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Compound Detail

CHEMBL355631

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COc1cc[nH]c1/C=C1\C(=O)Nc2ccc(F)c(C#C[C@@H]3CCCN3)c21

Basic Information

ChEMBL ID CHEMBL355631
Phase Preclinical
Structure Type MOL
InChI Key NOCXREGHIRXAHY-PBBNAPBQSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

351.4
MW (Da)
2.76
ALogP
3
HBA
3
HBD
66.2
PSA (Ų)
0.58
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 C20H18FN3O2
MW 351.38
Aromatic Rings 2
Heavy Atoms 26
NP-Likeness -0.13

Activity Summary

IC50 4 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin E
CHEMBL2094126
IC50 8.7 8.7 2.0 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 8.7 8.7 2.0 1
MDA-MB-435
CHEMBL614697
IC50 7.51 7.51 31.0 1
SW480
CHEMBL612544
IC50 7.4 7.4 40.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15012993 10.1016/j.bmcl.2003.12.009 Cyclin-dependent kinase 2/cyclin E 1
15012993 10.1016/j.bmcl.2003.12.009 MDA-MB-435 1
15012993 10.1016/j.bmcl.2003.12.009 SW480 1
27543880 10.1016/j.ejmech.2016.08.011 Cyclin-dependent kinase 2 1

Data from ChEMBL 36 via Core Engine