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Compound Detail

CHEMBL437330

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Cc1ccccc1C(=O)c1cnc(Nc2ccc(N3CCN(C)CC3)cc2)nc1N

Basic Information

ChEMBL ID CHEMBL437330
Phase Preclinical
Structure Type MOL
InChI Key SYOMYBAFMYPWKL-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

402.5
MW (Da)
3.09
ALogP
7
HBA
2
HBD
87.4
PSA (Ų)
0.63
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H26N6O
MW 402.50
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -1.52

Activity Summary

IC50 1 meas. best 4.78
Ki 1 meas. best 6.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
Ki 6.23 6.23 584.0 1
HCT-116
CHEMBL394
IC50 4.78 4.78 16500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cyclin-dependent kinase 4/cyclin D1 Ki = 584.0 nM 6.23 Inhibition of CDK4/Cyclin D1 17064073
HCT-116 IC50 = 16500.0 nM 4.78 Inhibition of HCT116 cell growth 17064073

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