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Compound Detail

CHEMBL271715

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O=C1NC(=O)c2c1c(-c1ccccc1Cl)cc1c2c2cc(O)c(OCCCN3CCOCC3)cc2n1CCO

Basic Information

ChEMBL ID CHEMBL271715
Phase Preclinical
Structure Type MOL
InChI Key VSGRXSHIXKUPPN-UHFFFAOYSA-N
4
Targets
6
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

550.0
MW (Da)
3.80
ALogP
8
HBA
3
HBD
113.3
PSA (Ų)
0.23
QED
1
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28ClN3O6
MW 550.01
Aromatic Rings 4
Heavy Atoms 39
NP-Likeness -0.40

Activity Summary

IC50 6 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Wee1-like protein kinase
CHEMBL5491
IC50 7.82 7.82 15.0 3
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.6 6.6 250.0 1
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 6.54 6.54 290.0 1
HT-29
CHEMBL384
IC50 6.28 6.28 530.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18191399 10.1016/j.bmcl.2007.12.046 Unchecked 4
18191399 10.1016/j.bmcl.2007.12.046 Serine/threonine-protein kinase Chk1 2
18976834 10.1016/j.ejmech.2008.09.027 Wee1-like protein kinase 2
18191399 10.1016/j.bmcl.2007.12.046 HT-29 2
18191399 10.1016/j.bmcl.2007.12.046 Ribosomal protein S6 kinase alpha-1 1
18191399 10.1016/j.bmcl.2007.12.046 Wee1-like protein kinase 1
18191399 10.1016/j.bmcl.2007.12.046 Serine/threonine-protein kinase Sgk1 1
18191399 10.1016/j.bmcl.2007.12.046 RAC-alpha serine/threonine-protein kinase 1
18191399 10.1016/j.bmcl.2007.12.046 [Pyruvate dehydrogenase (acetyl-transferring)] kinase isozyme 1, mitochondrial 1
18191399 10.1016/j.bmcl.2007.12.046 Protein kinase C alpha type 1
18191399 10.1016/j.bmcl.2007.12.046 MAP kinase-activated protein kinase 5 1
18191399 10.1016/j.bmcl.2007.12.046 Ribosomal protein S6 kinase alpha-5 1
18191399 10.1016/j.bmcl.2007.12.046 MAP kinase-activated protein kinase 2 1
18191399 10.1016/j.bmcl.2007.12.046 Mitogen-activated protein kinase 13 1
18191399 10.1016/j.bmcl.2007.12.046 Mitogen-activated protein kinase 12 1
18191399 10.1016/j.bmcl.2007.12.046 Mitogen-activated protein kinase 11 1
18191399 10.1016/j.bmcl.2007.12.046 Mitogen-activated protein kinase 14 1
18191399 10.1016/j.bmcl.2007.12.046 No relevant target 1
18191399 10.1016/j.bmcl.2007.12.046 Mitogen-activated protein kinase 1 1
18191399 10.1016/j.bmcl.2007.12.046 Dual specificity mitogen-activated protein kinase kinase 1 1

Data from ChEMBL 36 via Core Engine