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Assay Detail

CHEMBL1018988

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 membranes
14
Total Activities
8
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis and biological evaluation of novel bicyclo[1.1.1]pentane-based omega-acidic amino acids as glutamate receptors ligands.
Filosa R, Carmela Fulco M, Marinozzi M, Giacchè N, Macchiarulo A, Peduto A, Massa A, de Caprariis P, Thomsen C, Christoffersen CT, Pellicciari R.
Bioorg Med Chem (2009) 17 : 242 -250
PubMed 19042134 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.37 6.54
logKi 5 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.54
CHEMBL467235 2 6.14
CHEMBL445241 2 5.34
CHEMBL450025 2 4.54
CHEMBL448885 2 4.28
CHEMBL444718 2 -
CHEMBL467234 2 -
CHEMBL33567 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL575060 GLUTAMIC ACID Ki = 290.0 nM 6.54
CHEMBL467235 Ki = 730.0 nM 6.14
CHEMBL445241 Ki = 4600.0 nM 5.34
CHEMBL450025 Ki = 29000.0 nM 4.54
CHEMBL448885 Ki = 53000.0 nM 4.28
CHEMBL444718 Ki = 300000.0 nM -
CHEMBL467234 logKi = 2.09 -
CHEMBL33567 Ki > 300000.0 nM -
CHEMBL444718 logKi = 2.48 -
CHEMBL450025 logKi = 1.46 -
CHEMBL467234 Ki = 124000.0 nM -
CHEMBL448885 logKi = 1.72 -
CHEMBL445241 logKi = 0.66 -
CHEMBL467235 Ki = 724435960.07 nM -