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Compound Detail

CHEMBL534486

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COc1cccc(OC)c1C/N=C(\N)c1cc2ccccc2[nH]1.Cl

Basic Information

ChEMBL ID CHEMBL534486
Phase Preclinical
Structure Type MOL
InChI Key XWPVMEWYGZVHAN-UHFFFAOYSA-N
Parent Compound CHEMBL1187939
Active Moiety CHEMBL1187939
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

309.4
MW (Da)
3.09
ALogP
3
HBA
2
HBD
72.6
PSA (Ų)
0.56
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20ClN3O2
MW 345.83
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.32

Activity Summary

IC50 1 meas. best 8.27

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate NMDA receptor
CHEMBL1907608
IC50 8.27 8.27 5.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutamate NMDA receptor IC50 = 5.4 nM 8.27 Inhibition of NMDA-evoked intracellular calcium increase in rat cortical cells 16213709

Literature References

PubMed DOI Target Context # Activities
16213709 10.1016/j.bmcl.2005.08.110 Glutamate NMDA receptor 1
16213709 10.1016/j.bmcl.2005.08.110 Glutamate NMDA receptor; GRIN1/GRIN2A 1

Data from ChEMBL 36 via Core Engine