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Compound Detail

CHEMBL120664

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O=C1Cc2c([nH]c3ccc(C(F)(F)F)cc23)-c2cc(C#CC3(O)CCCCC3)ccc2N1

Basic Information

ChEMBL ID CHEMBL120664
Phase Preclinical
Structure Type MOL
InChI Key KDNLNRGFWZEMNV-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

438.4
MW (Da)
5.40
ALogP
2
HBA
3
HBD
65.1
PSA (Ų)
0.41
QED
1
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H21F3N2O2
MW 438.45
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -0.27

Activity Summary

IC50 4 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glycogen synthase kinase-3 beta
CHEMBL262
IC50 5.7 5.7 1999.9 1
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 5.5 5.5 3198.9 2
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 5.08 5.08 8298.5 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

Data from ChEMBL 36 via Core Engine