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Compound Detail

CHEMBL248911

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N#Cc1ccc(-c2n[nH]c3c2Cc2ccc(OCCCN4CCOCC4)cc2-3)cn1

Basic Information

ChEMBL ID CHEMBL248911
Phase Preclinical
Structure Type MOL
InChI Key PCSOFGQRRCUQEB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
3
Publications
0
Known Names

Molecular Properties

401.5
MW (Da)
3.02
ALogP
6
HBA
1
HBD
87.1
PSA (Ų)
0.50
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 C23H23N5O2
MW 401.47
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.34

Activity Summary

IC50 1 meas. best 8.49

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 8.49 8.49 3.2 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2600.0 ng.hr.mL-1 Mus musculus
AUC 2000.0 ng.hr.mL-1 Mus musculus
AUC 3000.0 ng.hr.mL-1 Mus musculus
CL 63.33 mL.min-1.kg-1 Mus musculus
Cmax 660.0 nM Mus musculus
F 44.0 % Mus musculus
T1/2 1.4 hr Mus musculus
Vd 7.6 L.kg-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 = 3.2 nM 8.49 Inhibition of recombinant CHK1 17768051

Literature References

PubMed DOI Target Context # Activities
17768051 10.1016/j.bmcl.2007.07.069 Mus musculus 8
17768051 10.1016/j.bmcl.2007.07.069 Serine/threonine-protein kinase Chk1 1
17768051 10.1016/j.bmcl.2007.07.069 HeLa 1

Data from ChEMBL 36 via Core Engine