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Compound Detail

CHEMBL4634096

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CCc1nc(N)nc(N)c1-c1ccc(-c2ccc(/C=C/C(=O)NO)cc2)cc1

Basic Information

ChEMBL ID CHEMBL4634096
Phase Preclinical
Structure Type MOL
InChI Key CHZMNTOWTCRUDZ-LFYBBSHMSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

375.4
MW (Da)
3.06
ALogP
6
HBA
4
HBD
127.2
PSA (Ų)
0.31
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H21N5O2
MW 375.43
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.25

Activity Summary

IC50 6 meas. best 7.14

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 7.14 7.14 73.0 1
Histone deacetylase 1
CHEMBL325
IC50 5.43 5.43 3700.0 1
MDA-MB-231
CHEMBL400
IC50 5.26 5.26 5430.0 1
Vero
CHEMBL391
IC50 5.16 5.16 6900.0 1
MCF7
CHEMBL387
IC50 5.03 5.03 9300.0 1
A549
CHEMBL392
IC50 5.0 5.0 10000.0 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
32061484 10.1016/j.bmc.2020.115345 Vero 1

Data from ChEMBL 36 via Core Engine