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Compound Detail

CHEMBL3775502

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CC(C)c1n[nH]c2c(NCc3ccc(-c4ccccn4)cc3)nc(NCCO)nc12

Basic Information

ChEMBL ID CHEMBL3775502
Phase Preclinical
Structure Type MOL
InChI Key GVIGDUKISNSSHK-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

403.5
MW (Da)
3.55
ALogP
7
HBA
4
HBD
111.6
PSA (Ų)
0.36
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H25N7O
MW 403.49
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -1.19

Activity Summary

IC50 6 meas. best 7.57

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
NON-PROTEIN TARGET
CHEMBL3879801
IC50 7.57 7.49 27.0 2
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 7.51 7.51 31.0 1
K562
CHEMBL385
IC50 7.42 7.42 38.0 1
Cyclin-dependent kinase 5
CHEMBL4036
IC50 7.31 7.31 49.0 1
MCF7
CHEMBL387
IC50 7.29 7.29 51.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26851505 10.1016/j.ejmech.2016.01.011 NON-PROTEIN TARGET 2
26851505 10.1016/j.ejmech.2016.01.011 MCF7 1
26851505 10.1016/j.ejmech.2016.01.011 K562 1
26851505 10.1016/j.ejmech.2016.01.011 Cyclin-dependent kinase 5 1
26851505 10.1016/j.ejmech.2016.01.011 Cyclin-dependent kinase 2/cyclin E1 1

Data from ChEMBL 36 via Core Engine