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Assay Detail

CHEMBL644174

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

Binding
In vitro inhibition of binding of [3H]AMPA towards AMPA receptor in rat
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
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 34 6.21 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL315547 1 7.17
CHEMBL310892 1 7.16
CHEMBL85900 1 7.10
CHEMBL538017 1 6.92
CHEMBL543364 1 6.80
CHEMBL82626 1 6.77
CHEMBL86904 1 6.70
CHEMBL82005 1 6.70
CHEMBL84775 1 6.54
CHEMBL555079 1 6.54
CHEMBL85203 1 6.51
CHEMBL539019 1 6.51
CHEMBL553895 1 6.47
CHEMBL84990 1 6.42
CHEMBL553775 1 6.42
CHEMBL543367 1 6.42
CHEMBL82513 1 6.27
CHEMBL85211 1 6.21
CHEMBL82071 1 6.19
CHEMBL554460 1 5.92
CHEMBL82963 1 5.92
CHEMBL83923 1 5.89
CHEMBL313910 1 5.89
CHEMBL84778 1 5.85
CHEMBL543132 1 5.72
CHEMBL83474 1 5.70
CHEMBL87416 1 5.70
CHEMBL83198 1 5.62
CHEMBL86313 1 5.52
CHEMBL84987 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL315547 IC50 = 68.0 nM 7.17
CHEMBL310892 IC50 = 70.0 nM 7.16
CHEMBL85900 IC50 = 80.0 nM 7.10
CHEMBL538017 IC50 = 120.0 nM 6.92
CHEMBL543364 IC50 = 160.0 nM 6.80
CHEMBL82626 IC50 = 170.0 nM 6.77
CHEMBL86904 IC50 = 200.0 nM 6.70
CHEMBL82005 IC50 = 200.0 nM 6.70
CHEMBL84775 IC50 = 290.0 nM 6.54
CHEMBL555079 IC50 = 290.0 nM 6.54
CHEMBL85203 IC50 = 310.0 nM 6.51
CHEMBL539019 IC50 = 310.0 nM 6.51
CHEMBL553895 IC50 = 340.0 nM 6.47
CHEMBL543367 IC50 = 380.0 nM 6.42
CHEMBL553775 IC50 = 380.0 nM 6.42
CHEMBL84990 IC50 = 380.0 nM 6.42
CHEMBL82513 IC50 = 540.0 nM 6.27
CHEMBL85211 IC50 = 610.0 nM 6.21
CHEMBL82071 IC50 = 640.0 nM 6.19
CHEMBL554460 IC50 = 1200.0 nM 5.92
CHEMBL82963 IC50 = 1200.0 nM 5.92
CHEMBL83923 IC50 = 1300.0 nM 5.89
CHEMBL313910 IC50 = 1300.0 nM 5.89
CHEMBL84778 IC50 = 1400.0 nM 5.85
CHEMBL543132 IC50 = 1900.0 nM 5.72
CHEMBL83474 IC50 = 2000.0 nM 5.70
CHEMBL87416 IC50 = 2000.0 nM 5.70
CHEMBL83198 IC50 = 2400.0 nM 5.62
CHEMBL86313 IC50 = 3000.0 nM 5.52
CHEMBL84987 IC50 = 3800.0 nM 5.42
CHEMBL554613 IC50 = 4300.0 nM 5.37
CHEMBL84432 IC50 = 4500.0 nM 5.35
CHEMBL543131 IC50 = 4700.0 nM 5.33
CHEMBL83360 IC50 = 105000.0 nM -