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Compound Detail

CHEMBL3828218

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CN(Cc1nc2c(N3CCOCC3)nc(-c3ccc(N)cc3)nc2n1C1CCCC1)c1ncc(C(=O)NO)cn1

Basic Information

ChEMBL ID CHEMBL3828218
Phase Preclinical
Structure Type MOL
InChI Key DZTRXWBNYFRNIH-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

544.6
MW (Da)
2.57
ALogP
12
HBA
3
HBD
160.4
PSA (Ų)
0.18
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H32N10O3
MW 544.62
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.47

Activity Summary

IC50 1 meas. best 6.72

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 6.72 6.72 190.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 1 IC50 = 190.0 nM 6.72 Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 exp... 27186676

Literature References

PubMed DOI Target Context # Activities
27186676 10.1021/acs.jmedchem.6b00579 Histone deacetylase 1 1
27186676 10.1021/acs.jmedchem.6b00579 PI3-kinase p110-alpha/p85-alpha 1

Data from ChEMBL 36 via Core Engine