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Compound Detail

CHEMBL4754763

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CCC(=O)CCCCC[C@H](NC(=O)C1CN(C)C1)c1[nH]c(-c2ccc(F)cc2)nc1C#N

Basic Information

ChEMBL ID CHEMBL4754763
Phase Preclinical
Structure Type MOL
InChI Key QQGKDRSESGQPHS-FQEVSTJZSA-N
6
Targets
7
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

439.5
MW (Da)
3.74
ALogP
5
HBA
2
HBD
101.9
PSA (Ų)
0.52
QED
0
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H30FN5O2
MW 439.54
Aromatic Rings 2
Heavy Atoms 32
NP-Likeness -0.65

Activity Summary

IC50 5 meas. best 7.86
EC50 2 meas. best 5.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 3
CHEMBL1829
IC50 7.86 7.86 13.8 1
Histone deacetylase 1
CHEMBL325
IC50 7.59 7.59 25.9 1
Histone deacetylase 2
CHEMBL1937
IC50 6.93 6.93 117.0 1
Class 1 histone deacetylase
CHEMBL4523988
EC50 5.81 5.745 1564.0 2
Histone deacetylase 8
CHEMBL3192
IC50 4.71 4.71 19650.0 1
Histone deacetylase 6
CHEMBL1865
IC50 4.43 4.43 36930.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32738976 10.1016/j.bmcl.2020.127367 Class 1 histone deacetylase 2
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 8 1
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 6 1
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 2 1
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 3 1
32738976 10.1016/j.bmcl.2020.127367 Histone deacetylase 1 1

Data from ChEMBL 36 via Core Engine