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Compound Detail

CHEMBL1809191

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CC(=O)N1CCN(c2ccc(Nc3nccc(-c4cnc5ccccn45)n3)cc2)CC1

Basic Information

ChEMBL ID CHEMBL1809191
Phase Preclinical
Structure Type MOL
InChI Key CCEAKNFETFDIHE-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

413.5
MW (Da)
3.20
ALogP
7
HBA
1
HBD
78.7
PSA (Ų)
0.55
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23N7O
MW 413.49
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -1.94

Activity Summary

IC50 2 meas. best 7.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.11 7.11 78.0 1
Insulin-like growth factor 1 receptor
CHEMBL1957
IC50 6.57 6.57 270.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 78.0 nM 7.11 Inhibition of CDK2 21775140
Insulin-like growth factor 1 receptor IC50 = 270.0 nM 6.57 Inhibition of IGF1R 21775140

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3301361 No relevant target 2
21775140 10.1016/j.bmcl.2011.06.093 Insulin-like growth factor 1 receptor 1
21775140 10.1016/j.bmcl.2011.06.093 Cyclin-dependent kinase 2 1

Data from ChEMBL 36 via Core Engine