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Compound Detail

CHEMBL3621298

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Nc1ccccc1NC(=O)CCCCCCC(=O)Nc1ccc2c(c1)/C(=C/c1ccc[nH]1)C(=O)N2

Basic Information

ChEMBL ID CHEMBL3621298
Phase Preclinical
Structure Type MOL
InChI Key YBIREACTYDYGTB-PGMHBOJBSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

471.6
MW (Da)
5.01
ALogP
4
HBA
5
HBD
129.1
PSA (Ų)
0.16
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H29N5O3
MW 471.56
Aromatic Rings 3
Heavy Atoms 35
NP-Likeness -0.80

Activity Summary

IC50 4 meas. best 6.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 6.43 6.43 373.0 1
Histone deacetylase 3
CHEMBL1829
IC50 6.41 6.41 394.0 1
Histone deacetylase 2
CHEMBL1937
IC50 5.65 5.65 2230.0 1
Histone deacetylase 6
CHEMBL1865
IC50 5.34 5.34 4610.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 1 IC50 = 373.0 nM 6.43 Inhibition of HDAC1 (unknown origin) -
Histone deacetylase 3 IC50 = 394.0 nM 6.41 Inhibition of HDAC3 (unknown origin) -
Histone deacetylase 2 IC50 = 2230.0 nM 5.65 Inhibition of HDAC2 (unknown origin) -
Histone deacetylase 6 IC50 = 4610.0 nM 5.34 Inhibition of HDAC6 (unknown origin) -

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C4MD00211C Histone deacetylase 3 1
- 10.1039/C4MD00211C Histone deacetylase 2 1
- 10.1039/C4MD00211C Histone deacetylase 1 1
- 10.1039/C4MD00211C Platelet-derived growth factor receptor beta 1
- 10.1039/C4MD00211C Platelet-derived growth factor receptor alpha 1
- 10.1039/C4MD00211C Vascular endothelial growth factor receptor 2 1
- 10.1039/C4MD00211C Vascular endothelial growth factor receptor 1 1
- 10.1039/C4MD00211C Histone deacetylase 4 1
- 10.1039/C4MD00211C Histone deacetylase 5 1
- 10.1039/C4MD00211C Histone deacetylase 6 1
- 10.1039/C4MD00211C Histone deacetylase 7 1
- 10.1039/C4MD00211C Histone deacetylase 8 1
- 10.1039/C4MD00211C Histone deacetylase 9 1

Data from ChEMBL 36 via Core Engine