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Compound Detail

CHEMBL271084

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Cn1c2cc(CCCCN3CCCC3)c(O)cc2c2c3c(c(-c4ccccc4Cl)cc21)C(=O)NC3=O

Basic Information

ChEMBL ID CHEMBL271084
Phase Preclinical
Structure Type MOL
InChI Key WCRUEPKTOWQCQO-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

502.0
MW (Da)
5.66
ALogP
5
HBA
2
HBD
74.6
PSA (Ų)
0.26
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H28ClN3O3
MW 502.01
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.12

Activity Summary

IC50 2 meas. best 8.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 8.4 8.4 4.0 1
Wee1-like protein kinase
CHEMBL5491
IC50 7.44 7.44 36.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase Chk1 IC50 = 4.0 nM 8.4 Inhibition of Chk1 18191399
Wee1-like protein kinase IC50 = 36.0 nM 7.44 Inhibition of human Wee1 18191399

Literature References

PubMed DOI Target Context # Activities
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 Chk1 1
18191399 10.1016/j.bmcl.2007.12.046 No relevant target 1

Data from ChEMBL 36 via Core Engine