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Assay Detail

CHEMBL1671028

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

Binding
Displacement of [3H]CGP 39653 from NMDA receptor in Sprague-Dawley rat brain synaptic membrane after 60 mins by scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Synthesis of new isoxazoline-based acidic amino acids and investigation of their affinity and selectivity profile at ionotropic glutamate receptors.
Pinto A, Conti P, Grazioso G, Tamborini L, Madsen U, Nielsen B, De Micheli C.
Eur J Med Chem (2011) 46 : 787 -793
PubMed 21220180 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.56 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL197633 1 6.68
CHEMBL421402 1 6.43
CHEMBL199181 1 6.02
CHEMBL1669239 1 5.52
CHEMBL1669240 1 5.29
CHEMBL1669237 1 4.75
CHEMBL1669238 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL197633 Ki = 210.0 nM 6.68
CHEMBL421402 Ki = 370.0 nM 6.43
CHEMBL199181 Ki = 960.0 nM 6.02
CHEMBL1669239 Ki = 3000.0 nM 5.52
CHEMBL1669240 Ki = 5100.0 nM 5.29
CHEMBL1669237 Ki = 18000.0 nM 4.75
CHEMBL1669238 Ki = 60000.0 nM 4.22