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Assay Detail

CHEMBL747201

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

Binding
Inhibition of [3H]glycine binding to rat cortical membranes
20
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor ionotropic, NMDA 1 (CHEMBL330)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Derivatives of 1-hydroxy-3-aminopyrrolidin-2-one (HA-966). Partial agonists at the glycine site of the NMDA receptor
Leeson PD, Williams BJ, Rowley M, Moore KW, Baker R, Kemp JA, Priestley T, Foster AC, Donald AE
Bioorg Med Chem Lett (1993) 3 : 71 -76
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 4.96 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131567 1 5.89
CHEMBL283819 2 5.85
CHEMBL335231 2 4.90
CHEMBL162442 1 4.82
CHEMBL337030 1 4.72
CHEMBL2115569 1 4.32
CHEMBL165945 1 4.07
CHEMBL350810 1 -
CHEMBL165719 1 -
CHEMBL351085 1 -
CHEMBL433711 1 -
CHEMBL350522 1 -
CHEMBL162177 1 -
CHEMBL350158 1 -
CHEMBL351464 1 -
CHEMBL353569 1 -
CHEMBL2115541 1 -
CHEMBL164785 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131567 IC50 = 1300.0 nM 5.89
CHEMBL283819 IC50 = 1400.0 nM 5.85
CHEMBL283819 IC50 = 2900.0 nM 5.54
CHEMBL335231 IC50 = 12500.0 nM 4.90
CHEMBL162442 IC50 = 15000.0 nM 4.82
CHEMBL337030 IC50 = 19000.0 nM 4.72
CHEMBL335231 IC50 = 27200.0 nM 4.57
CHEMBL2115569 IC50 = 48000.0 nM 4.32
CHEMBL165945 IC50 = 86000.0 nM 4.07
CHEMBL350810 IC50 > 100000.0 nM -
CHEMBL165719 IC50 = 313000.0 nM -
CHEMBL351085 IC50 > 100000.0 nM -
CHEMBL433711 IC50 > 100000.0 nM -
CHEMBL350522 IC50 > 100000.0 nM -
CHEMBL162177 IC50 > 100000.0 nM -
CHEMBL350158 IC50 > 100000.0 nM -
CHEMBL351464 IC50 = 339000.0 nM -
CHEMBL353569 IC50 > 100000.0 nM -
CHEMBL2115541 IC50 > 100000.0 nM -
CHEMBL164785 IC50 > 100000.0 nM -