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Assay Detail

CHEMBL747490

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

Binding
Binding affinity towards NMDA receptor by displacement of [3H]CGP-39653 radioligand.
4
Total Activities
4
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

A rational approach to the design of selective substrates and potent nontransportable inhibitors of the excitatory amino acid transporter EAAC1 (EAAT3). new glutamate and aspartate analogues as potential neuroprotective agents.
Campiani G, De Angelis M, Armaroli S, Fattorusso C, Catalanotti B, Ramunno A, Nacci V, Novellino E, Grewer C, Ionescu D, Rauen T, Griffiths R, Sinclair C, Fumagalli E, Mennini T.
J Med Chem (2001) 44 : 2507 -2510
PubMed 11472204 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.90 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.70
CHEMBL86273 1 6.31
CHEMBL82172 1 5.52
CHEMBL82935 1 5.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID Ki = 200.0 nM 6.70
CHEMBL86273 Ki = 490.0 nM 6.31
CHEMBL82172 Ki = 3000.0 nM 5.52
CHEMBL82935 Ki = 9000.0 nM 5.05