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Compound Detail

CHEMBL4853828

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COc1ccc(C(=O)NO)cc1NC(=O)c1ccc2[nH]c3c(c2c1)CN(C)CC3.Cl

Basic Information

ChEMBL ID CHEMBL4853828
Phase Preclinical
Structure Type MOL
InChI Key KVRSVMKECKEIPI-UHFFFAOYSA-N
Parent Compound CHEMBL5028001
Active Moiety CHEMBL5028001
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

394.4
MW (Da)
2.54
ALogP
5
HBA
4
HBD
106.7
PSA (Ų)
0.40
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 C21H23ClN4O4
MW 430.89
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.99

Activity Summary

IC50 2 meas. best 6.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 8
CHEMBL3797017
IC50 6.7 6.7 200.0 1
Histone deacetylase 8
CHEMBL3192
IC50 6.54 6.54 290.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34392190 10.1016/j.ejmech.2021.113745 Histone deacetylase 8 2
34392190 10.1016/j.ejmech.2021.113745 Schistosoma mansoni 2
34392190 10.1016/j.ejmech.2021.113745 HEK293 1

Data from ChEMBL 36 via Core Engine