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Compound Detail

CHEMBL445410

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COc1cc2c(cc1CN[C@H]1CC[C@H](O)CC1)Cc1c-2n[nH]c1-c1ccc(C#N)cc1

Basic Information

ChEMBL ID CHEMBL445410
Phase Preclinical
Structure Type MOL
InChI Key VUOMCYBVXLTIPV-MXVIHJGJSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

414.5
MW (Da)
3.92
ALogP
5
HBA
3
HBD
94.0
PSA (Ų)
0.46
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H26N4O2
MW 414.51
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -0.56

Activity Summary

EC50 2 meas. best 5.89
IC50 1 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 7.77 7.77 17.0 1
NCI-H1299
CHEMBL612255
EC50 5.89 5.89 1300.0 1
HeLa
CHEMBL399
EC50 4.79 4.79 16300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17827013 10.1016/j.bmcl.2007.07.102 Serine/threonine-protein kinase Chk1 1
17827013 10.1016/j.bmcl.2007.07.102 Molecular identity unknown 1
17827013 10.1016/j.bmcl.2007.07.102 HeLa 1
17827013 10.1016/j.bmcl.2007.07.102 NCI-H1299 1

Data from ChEMBL 36 via Core Engine