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Compound Detail

CHEMBL318208

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Cn1c2c(c3cc(Br)ccc31)CC(=O)Nc1ccccc1-2

Basic Information

ChEMBL ID CHEMBL318208
Phase Preclinical
Structure Type MOL
InChI Key CYWSKAGHMPTBMS-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

341.2
MW (Da)
4.10
ALogP
2
HBA
1
HBD
34.0
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 C17H13BrN2O
MW 341.21
Aromatic Rings 3
Heavy Atoms 21
NP-Likeness -0.30

Activity Summary

IC50 6 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 6.4 6.4 399.9 2
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 5.21 5.21 6194.4 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 5.21 5.21 6200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

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

Data from ChEMBL 36 via Core Engine