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Compound Detail

CHEMBL540993

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O=C1Nc2cc(CCOc3ccc(N4CCOCC4)cc3)ccc2Nc2cc(-c3cn(Cc4cc(F)cc(F)c4)c4cnccc34)ccc21

Basic Information

ChEMBL ID CHEMBL540993
Phase Preclinical
Structure Type MOL
InChI Key JIVPBQZUQYHPRB-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

657.7
MW (Da)
7.80
ALogP
7
HBA
2
HBD
80.7
PSA (Ų)
0.17
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C39H33F2N5O3
MW 657.72
Aromatic Rings 6
Heavy Atoms 49
NP-Likeness -1.05

Activity Summary

Ki 1 meas. best 7.9

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
Ki 7.9 7.9 12.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Serine/threonine-protein kinase Chk1 Ki = 12.59 nM 7.9 Inhibition of Chk1 19385614

Literature References

PubMed DOI Target Context # Activities
19385614 10.1021/jm801444x Serine/threonine-protein kinase Chk1 1

Data from ChEMBL 36 via Core Engine