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Assay Detail

CHEMBL751621

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Compound was evaluated for its ability to displace [3H]CCP binding for NMDA receptor
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Excitatory amino acids: 6-phosphonomethyltetrahydro-4-pyrimidinecarboxylic acids and their acyclic analogues are competitive N-methyl-D-aspartic acid receptor antagonists.
Bigge CF, Wu J, Drummond JT, Coughenour LL, Hanchin CM
Bioorg Med Chem Lett (1992) 2 : 207 -212
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.47 7.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL39664 SELFOTEL 2.0 1 7.62
CHEMBL22304 1 7.55
CHEMBL302889 1 6.89
CHEMBL304704 1 6.62
CHEMBL68347 1 6.38
CHEMBL293473 1 5.84
CHEMBL67775 1 5.64
CHEMBL67244 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL39664 SELFOTEL IC50 = 24.0 nM 7.62
CHEMBL22304 IC50 = 28.0 nM 7.55
CHEMBL302889 IC50 = 130.0 nM 6.89
CHEMBL304704 IC50 = 240.0 nM 6.62
CHEMBL68347 IC50 = 420.0 nM 6.38
CHEMBL293473 IC50 = 1440.0 nM 5.84
CHEMBL67775 IC50 = 2270.0 nM 5.64
CHEMBL67244 IC50 = 5950.0 nM 5.22