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Compound Detail

CHEMBL328194

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COc1cc2c(cc1OC)-c1[nH]c3ccc(C(F)(F)F)cc3c1CC(=O)N2

Basic Information

ChEMBL ID CHEMBL328194
Phase Preclinical
Structure Type MOL
InChI Key RVTOIQOTZUKDTE-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

376.3
MW (Da)
4.37
ALogP
3
HBA
2
HBD
63.4
PSA (Ų)
0.70
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H15F3N2O3
MW 376.33
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.26

Activity Summary

IC50 6 meas. best 7.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 7.12 7.12 75.0 2
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 6.55 6.55 279.9 2
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.55 6.55 280.0 1
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 6.37 6.37 429.5 1

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