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Compound Detail

CHEMBL400397

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N#Cc1ncc2nc1OC/C=C\COc1cc(OCCCN3CCOCC3)c(Cl)cc1NC(=O)N2

Basic Information

ChEMBL ID CHEMBL400397
Phase Preclinical
Structure Type MOL
InChI Key IDPPCTVUQPDPFF-UPHRSURJSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

500.9
MW (Da)
3.07
ALogP
9
HBA
2
HBD
130.9
PSA (Ų)
0.47
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25ClN6O5
MW 500.94
Aromatic Rings 2
Heavy Atoms 35
NP-Likeness -0.98

Activity Summary

EC50 1 meas. best 5.72
IC50 1 meas. best 9.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 9.52 9.52 0.3 1
HeLa
CHEMBL399
EC50 5.72 5.72 1900.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase Chk1 IC50 = 0.3 nM 9.52 Inhibition of Chk1 17935989
HeLa EC50 = 1900.0 nM 5.72 Cytotoxicity against HeLa cells by MTS assay 17935989

Literature References

PubMed DOI Target Context # Activities
17935989 10.1016/j.bmcl.2007.09.063 Serine/threonine-protein kinase Chk1 1
17935989 10.1016/j.bmcl.2007.09.063 HeLa 1
17935989 10.1016/j.bmcl.2007.09.063 Molecular identity unknown 1
17935989 10.1016/j.bmcl.2007.09.063 NCI-H1299 1

Data from ChEMBL 36 via Core Engine