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Compound Detail

CHEMBL120703

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CC(C)(C)OC(=O)Nc1ccc(Nc2[nH]nc3ncnc(Nc4cccc(Cl)c4)c23)cc1

Basic Information

ChEMBL ID CHEMBL120703
Phase Preclinical
Structure Type MOL
InChI Key UJPPYLLBYAYYPH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

451.9
MW (Da)
5.84
ALogP
7
HBA
4
HBD
116.8
PSA (Ų)
0.30
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22ClN7O2
MW 451.92
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -1.45

Activity Summary

IC50 1 meas. best 4.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 1
CHEMBL308
IC50 4.24 4.24 57000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 1 IC50 = 57000.0 nM 4.24 Inhibitory activity against CDK1 Ser/Thr kinase 9357527

Literature References

PubMed DOI Target Context # Activities
9357527 10.1021/jm970124v Epidermal growth factor receptor 2
9357527 10.1021/jm970124v Tyrosine-protein kinase ABL1 1
9357527 10.1021/jm970124v Proto-oncogene tyrosine-protein kinase Src 1
9357527 10.1021/jm970124v Protein kinase C alpha type 1
9357527 10.1021/jm970124v Cyclin-dependent kinase 1 1
9357527 10.1021/jm970124v Balb/MK 1
9357527 10.1021/jm970124v Platelet-derived growth factor receptor 1

Data from ChEMBL 36 via Core Engine