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Assay Detail

CHEMBL4351310

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

Binding
Displacement of [3H]CGP39653 from NMDA receptor in rat brain synaptic cortical membranes after 60 mins by scintillation counting method
9
Total Activities
8
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

Use of the 4-Hydroxytriazole Moiety as a Bioisosteric Tool in the Development of Ionotropic Glutamate Receptor Ligands.
Sainas S, Temperini P, Farnsworth JC, Yi F, Møllerud S, Jensen AA, Nielsen B, Passoni A, Kastrup JS, Hansen KB, Boschi D, Pickering DS, Clausen RP, Lolli ML.
J Med Chem (2019) 62 : 4467 -4482
PubMed 30943028 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.22 6.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.70
CHEMBL291278 N-METHYL-D-ASPARTIC ACID (NMDA) 2.0 1 5.21
CHEMBL4444367 2 4.49
CHEMBL4451018 1 -
CHEMBL4448290 1 -
CHEMBL4556711 1 -
CHEMBL4529665 1 -
CHEMBL275040 KAINIC ACID 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID Ki = 200.0 nM 6.70
CHEMBL291278 N-METHYL-D-ASPARTIC ACID (NMDA) Ki = 6200.0 nM 5.21
CHEMBL4444367 Ki = 32359.37 nM 4.49
CHEMBL4444367 Ki = 34000.0 nM 4.47
CHEMBL4451018 Ki > 100000.0 nM -
CHEMBL4448290 Ki > 100000.0 nM -
CHEMBL4556711 Ki > 100000.0 nM -
CHEMBL4529665 Ki > 100000.0 nM -
CHEMBL275040 KAINIC ACID Ki > 100000.0 nM -