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Assay Detail

CHEMBL752506

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

Binding
Inhibition by displacing [3H]-Glycine of N-methyl-D-aspartate glutamate receptor 1 in rat cortical membranes
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological evaluation of a new set of pyrazolo[1,5-c]quinazoline-2-carboxylates as novel excitatory amino acid antagonists.
Varano F, Catarzi D, Colotta V, Filacchioni G, Galli A, Costagli C, Carlà V.
J Med Chem (2002) 45 : 1035 -1044
PubMed 11855983 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 5.53 7.13

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274588 1 7.13
CHEMBL8693 1 6.72
CHEMBL8829 1 5.09
CHEMBL267276 TQX-173 1 4.47
CHEMBL267006 1 4.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274588 Ki = 74.0 nM 7.13
CHEMBL8693 Ki = 190.0 nM 6.72
CHEMBL8829 Ki = 8200.0 nM 5.09
CHEMBL267276 TQX-173 Ki = 33500.0 nM 4.47
CHEMBL267006 Ki = 57000.0 nM 4.24