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Compound Detail

CHEMBL4577929

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C=CC(C)c1c(-c2ccccc2)[nH]c2c(C#N)cnn2c1=O

Basic Information

ChEMBL ID CHEMBL4577929
Phase Preclinical
Structure Type MOL
InChI Key GMGWCLPOEYUQNF-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

290.3
MW (Da)
2.85
ALogP
4
HBA
1
HBD
74.0
PSA (Ų)
0.75
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C17H14N4O
MW 290.33
Aromatic Rings 3
Heavy Atoms 22
NP-Likeness -0.75

Activity Summary

EC50 1 meas. best 4.79
IC50 1 meas. best 7.81

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific demethylase 5A
CHEMBL2424504
IC50 7.81 7.81 15.5 1
Unchecked
CHEMBL612545
EC50 4.79 4.79 16400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27406798 10.1016/j.bmcl.2016.06.078 Unchecked 1
27406798 10.1016/j.bmcl.2016.06.078 Lysine-specific demethylase 5A 1

Data from ChEMBL 36 via Core Engine