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Compound Detail

CHEMBL4066293

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COc1ccc([C@@H]2C(=O)N([C@H]3CC[C@H](N)CC3)[C@H]2c2ccc(C#N)cc2)cc1

Basic Information

ChEMBL ID CHEMBL4066293
Phase Preclinical
Structure Type MOL
InChI Key QQJNACDYKNZCPI-LGGPRVQUSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

375.5
MW (Da)
3.50
ALogP
4
HBA
1
HBD
79.3
PSA (Ų)
0.83
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H25N3O2
MW 375.47
Aromatic Rings 2
Heavy Atoms 28
NP-Likeness -0.46

Activity Summary

Kd 1 meas. best 4.28

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific histone demethylase 1A
CHEMBL6136
Kd 4.28 4.28 53000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Lysine-specific histone demethylase 1A Kd = 53000.0 nM 4.28 Binding affinity to LSD1 (unknown origin) by SPR analysis 28927796

Literature References

PubMed DOI Target Context # Activities
28927796 10.1016/j.bmcl.2017.08.052 Lysine-specific histone demethylase 1A 2

Data from ChEMBL 36 via Core Engine