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Compound Detail

CHEMBL3775735

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O=C(O)c1ccc(CN2CCC(CN[C@H]3C[C@@H]3c3ccccc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL3775735
Phase Preclinical
Structure Type MOL
InChI Key LRULVYSBRWUVGR-YADHBBJMSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

364.5
MW (Da)
3.74
ALogP
3
HBA
2
HBD
52.6
PSA (Ų)
0.79
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 C23H28N2O2
MW 364.49
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.79

Activity Summary

IC50 2 meas. best 6.21

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific histone demethylase 1A
CHEMBL6136
IC50 6.21 5.99 610.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26700437 10.1021/acs.jmedchem.5b01323 Lysine-specific histone demethylase 1A 2
26700437 10.1021/acs.jmedchem.5b01323 HeLa 2
29247860 10.1016/j.ejmech.2017.12.001 SJRH30 2
29247860 10.1016/j.ejmech.2017.12.001 Lysine-specific histone demethylase 1A 2
29439916 10.1016/j.bmc.2018.01.031 HCT-116 1
29439916 10.1016/j.bmc.2018.01.031 PA-1 1
29439916 10.1016/j.bmc.2018.01.031 F9 1
29439916 10.1016/j.bmc.2018.01.031 NIH3T3 1

Data from ChEMBL 36 via Core Engine