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Compound Detail

CHEMBL245796

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COc1cc2c(cc1OC)-c1n[nH]c(-c3ccc(-c4ccc(O)cc4)cc3)c1C2

Basic Information

ChEMBL ID CHEMBL245796
Phase Preclinical
Structure Type MOL
InChI Key VXNCNVGVUUUFPK-UHFFFAOYSA-N
2
Targets
5
Activities
3
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

384.4
MW (Da)
5.04
ALogP
4
HBA
2
HBD
67.4
PSA (Ų)
0.46
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H20N2O3
MW 384.44
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.04

Activity Summary

IC50 3 meas. best 8.8
EC50 1 meas. best 6.7
Ki 1 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 8.8 8.7667 1.6 3
Serine/threonine-protein kinase Chk1
CHEMBL4630
Ki 8.8 8.8 1.6 1
NCI-H1299
CHEMBL612255
EC50 6.7 6.7 200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17544271 10.1016/j.bmcl.2007.05.027 Serine/threonine-protein kinase Chk1 1
17544271 10.1016/j.bmcl.2007.05.027 HeLa 1
17544271 10.1016/j.bmcl.2007.05.027 Molecular identity unknown 1
17544271 10.1016/j.bmcl.2007.05.027 NCI-H1299 1
17544271 10.1016/j.bmcl.2007.05.027 SW-620 1
17768051 10.1016/j.bmcl.2007.07.069 Serine/threonine-protein kinase Chk1 1
17768051 10.1016/j.bmcl.2007.07.069 HeLa 1
17768051 10.1016/j.bmcl.2007.07.069 NON-PROTEIN TARGET 1
17827013 10.1016/j.bmcl.2007.07.102 Serine/threonine-protein kinase Chk1 1
19385614 10.1021/jm801444x Serine/threonine-protein kinase Chk1 1

Data from ChEMBL 36 via Core Engine