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Compound Detail

CHEMBL243931

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O=c1ccc(=O)c2c1c1[nH]c3ccc(O)cc3c1c1c(=O)[nH]c(=O)c21

Basic Information

ChEMBL ID CHEMBL243931
Phase Preclinical
Structure Type MOL
InChI Key DCKZKNXQWSTPNW-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
19
Publications
0
Known Names

Molecular Properties

332.3
MW (Da)
0.98
ALogP
5
HBA
3
HBD
120.1
PSA (Ų)
0.39
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H8N2O5
MW 332.27
Aromatic Rings 5
Heavy Atoms 25
NP-Likeness 0.61

Activity Summary

IC50 4 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Serine/threonine-protein kinase Chk1
CHEMBL4630
IC50 7.57 7.57 27.0 1
L1210
CHEMBL386
IC50 5.08 5.08 8400.0 1
HCT-116
CHEMBL394
IC50 4.81 4.81 15400.0 1
HT-29
CHEMBL384
IC50 4.3 4.3 50600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17722905 10.1021/jm070664k Unchecked 5
17722905 10.1021/jm070664k Serine/threonine-protein kinase Chk1 3
17722905 10.1021/jm070664k RAF proto-oncogene serine/threonine-protein kinase 1
17722905 10.1021/jm070664k Protein kinase C alpha type 1
17722905 10.1021/jm070664k RAC-alpha serine/threonine-protein kinase 1
17722905 10.1021/jm070664k Ribosomal protein S6 kinase beta-1 1
17722905 10.1021/jm070664k Dual specificity mitogen-activated protein kinase kinase 1 1
17722905 10.1021/jm070664k MAP kinase-activated protein kinase 2 1
17722905 10.1021/jm070664k Mitogen-activated protein kinase 1 1
17722905 10.1021/jm070664k Glycogen synthase kinase-3 beta 1
17722905 10.1021/jm070664k Glycogen synthase kinase-3 alpha 1
17722905 10.1021/jm070664k Casein kinase I isoform delta 1
17722905 10.1021/jm070664k Casein kinase II subunit alpha 1
17722905 10.1021/jm070664k CDK9/cyclin T1 1
17722905 10.1021/jm070664k Cyclin-dependent kinase 5/CDK5 activator 1 1
17722905 10.1021/jm070664k Proto-oncogene tyrosine-protein kinase Src 1
17722905 10.1021/jm070664k L1210 1
17722905 10.1021/jm070664k HCT-116 1
17722905 10.1021/jm070664k HT-29 1

Data from ChEMBL 36 via Core Engine