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Compound Detail

CHEMBL121958

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COC(=O)/C=C/c1ccc2c(c1)-c1[nH]c3ccc(C(F)(F)F)cc3c1CC(=O)N2

Basic Information

ChEMBL ID CHEMBL121958
Phase Preclinical
Structure Type MOL
InChI Key DJCQWLAUTLNODY-XVNBXDOJSA-N
4
Targets
5
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

400.4
MW (Da)
4.53
ALogP
3
HBA
2
HBD
71.2
PSA (Ų)
0.49
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 C21H15F3N2O3
MW 400.36
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.05

Activity Summary

IC50 5 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 6.46 6.46 349.9 1
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 5.37 5.37 4295.4 2
Unchecked
CHEMBL612545
IC50 5.37 5.37 4300.0 1
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 4.82 4.82 14996.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10741555 10.1016/s0960-894x(00)00048-2 Cyclin-dependent kinase 1/cyclin B 1
10741555 10.1016/s0960-894x(00)00048-2 HCT-116 1
10741555 10.1016/s0960-894x(00)00048-2 NON-PROTEIN TARGET 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
28803677 10.1016/j.ejmech.2017.07.042 Unchecked 1

Data from ChEMBL 36 via Core Engine