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Compound Detail

CHEMBL1241758

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O=C(Nc1cc(C2CCC2)c[nH]1)Nc1cccc2ccncc12

Basic Information

ChEMBL ID CHEMBL1241758
Phase Preclinical
Structure Type MOL
InChI Key JAPIBZGEANTMOW-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

306.4
MW (Da)
4.47
ALogP
2
HBA
3
HBD
69.8
PSA (Ų)
0.67
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H18N4O
MW 306.37
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.88

Activity Summary

IC50 2 meas. best 8.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 5
CHEMBL4036
IC50 8.3 8.3 5.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 7.26 7.26 55.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 5 IC50 = 5.0 nM 8.3 Inhibition of CDK5 16584130
Cyclin-dependent kinase 1 IC50 = 55.0 nM 7.26 Inhibition of CDK1 16584130

Literature References

PubMed DOI Target Context # Activities
16584130 10.1208/aapsj080125 Cyclin-dependent kinase 5 1
16584130 10.1208/aapsj080125 Cyclin-dependent kinase 1 1

Data from ChEMBL 36 via Core Engine