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Assay Detail

CHEMBL1013086

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

Binding
Displacement of [3H]CGP 39653 from NMDA receptor in rat synaptosomes
13
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Chemo-enzymatic synthesis of a series of 2,4-syn-functionalized (S)-glutamate analogues: new insight into the structure-activity relation of ionotropic glutamate receptor subtypes 5, 6, and 7.
Sagot E, Pickering DS, Pu X, Umberti M, Stensbøl TB, Nielsen B, Chapelet M, Bolte J, Gefflaut T, Bunch L.
J Med Chem (2008) 51 : 4093 -4103
PubMed 18578478 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 13 4.46 4.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL500448 2 4.82
CHEMBL446256 2 4.59
CHEMBL482081 2 4.28
CHEMBL518313 2 4.14
CHEMBL479805 1 -
CHEMBL500042 1 -
CHEMBL479804 1 -
CHEMBL482080 1 -
CHEMBL479797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL500448 Ki = 15000.0 nM 4.82
CHEMBL500448 Ki = 15135.61 nM 4.82
CHEMBL446256 Ki = 25703.96 nM 4.59
CHEMBL446256 Ki = 26000.0 nM 4.58
CHEMBL482081 Ki = 52000.0 nM 4.28
CHEMBL482081 Ki = 52480.75 nM 4.28
CHEMBL518313 Ki = 72000.0 nM 4.14
CHEMBL518313 Ki = 72443.6 nM 4.14
CHEMBL479805 Ki > 100000.0 nM -
CHEMBL500042 Ki > 100000.0 nM -
CHEMBL479804 Ki > 100000.0 nM -
CHEMBL482080 Ki > 100000.0 nM -
CHEMBL479797 Ki > 100000.0 nM -