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Assay Detail

CHEMBL748771

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

Binding
Displacement of [3H]-5-7 dichlorokynurenic acid ([3H]- DCKA) from N-methyl-D-aspartate glutamate receptor glycine site of rat brain membrane homogenate
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Brain
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

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
Ki 13 7.35 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139982 1 8.15
CHEMBL138208 1 7.86
CHEMBL31741 1 7.85
CHEMBL337346 1 7.62
CHEMBL136791 1 7.62
CHEMBL337851 1 7.57
CHEMBL138159 1 7.38
CHEMBL139009 1 7.32
CHEMBL344145 1 7.19
CHEMBL136501 1 6.67
CHEMBL137509 1 6.56
CHEMBL276907 1 6.37
CHEMBL138491 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139982 Ki = 7.1 nM 8.15
CHEMBL138208 Ki = 13.8 nM 7.86
CHEMBL31741 Ki = 14.0 nM 7.85
CHEMBL337346 Ki = 24.0 nM 7.62
CHEMBL136791 Ki = 24.2 nM 7.62
CHEMBL337851 Ki = 26.8 nM 7.57
CHEMBL138159 Ki = 42.0 nM 7.38
CHEMBL139009 Ki = 47.6 nM 7.32
CHEMBL344145 Ki = 64.3 nM 7.19
CHEMBL136501 Ki = 216.0 nM 6.67
CHEMBL137509 Ki = 278.0 nM 6.56
CHEMBL276907 Ki = 427.0 nM 6.37
CHEMBL138491 Ki > 1000.0 nM -