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Assay Detail

CHEMBL862169

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

Binding
Displacement of L-[3H]glutamate from glutamate receptor in rat brain synaptic membrane
16
Total Activities
16
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

New Gly-Pro-Glu (GPE) analogues: expedite solid-phase synthesis and biological activity.
Alonso De Diego SA, Gutiérrez-Rodríguez M, Pérez de Vega MJ, Casabona D, Cativiela C, González-Muñiz R, Herranz R, Cenarruzabeitia E, Frechilla D, Del Río J, Jimeno ML, García-López MT.
Bioorg Med Chem Lett (2006) 16 : 1392 -1396
PubMed 16321525 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.07 6.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL206162 1 6.32
CHEMBL203213 1 5.62
CHEMBL381831 1 5.58
CHEMBL204215 1 5.31
CHEMBL205662 1 5.27
CHEMBL380624 1 5.03
CHEMBL203239 1 4.81
CHEMBL382011 1 4.71
CHEMBL382606 1 4.66
CHEMBL203990 1 4.65
CHEMBL197084 TROFINETIDE 4.0 1 4.50
CHEMBL203622 1 4.38
CHEMBL205663 1 -
CHEMBL203518 1 -
CHEMBL380653 1 -
CHEMBL1791354 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL206162 Ki = 480.0 nM 6.32
CHEMBL203213 Ki = 2390.0 nM 5.62
CHEMBL381831 Ki = 2660.0 nM 5.58
CHEMBL204215 Ki = 4850.0 nM 5.31
CHEMBL205662 Ki = 5400.0 nM 5.27
CHEMBL380624 Ki = 9240.0 nM 5.03
CHEMBL203239 Ki = 15540.0 nM 4.81
CHEMBL382011 Ki = 19500.0 nM 4.71
CHEMBL382606 Ki = 22030.0 nM 4.66
CHEMBL203990 Ki = 22370.0 nM 4.65
CHEMBL197084 TROFINETIDE Ki = 31240.0 nM 4.50
CHEMBL203622 Ki = 41300.0 nM 4.38
CHEMBL205663 Ki > 100000.0 nM -
CHEMBL203518 Ki > 100000.0 nM -
CHEMBL380653 Ki > 100000.0 nM -
CHEMBL1791354 Ki > 100000.0 nM -