator 1 1

Data from ChEMBL 36 via Core Engine