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Compound Detail

CHEMBL4453997

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COc1ccc(-c2n[nH]c3c2C(=O)c2c(C=O)cccc2-3)cc1

Basic Information

ChEMBL ID CHEMBL4453997
Phase Preclinical
Structure Type MOL
InChI Key TVZCIMNGAOZHSH-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

304.3
MW (Da)
3.11
ALogP
4
HBA
1
HBD
72.0
PSA (Ų)
0.59
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H12N2O3
MW 304.31
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.20

Activity Summary

IC50 2 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4
CHEMBL331
IC50 9.7 9.7 0.2 1
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.24 7.24 57.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4 IC50 = 0.2 nM 9.7 Inhibition of CDK4 (unknown origin) 31167153
Cyclin-dependent kinase 2 IC50 = 57.0 nM 7.24 Inhibition of CDK2 (unknown origin) 31167153

Literature References

PubMed DOI Target Context # Activities
31167153 10.1016/j.ejmech.2019.05.070 Cyclin-dependent kinase 4 1
31167153 10.1016/j.ejmech.2019.05.070 Cyclin-dependent kinase 2 1

Data from ChEMBL 36 via Core Engine