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Compound Detail

CHEMBL4102189

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COC(=O)CCCCCCC(=O)Nc1ccc(Nc2ncc3cc(C(=O)N(C)C)n(C4CCCC4)c3n2)nc1

Basic Information

ChEMBL ID CHEMBL4102189
Phase Preclinical
Structure Type MOL
InChI Key UTPPSMUUXGKWBH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

535.6
MW (Da)
4.84
ALogP
9
HBA
2
HBD
131.3
PSA (Ų)
0.25
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H37N7O4
MW 535.65
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -1.20

Activity Summary

IC50 1 meas. best 7.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK4/Cyclin D3
CHEMBL3038472
IC50 7.33 7.33 47.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CDK4/Cyclin D3 IC50 = 47.0 nM 7.33 Inhibition of recombinant human full length N-terminal GST-tagged CDK4/Cyclin-D3... 29518312

Literature References

PubMed DOI Target Context # Activities
29518312 10.1021/acs.jmedchem.8b00209 Histone deacetylase 1 2
29518312 10.1021/acs.jmedchem.8b00209 CDK4/Cyclin D3 1

Data from ChEMBL 36 via Core Engine