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Assay Detail

CHEMBL803551

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

Functional
In vitro antagonist activity by its ability to inhibit glutamate-induced accumulation of [45Ca2+]- in cultured rat cortical neurons.
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Exploration of N-phosphonoalkyl-, N-phosphonoalkenyl-, and N-(phosphonoalkyl)phenyl-spaced alpha-amino acids as competitive N-methyl-D-aspartic acid antagonists.
Bigge CF, Johnson G, Ortwine DF, Drummond JT, Retz DM, Brahce LJ, Coughenour LL, Marcoux FW, Probert AW.
J Med Chem (1992) 35 : 1371 -1384
PubMed 1533423 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 4.81 5.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22304 1 5.62
CHEMBL29244 1 5.28
CHEMBL28862 1 5.21
CHEMBL29255 1 4.78
CHEMBL274440 AP-7 1 4.52
CHEMBL3349424 1 4.44
CHEMBL28609 1 4.40
CHEMBL27735 1 4.23
CHEMBL29193 1 -
CHEMBL443231 1 -
CHEMBL284880 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22304 IC50 = 2400.0 nM 5.62
CHEMBL29244 IC50 = 5200.0 nM 5.28
CHEMBL28862 IC50 = 6100.0 nM 5.21
CHEMBL29255 IC50 = 16700.0 nM 4.78
CHEMBL274440 AP-7 IC50 = 30000.0 nM 4.52
CHEMBL3349424 IC50 = 36000.0 nM 4.44
CHEMBL28609 IC50 = 40000.0 nM 4.40
CHEMBL27735 IC50 = 59000.0 nM 4.23
CHEMBL29193 IC50 = 144000.0 nM -
CHEMBL443231 IC50 > 250000.0 nM -
CHEMBL284880 IC50 = 137000.0 nM -