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Compound Detail

CHEMBL8992

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O=C(O)C1=NN2C(=O)Nc3ccccc3C2C1

Basic Information

ChEMBL ID CHEMBL8992
Phase Preclinical
Structure Type MOL
InChI Key WVASWHNMKDOZPG-UHFFFAOYSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

231.2
MW (Da)
1.42
ALogP
3
HBA
2
HBD
82.0
PSA (Ų)
0.77
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C11H9N3O3
MW 231.21
Aromatic Rings 1
Heavy Atoms 17
NP-Likeness -0.55

Activity Summary

Ki 4 meas. best 5.7
IC50 2 meas. best 4.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, NMDA 1
CHEMBL330
Ki 5.7 5.7 2000.0 2
Glutamate NMDA receptor
CHEMBL1907608
IC50 4.76 4.76 17500.0 1
Glutamate receptor ionotropic, kainate
CHEMBL2094119
IC50 4.71 4.71 19500.0 1
Glutamate receptor ionotropic, AMPA
CHEMBL2093871
Ki 4.02 4.02 96000.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12954059 10.1021/jm030833a Glutamate receptor ionotropic, AMPA 1
12954059 10.1021/jm030833a Glutamate receptor ionotropic, NMDA 1 1
11855983 10.1021/jm010995b Glutamate receptor ionotropic, NMDA 1 1
11855983 10.1021/jm010995b Glutamate receptor ionotropic, AMPA 1
11855983 10.1021/jm010995b Glutamate receptor ionotropic, kainate 1
11855983 10.1021/jm010995b Glutamate NMDA receptor 1

Data from ChEMBL 36 via Core Engine