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Assay Detail

CHEMBL748572

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

Binding
Inhibition of [3H]L-689,560 binding to Glycine site of NMDA receptor of rat cortical membranes
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

2-carboxy indolines and indoles as potential glycine/NMDA antagonists: effect of five-membered ring conformation on affinity.
Rowley M, Leeson PD, Grimwood S, Foster A, Saywell K
Bioorg Med Chem Lett (1992) 2 : 1627 -1630
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.51 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL42871 1 7.57
CHEMBL43372 1 7.44
CHEMBL31344 1 7.16
CHEMBL42415 1 6.09
CHEMBL415462 1 5.75
CHEMBL43307 1 5.05
CHEMBL42416 1 -
CHEMBL42323 1 -
CHEMBL42499 1 -
CHEMBL298435 1 -
CHEMBL46910 1 -
CHEMBL42380 1 -
CHEMBL295647 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL42871 IC50 = 27.0 nM 7.57
CHEMBL43372 IC50 = 36.0 nM 7.44
CHEMBL31344 IC50 = 70.0 nM 7.16
CHEMBL42415 IC50 = 810.0 nM 6.09
CHEMBL415462 IC50 = 1780.0 nM 5.75
CHEMBL43307 IC50 = 9000.0 nM 5.05
CHEMBL42416 IC50 > 100000.0 nM -
CHEMBL42323 IC50 > 300000.0 nM -
CHEMBL42499 IC50 > 100000.0 nM -
CHEMBL298435 IC50 > 100000.0 nM -
CHEMBL46910 IC50 > 100000.0 nM -
CHEMBL42380 IC50 > 100000.0 nM -
CHEMBL295647 IC50 > 100000.0 nM -