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Compound Detail

CHEMBL2425959

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Cc1nc2cc(/C=C/C(=O)NO)ccc2c(=O)n1CCc1c[nH]c2ccccc12

Basic Information

ChEMBL ID CHEMBL2425959
Phase Preclinical
Structure Type MOL
InChI Key PYZKRYQFSYSEQK-VQHVLOKHSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

388.4
MW (Da)
2.95
ALogP
5
HBA
3
HBD
100.0
PSA (Ų)
0.28
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 C22H20N4O3
MW 388.43
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -0.69

Activity Summary

IC50 6 meas. best 7.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 6
CHEMBL1865
IC50 7.82 7.82 15.0 1
Histone deacetylase 1
CHEMBL325
IC50 6.12 6.12 758.0 1
Histone deacetylase 11
CHEMBL3310
IC50 5.92 5.92 1210.0 1
Histone deacetylase 8
CHEMBL3192
IC50 5.8 5.8 1590.0 1
Histone deacetylase 2
CHEMBL1937
IC50 5.66 5.66 2210.0 1
Amyloid-beta precursor protein
CHEMBL2487
IC50 5.13 5.13 7400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23905680 10.1021/jm400564j Amyloid-beta precursor protein 2
23905680 10.1021/jm400564j Unchecked 2
23905680 10.1021/jm400564j Vero 1
23905680 10.1021/jm400564j PC-12 1
23905680 10.1021/jm400564j ADMET 1
23905680 10.1021/jm400564j Histone deacetylase 11 1
23905680 10.1021/jm400564j Histone deacetylase 6 1
23905680 10.1021/jm400564j Histone deacetylase 8 1
23905680 10.1021/jm400564j Histone deacetylase 2 1
23905680 10.1021/jm400564j Histone deacetylase 1 1

Data from ChEMBL 36 via Core Engine