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Assay Detail

CHEMBL749210

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

Binding
In vitro inhibition of binding of [3H]MDL-105519 towards glycine binding site of NMDA receptor in rat
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate NMDA receptor (CHEMBL1907608)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

N-phosphonoalkyl-5-aminomethylquinoxaline-2,3-diones: in vivo active AMPA and NMDA(glycine) antagonists.
Auberson YP, Acklin P, Bischoff S, Moretti R, Ofner S, Schmutz M, Veenstra SJ.
Bioorg Med Chem Lett (1999) 9 : 249 -254
PubMed 10021939 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 6.41 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL86313 1 8.22
CHEMBL82963 1 8.22
CHEMBL82626 1 7.50
CHEMBL543131 1 7.40
CHEMBL443011 1 7.35
CHEMBL83198 1 7.00
CHEMBL87710 1 6.96
CHEMBL313510 1 6.92
CHEMBL84432 1 6.92
CHEMBL83474 1 6.52
CHEMBL87416 1 6.51
CHEMBL84778 1 6.43
CHEMBL313910 1 6.38
CHEMBL85567 1 6.30
CHEMBL82513 1 6.23
CHEMBL543364 1 6.12
CHEMBL84775 1 6.00
CHEMBL543367 1 5.89
CHEMBL539019 1 5.77
CHEMBL554613 1 5.66
CHEMBL83360 1 5.48
CHEMBL310892 1 5.41
CHEMBL315547 1 5.40
CHEMBL85211 1 5.05
CHEMBL553775 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL86313 IC50 = 6.0 nM 8.22
CHEMBL82963 IC50 = 6.0 nM 8.22
CHEMBL82626 IC50 = 32.0 nM 7.50
CHEMBL543131 IC50 = 40.0 nM 7.40
CHEMBL443011 IC50 = 45.0 nM 7.35
CHEMBL83198 IC50 = 100.0 nM 7.00
CHEMBL87710 IC50 = 110.0 nM 6.96
CHEMBL313510 IC50 = 120.0 nM 6.92
CHEMBL84432 IC50 = 120.0 nM 6.92
CHEMBL83474 IC50 = 300.0 nM 6.52
CHEMBL87416 IC50 = 310.0 nM 6.51
CHEMBL84778 IC50 = 370.0 nM 6.43
CHEMBL313910 IC50 = 420.0 nM 6.38
CHEMBL85567 IC50 = 500.0 nM 6.30
CHEMBL82513 IC50 = 590.0 nM 6.23
CHEMBL543364 IC50 = 760.0 nM 6.12
CHEMBL84775 IC50 = 1000.0 nM 6.00
CHEMBL543367 IC50 = 1300.0 nM 5.89
CHEMBL539019 IC50 = 1700.0 nM 5.77
CHEMBL554613 IC50 = 2200.0 nM 5.66
CHEMBL83360 IC50 = 3300.0 nM 5.48
CHEMBL310892 IC50 = 3900.0 nM 5.41
CHEMBL315547 IC50 = 4000.0 nM 5.40
CHEMBL85211 IC50 = 9000.0 nM 5.05
CHEMBL553775 IC50 = 19000.0 nM 4.72