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Compound Detail

CHEMBL1819265

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O=C(/C=C/c1ccc(CNCCc2c[nH]c3ccncc23)cc1)NO

Basic Information

ChEMBL ID CHEMBL1819265
Phase Preclinical
Structure Type MOL
InChI Key GYVBOCYZRIRHIA-AATRIKPKSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

336.4
MW (Da)
2.41
ALogP
4
HBA
4
HBD
90.0
PSA (Ų)
0.23
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20N4O2
MW 336.40
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.40

Activity Summary

IC50 2 meas. best 7.68

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone deacetylase 1
CHEMBL325
IC50 7.68 7.68 21.0 1
HCT-116
CHEMBL394
IC50 5.38 5.38 4120.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone deacetylase 1 IC50 = 21.0 nM 7.68 Inhibition of HDAC1 21650221
HCT-116 IC50 = 4120.0 nM 5.38 Antiproliferative activity against human HCT116 cells assessed as growth inhibit... 21650221

Literature References

PubMed DOI Target Context # Activities
21650221 10.1021/jm200388e Histone deacetylase 1 1
21650221 10.1021/jm200388e HCT-116 1
21650221 10.1021/jm200388e Voltage-gated inwardly rectifying potassium channel KCNH2 1
21650221 10.1021/jm200388e ADMET 1

Data from ChEMBL 36 via Core Engine