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Compound Detail

CHEMBL1215292

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COc1ccc2nc(/C=C/c3cccc([N+](=O)[O-])c3)n(-c3ccc(C(=O)O)cc3)c(=O)c2c1

Basic Information

ChEMBL ID CHEMBL1215292
Phase Preclinical
Structure Type MOL
InChI Key GNLVJIICVWDSNI-LFYBBSHMSA-N
4
Targets
7
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

443.4
MW (Da)
4.17
ALogP
7
HBA
1
HBD
124.6
PSA (Ų)
0.35
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H17N3O6
MW 443.42
Aromatic Rings 4
Heavy Atoms 33
NP-Likeness -1.09

Activity Summary

IC50 7 meas. best 5.52

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ionotropic glutamate receptor NMDA 1/2D
CHEMBL3038506
IC50 5.52 5.52 3000.0 1
Glutamate receptor ionotropic, NMDA 2D
CHEMBL2591
IC50 5.41 5.41 3900.0 1
Glutamate NMDA receptor; Grin1/Grin2c
CHEMBL2096911
IC50 5.22 5.22 6000.0 1
Glutamate receptor ionotropic, NMDA 2C
CHEMBL4109
IC50 5.15 5.15 7100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20684595 10.1021/jm100027p Unchecked 3
20684595 10.1021/jm100027p Glutamate NMDA receptor; Grin1/Grin2a 1
20684595 10.1021/jm100027p Glutamate NMDA receptor; Grin1/Grin2b 1
20684595 10.1021/jm100027p Glutamate NMDA receptor; Grin1/Grin2c 1
20684595 10.1021/jm100027p Ionotropic glutamate receptor NMDA 1/2D 1
20684595 10.1021/jm100027p Glutamate receptor 1 1
29446949 10.1021/acs.jmedchem.7b01640 Glutamate receptor ionotropic, NMDA 2D 1
29446949 10.1021/acs.jmedchem.7b01640 Glutamate receptor ionotropic, NMDA 2C 1
29446949 10.1021/acs.jmedchem.7b01640 Glutamate receptor ionotropic, NMDA 2B 1
29446949 10.1021/acs.jmedchem.7b01640 Glutamate receptor ionotropic, NMDA 2A 1

Data from ChEMBL 36 via Core Engine