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Compound Detail

CHEMBL507142

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CNC(=O)c1ccc(Nc2nccc(-c3cnc(C4CC4)n3C(C)C)n2)cc1

Basic Information

ChEMBL ID CHEMBL507142
Phase Preclinical
Structure Type MOL
InChI Key MNGXBJAUUYRGET-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

376.5
MW (Da)
3.90
ALogP
6
HBA
2
HBD
84.7
PSA (Ų)
0.68
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24N6O
MW 376.46
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -1.39

Activity Summary

IC50 2 meas. best 7.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.09 7.09 81.0 1
LoVo
CHEMBL614721
IC50 6.18 6.18 660.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 81.0 nM 7.09 Inhibition of CDK2 18986805
LoVo IC50 = 660.0 nM 6.18 Antiproliferative activity against human LoVo cells assessed as inhibition of Br... 18986805

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 No relevant target 2
18986805 10.1016/j.bmcl.2008.10.075 Cyclin-dependent kinase 2 1
18986805 10.1016/j.bmcl.2008.10.075 LoVo 1
18986805 10.1016/j.bmcl.2008.10.075 No relevant target 1

Data from ChEMBL 36 via Core Engine