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Compound Detail

CHEMBL4647014

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CCC(=O)CCCCC[C@H](NC(=O)[C@H]1CC12CCN(Cc1ccc(OC)cc1)CC2)c1ncc(-c2cc3ccccc3nc2OC)[nH]1

Basic Information

ChEMBL ID CHEMBL4647014
Phase Preclinical
Structure Type MOL
InChI Key TWKRUPMODSFFPO-VTIYRKAUSA-N
6
Targets
7
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

637.8
MW (Da)
7.03
ALogP
7
HBA
2
HBD
109.4
PSA (Ų)
0.13
QED
2
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C38H47N5O4
MW 637.83
Aromatic Rings 4
Heavy Atoms 47
NP-Likeness -0.37

Activity Summary

IC50 5 meas. best 8.77
EC50 2 meas. best 6.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 3
CHEMBL1829
IC50 8.77 8.77 1.7 1
Histone deacetylase 1
CHEMBL325
IC50 8.19 8.19 6.4 1
Histone deacetylase 2
CHEMBL1937
IC50 7.76 7.76 17.4 1
Human immunodeficiency virus
CHEMBL613758
EC50 6.95 6.85 113.0 2
Histone deacetylase 6
CHEMBL1865
IC50 6.01 6.01 972.0 1
Histone deacetylase 8
CHEMBL3192
IC50 5.49 5.49 3231.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32331932 10.1016/j.bmcl.2020.127197 Human immunodeficiency virus 2
32331932 10.1016/j.bmcl.2020.127197 Histone deacetylase 1 1
32331932 10.1016/j.bmcl.2020.127197 Histone deacetylase 2 1
32331932 10.1016/j.bmcl.2020.127197 Histone deacetylase 3 1
32331932 10.1016/j.bmcl.2020.127197 Histone deacetylase 6 1
32331932 10.1016/j.bmcl.2020.127197 Histone deacetylase 8 1

Data from ChEMBL 36 via Core Engine