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Assay Detail

CHEMBL748098

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Functional
Antagonistic activity for suppression of membrane current response elicited by fixed concentration of glycine and glutamate in Xenopus oocyte expressing N-methyl-D-aspartate glutamate receptor 1/2B
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Glutamate NMDA receptor; Grin1/Grin2b (CHEMBL2096666)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Evaluation and biological properties of reactive ligands for the mapping of the glycine site on the N-methyl-D-aspartate (NMDA) receptor.
Kreimeyer A, Laube B, Sturgess M, Goeldner M, Foucaud B.
J Med Chem (1999) 42 : 4394 -4404
PubMed 10543883 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 6.28 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL31741 1 7.75
CHEMBL139982 1 7.62
CHEMBL337851 1 7.50
CHEMBL138208 1 7.41
CHEMBL138159 1 6.81
CHEMBL139009 1 6.70
CHEMBL337346 1 6.47
CHEMBL136791 1 5.62
CHEMBL344145 1 4.62
CHEMBL137509 1 4.42
CHEMBL276907 1 4.20
CHEMBL136501 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL31741 IC50 = 18.0 nM 7.75
CHEMBL139982 IC50 = 24.0 nM 7.62
CHEMBL337851 IC50 = 32.0 nM 7.50
CHEMBL138208 IC50 = 39.0 nM 7.41
CHEMBL138159 IC50 = 155.0 nM 6.81
CHEMBL139009 IC50 = 200.0 nM 6.70
CHEMBL337346 IC50 = 335.0 nM 6.47
CHEMBL136791 IC50 = 2410.0 nM 5.62
CHEMBL344145 IC50 = 24000.0 nM 4.62
CHEMBL137509 IC50 = 38000.0 nM 4.42
CHEMBL276907 IC50 = 63000.0 nM 4.20
CHEMBL136501 IC50 > 100000.0 nM -