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Compound Detail

CHEMBL419045

GAVESTINEL SODIUM
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O=C(/C=C/c1c(C(=O)[O-])[nH]c2cc(Cl)cc(Cl)c12)Nc1ccccc1.[Na+]

Basic Information

ChEMBL ID CHEMBL419045
Name GAVESTINEL SODIUM
Phase Preclinical
Structure Type MOL
InChI Key GRSDSTMFQHAESM-UHDJGPCESA-M
Parent Compound CHEMBL44793
Active Moiety CHEMBL44793
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

375.2
MW (Da)
4.82
ALogP
2
HBA
3
HBD
82.2
PSA (Ų)
0.57
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 C18H11Cl2N2NaO3
MW 397.19
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -0.88

Activity Summary

IC50 2 meas. best 7.82
Ki 2 meas. best 8.5

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate receptor ionotropic, NMDA 1
CHEMBL330
Ki 8.5 8.5 3.2 1
Glutamate NMDA receptor
CHEMBL1907608
Ki 8.49 8.49 3.2 1
Glutamate NMDA receptor
CHEMBL1907608
IC50 7.82 7.82 15.2 1
Rattus norvegicus
CHEMBL376
IC50 6.58 6.58 262.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15715469 10.1021/jm0491849 Rattus norvegicus 6
15715469 10.1021/jm0491849 Mus musculus 3
9083472 10.1021/jm960644a Glutamate receptor ionotropic, NMDA 1 2
9083472 10.1021/jm960644a Mus musculus 2
10479281 10.1021/jm980576n Mus musculus 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
10479281 10.1021/jm980576n Glutamate NMDA receptor 1
10479281 10.1021/jm980576n Albumin 1
15715469 10.1021/jm0491849 Glutamate NMDA receptor 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1

Data from ChEMBL 36 via Core Engine