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Compound Detail

CHEMBL4210919

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CC(C)CCn1cnc2c(Nc3cccc(Cl)c3)nc(N[C@H]3CC[C@H](N)CC3)nc21

Basic Information

ChEMBL ID CHEMBL4210919
Phase Preclinical
Structure Type MOL
InChI Key BTTQBEBOAWSMQZ-QAQDUYKDSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

428.0
MW (Da)
4.95
ALogP
7
HBA
3
HBD
93.7
PSA (Ų)
0.49
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H30ClN7
MW 427.98
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.30

Activity Summary

IC50 2 meas. best 7.18

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Platelet-derived growth factor receptor alpha
CHEMBL2007
IC50 7.18 7.18 66.0 1
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 6.56 6.56 275.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29089259 10.1016/j.bmc.2017.10.032 EOL1 18
29089259 10.1016/j.bmc.2017.10.032 Platelet-derived growth factor receptor alpha 5
29089259 10.1016/j.bmc.2017.10.032 HCC827 2
29089259 10.1016/j.bmc.2017.10.032 K562 2
29089259 10.1016/j.bmc.2017.10.032 Cyclin-dependent kinase 2/cyclin E1 1
29089259 10.1016/j.bmc.2017.10.032 BT-474 1
29089259 10.1016/j.bmc.2017.10.032 MCF7 1

Data from ChEMBL 36 via Core Engine