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Compound Detail

CHEMBL4633409

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CCc1nc(N)nc(N)c1-c1ccc(/C=C/C(=O)NO)cc1

Basic Information

ChEMBL ID CHEMBL4633409
Phase Preclinical
Structure Type MOL
InChI Key JOYSLHNWDIQPJZ-VMPITWQZSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

299.3
MW (Da)
1.39
ALogP
6
HBA
4
HBD
127.2
PSA (Ų)
0.38
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H17N5O2
MW 299.33
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness -0.28

Activity Summary

IC50 3 meas. best 6.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 6.4 6.4 400.0 1
Histone deacetylase 8
CHEMBL3192
IC50 5.75 5.75 1800.0 1
Histone deacetylase 1
CHEMBL325
IC50 5.66 5.66 2200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32061484 10.1016/j.bmc.2020.115345 Histone deacetylase 1 1
32061484 10.1016/j.bmc.2020.115345 Histone deacetylase 6 1
32061484 10.1016/j.bmc.2020.115345 Histone deacetylase 8 1
32061484 10.1016/j.bmc.2020.115345 A549 1
32061484 10.1016/j.bmc.2020.115345 MCF7 1
32061484 10.1016/j.bmc.2020.115345 MDA-MB-231 1

Data from ChEMBL 36 via Core Engine