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Compound Detail

CHEMBL519422

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CCn1c(-c2ccnc(Nc3ccc(C(=O)NC)cc3)n2)cnc1C

Basic Information

ChEMBL ID CHEMBL519422
Phase Preclinical
Structure Type MOL
InChI Key HBGBNRBGCBVAFP-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

336.4
MW (Da)
2.77
ALogP
6
HBA
2
HBD
84.7
PSA (Ų)
0.75
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20N6O
MW 336.40
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.53

Activity Summary

IC50 2 meas. best 7.25

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 7.25 7.25 56.0 1
LoVo
CHEMBL614721
IC50 5.51 5.51 3100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 2 IC50 = 56.0 nM 7.25 Inhibition of CDK2 18986805
LoVo IC50 = 3100.0 nM 5.51 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