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Assay Detail

CHEMBL748770

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

Binding
Displacement of [3H]glycine from glycine site on the NMDA receptor.
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and excitatory amino acid pharmacology of a series of heterocyclic-fused quinoxalinones and quinazolinones.
McQuaid LA, Smith EC, South KK, Mitch CH, Schoepp DD, True RA, Calligaro DO, O'Malley PJ, Lodge D, Ornstein PL.
J Med Chem (1992) 35 : 3319 -3324
PubMed 1382133 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 18 5.94 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL50267 1 7.40
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE 1 6.68
CHEMBL112386 1 6.20
CHEMBL325124 1 5.90
CHEMBL112193 1 5.83
CHEMBL323414 1 5.54
CHEMBL113270 1 5.41
CHEMBL109207 1 5.34
CHEMBL321171 1 5.13
CHEMBL113107 1 -
CHEMBL322734 1 -
CHEMBL112431 1 -
CHEMBL110799 1 -
CHEMBL113588 1 -
CHEMBL322354 1 -
CHEMBL114498 1 -
CHEMBL325557 1 -
CHEMBL112014 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL50267 Ki = 40.0 nM 7.40
CHEMBL284028 2,3-DIHYDROXY-6,7-DICHLOROQUINOXALINE Ki = 210.0 nM 6.68
CHEMBL112386 Ki = 630.0 nM 6.20
CHEMBL325124 Ki = 1260.0 nM 5.90
CHEMBL112193 Ki = 1480.0 nM 5.83
CHEMBL323414 Ki = 2850.0 nM 5.54
CHEMBL113270 Ki = 3920.0 nM 5.41
CHEMBL109207 Ki = 4580.0 nM 5.34
CHEMBL321171 Ki = 7350.0 nM 5.13
CHEMBL113107 Ki > 10000.0 nM -
CHEMBL322734 Ki > 10000.0 nM -
CHEMBL112431 Ki > 10000.0 nM -
CHEMBL110799 Ki > 10000.0 nM -
CHEMBL113588 Ki > 10000.0 nM -
CHEMBL322354 Ki > 10000.0 nM -
CHEMBL114498 Ki > 10000.0 nM -
CHEMBL325557 Ki > 10000.0 nM -
CHEMBL112014 Ki > 10000.0 nM -