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Compound Detail

CHEMBL3774636

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COc1ccc(CNc2nc(NCc3ccc(-c4ccccn4)cc3)c3[nH]nc(C(C)C)c3n2)cc1

Basic Information

ChEMBL ID CHEMBL3774636
Phase Preclinical
Structure Type MOL
InChI Key YXRWXFLAUSSXHR-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

479.6
MW (Da)
5.77
ALogP
7
HBA
3
HBD
100.6
PSA (Ų)
0.25
QED
1
Ro5 Violations
9
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H29N7O
MW 479.59
Aromatic Rings 5
Heavy Atoms 36
NP-Likeness -1.06

Activity Summary

IC50 6 meas. best 5.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 5.83 5.83 1483.0 1
K562
CHEMBL385
IC50 5.4 5.4 3950.0 1
Cyclin-dependent kinase 5
CHEMBL4036
IC50 5.36 5.36 4415.0 1
MCF7
CHEMBL387
IC50 5.28 5.28 5300.0 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 5.13 4.945 7487.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26851505 10.1016/j.ejmech.2016.01.011 MCF7 6
26851505 10.1016/j.ejmech.2016.01.011 NON-PROTEIN TARGET 3
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