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Compound Detail

CHEMBL249154

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N#Cc1ncc2nc1OCCCCOc1cc(P(=O)(O)O)c(Cl)cc1NC(=O)N2

Basic Information

ChEMBL ID CHEMBL249154
Phase Preclinical
Structure Type MOL
InChI Key ZYCNXNPOBIAGRO-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

439.8
MW (Da)
2.00
ALogP
7
HBA
4
HBD
166.7
PSA (Ų)
0.49
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H15ClN5O6P
MW 439.75
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness -0.66

Activity Summary

EC50 1 meas. best 4.76
IC50 1 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 8.1 8.1 8.0 1
HeLa
CHEMBL399
EC50 4.76 4.76 17400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase Chk1 IC50 = 8.0 nM 8.1 Inhibition of Chk1 17935989
HeLa EC50 = 17400.0 nM 4.76 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 NCI-H1299 1
17935989 10.1016/j.bmcl.2007.09.063 Molecular identity unknown 1

Data from ChEMBL 36 via Core Engine