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Compound Detail

CHEMBL233831

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COc1cc2c(cc1CN1CCN(C)CC1)Cc1c(-c3ccc(-c4ccc(O)c(F)c4)cc3)n[nH]c1-2

Basic Information

ChEMBL ID CHEMBL233831
Phase Preclinical
Structure Type MOL
InChI Key OKZVFXHUQZQGPK-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
2
Publications
0
Known Names

Molecular Properties

484.6
MW (Da)
4.92
ALogP
5
HBA
2
HBD
64.6
PSA (Ų)
0.37
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H29FN4O2
MW 484.58
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.77

Activity Summary

IC50 1 meas. best 7.55

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 7.55 7.55 28.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 690.0 ng.hr.mL-1 Mus musculus
AUC 1600.0 ng.hr.mL-1 Mus musculus
AUC 130.0 ng.hr.mL-1 Mus musculus
CL 183.33 mL.min-1.kg-1 Mus musculus
Cmax 1300.0 nM Mus musculus
Cmax 80.0 nM Mus musculus
F 6.0 % Mus musculus
T1/2 0.6 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17490879 10.1016/j.bmcl.2007.04.055 Mus musculus 9
17490879 10.1016/j.bmcl.2007.04.055 Serine/threonine-protein kinase Chk1 1

Data from ChEMBL 36 via Core Engine