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Compound Detail

CHEMBL383875

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COc1ccccc1C(=O)c1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1N

Basic Information

ChEMBL ID CHEMBL383875
Phase Preclinical
Structure Type MOL
InChI Key CBUPUJHKQHRYSF-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

418.5
MW (Da)
2.79
ALogP
8
HBA
2
HBD
96.6
PSA (Ų)
0.59
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 C23H26N6O2
MW 418.50
Aromatic Rings 3
Heavy Atoms 31
NP-Likeness -1.37

Activity Summary

Ki 3 meas. best 6.8
IC50 1 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
Ki 6.8 6.8 159.0 1
Cyclin-dependent kinase 1
CHEMBL308
Ki 5.9 5.9 1259.0 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 5.29 5.29 5141.0 1
HCT-116
CHEMBL394
IC50 4.96 4.96 11000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17064073 10.1021/jm0606138 Cyclin-dependent kinase 4/cyclin D1 1
17064073 10.1021/jm0606138 Cyclin-dependent kinase 1 1
17064073 10.1021/jm0606138 Cyclin-dependent kinase 2 1
17064073 10.1021/jm0606138 HCT-116 1

Data from ChEMBL 36 via Core Engine