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Compound Detail

CHEMBL123777

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CNCCCn1cc(C2=C(c3c[nH]c4ccccc34)C(=O)NC2=O)c2ccccc21

Basic Information

ChEMBL ID CHEMBL123777
Phase Preclinical
Structure Type MOL
InChI Key JSCLBFBGVZPWKQ-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

398.5
MW (Da)
3.30
ALogP
4
HBA
3
HBD
78.9
PSA (Ų)
0.34
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H22N4O2
MW 398.47
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.37

Activity Summary

IC50 2 meas. best 6.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 6.02 6.02 960.0 1
cAMP-dependent protein kinase (PKA)
CHEMBL2094138
IC50 5.45 5.45 3520.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14552792 10.1016/s0960-894x(03)00792-3 HCT-116 2
14552792 10.1016/s0960-894x(03)00792-3 NCI-H460 2
14552792 10.1016/s0960-894x(03)00792-3 Cyclin-dependent kinase 4/cyclin D1 1
14552792 10.1016/s0960-894x(03)00792-3 Cyclin-dependent kinase 2/cyclin E 1
14552792 10.1016/s0960-894x(03)00792-3 cAMP-dependent protein kinase (PKA) 1

Data from ChEMBL 36 via Core Engine