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Compound Detail

CHEMBL280867

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COc1ccc(-c2[nH]nc3c2C(=O)c2c(NC(=O)C(C)C)cccc2-3)cc1

Basic Information

ChEMBL ID CHEMBL280867
Phase Preclinical
Structure Type MOL
InChI Key JKYJMEJOTVNJIB-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

361.4
MW (Da)
3.89
ALogP
4
HBA
2
HBD
84.1
PSA (Ų)
0.58
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H19N3O3
MW 361.40
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.64

Activity Summary

IC50 4 meas. best 5.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 5.85 5.85 1412.5 1
Cyclin-dependent kinase 2/cyclin E
CHEMBL2094126
IC50 5.85 5.85 1400.0 1
HCT-116
CHEMBL394
IC50 5.54 5.54 2900.0 1
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 4.46 4.46 35000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11311054 10.1021/jm0100032 Cyclin-dependent kinase 4/cyclin D1 1
11311054 10.1021/jm0100032 Cyclin-dependent kinase 2/cyclin E 1
11311054 10.1021/jm0100032 HCT-116 1
11311054 10.1021/jm0100032 AG1523 1
26741853 10.1016/j.ejmech.2015.12.023 Cyclin-dependent kinase 2/cyclin E1 1

Data from ChEMBL 36 via Core Engine