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Compound Detail

CHEMBL4469253

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CC(C)c1c(-c2cnn(C3CC3)c2)[nH]c2c(C#N)cnn2c1=O

Basic Information

ChEMBL ID CHEMBL4469253
Phase Preclinical
Structure Type MOL
InChI Key HVWZVXNIDTTWSM-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

308.4
MW (Da)
2.22
ALogP
6
HBA
1
HBD
91.8
PSA (Ų)
0.80
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 C16H16N6O
MW 308.35
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.11

Activity Summary

EC50 1 meas. best 5.89
IC50 1 meas. best 8.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Lysine-specific demethylase 5A
CHEMBL2424504
IC50 8.1 8.1 7.9 1
Unchecked
CHEMBL612545
EC50 5.89 5.89 1300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27406798 10.1016/j.bmcl.2016.06.078 ADMET 2
27406798 10.1016/j.bmcl.2016.06.078 No relevant target 1
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