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Compound Detail

CHEMBL4646763

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COc1nc2ccccc2cc1-c1cnc([C@@H](N)CCCCCC(=O)c2ncc(CO)o2)[nH]1

Basic Information

ChEMBL ID CHEMBL4646763
Phase Preclinical
Structure Type MOL
InChI Key BMEYTXZHJHHKPN-SFHVURJKSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

449.5
MW (Da)
3.95
ALogP
8
HBA
3
HBD
140.2
PSA (Ų)
0.23
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 C24H27N5O4
MW 449.51
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -0.19

Activity Summary

IC50 3 meas. best 6.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 3/NCoR1
CHEMBL3038484
IC50 6.92 6.92 120.0 1
Histone deacetylase 1
CHEMBL325
IC50 6.71 6.71 194.0 1
Histone deacetylase 2
CHEMBL1937
IC50 6.33 6.33 470.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32676157 10.1021/acsmedchemlett.0c00302 Class 1 histone deacetylase 2
32676157 10.1021/acsmedchemlett.0c00302 Histone deacetylase 1 1
32676157 10.1021/acsmedchemlett.0c00302 Histone deacetylase 2 1
32676157 10.1021/acsmedchemlett.0c00302 Histone deacetylase 3/NCoR1 1
32676157 10.1021/acsmedchemlett.0c00302 Histone deacetylase 6 1
32676157 10.1021/acsmedchemlett.0c00302 Histone deacetylase 8 1

Data from ChEMBL 36 via Core Engine