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Compound Detail

CHEMBL3605416

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Nc1ccccc1NC(=O)c1ccc(CSC2=N[C@@H](c3ccccc3)CN2)cc1

Basic Information

ChEMBL ID CHEMBL3605416
Phase Preclinical
Structure Type MOL
InChI Key KHAQNNMTWYYNDF-OAQYLSRUSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

402.5
MW (Da)
4.45
ALogP
5
HBA
3
HBD
79.5
PSA (Ų)
0.55
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H22N4OS
MW 402.52
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -0.86

Activity Summary

IC50 4 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2)
CHEMBL2111363
IC50 7.42 7.42 38.0 1
Histone deacetylase 2
CHEMBL1937
IC50 6.75 6.75 180.0 1
Histone deacetylase 1
CHEMBL325
IC50 6.42 6.42 380.0 1
Histone deacetylase 8
CHEMBL3192
IC50 4.84 4.84 14300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26287310 10.1021/acs.jmedchem.5b00545 No relevant target 3
26287310 10.1021/acs.jmedchem.5b00545 Histone deacetylase 1 1
26287310 10.1021/acs.jmedchem.5b00545 Histone deacetylase 2 1
26287310 10.1021/acs.jmedchem.5b00545 Histone deacetylase 3/Nuclear receptor corepressor 2 (HDAC3/NCoR2) 1
26287310 10.1021/acs.jmedchem.5b00545 Histone deacetylase 6 1
26287310 10.1021/acs.jmedchem.5b00545 Histone deacetylase 8 1
26287310 10.1021/acs.jmedchem.5b00545 ADMET 1
26287310 10.1021/acs.jmedchem.5b00545 Albumin 1

Data from ChEMBL 36 via Core Engine