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Compound Detail

CHEMBL401177

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C[C@@H]1CN(CCCOc2ccc3c(c2)-c2[nH]nc(-c4ccc(C#N)nc4)c2C3)C[C@H](C)O1

Basic Information

ChEMBL ID CHEMBL401177
Phase Preclinical
Structure Type MOL
InChI Key LDEYSIHATAIBOO-CALCHBBNSA-N
1
Targets
1
Activities
1
Assay Types
1
PK Parameters
4
Publications
0
Known Names

Molecular Properties

429.5
MW (Da)
3.79
ALogP
6
HBA
1
HBD
87.1
PSA (Ų)
0.47
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H27N5O2
MW 429.52
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.14

Activity Summary

IC50 1 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 9.0 9.0 1.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3000.0 ng.hr.mL-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase Chk1 IC50 = 1.0 nM 9.0 Inhibition of recombinant CHK1 17768051

Literature References

PubMed DOI Target Context # Activities
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 No relevant target 1
17768051 10.1016/j.bmcl.2007.07.069 Mus musculus 1

Data from ChEMBL 36 via Core Engine