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Assay Detail

CHEMBL640417

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

Binding
Compound was evaluated for the inhibition of binding of [3H]AMPA to the AMPA receptor
5
Total Activities
5
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

Resolution, absolute stereochemistry, and pharmacology of the S-(+)- and R-(-)-isomers of the apparent partial AMPA receptor agonist (R,S)-2-amino-3-(3-hydroxy-5-phenylisoxazol-4-yl)propionic acid [(R,S)-APPA].
Ebert B, Lenz S, Brehm L, Bregnedal P, Hansen JJ, Frederiksen K, Bøgesø KP, Krogsgaard-Larsen P.
J Med Chem (1994) 37 : 878 -884
PubMed 7512140 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.53 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 7.40
CHEMBL83720 1 5.22
CHEMBL275040 KAINIC ACID 2.0 1 5.22
CHEMBL353261 1 4.28
CHEMBL315203 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA IC50 = 40.0 nM 7.40
CHEMBL83720 IC50 = 6000.0 nM 5.22
CHEMBL275040 KAINIC ACID IC50 = 6000.0 nM 5.22
CHEMBL353261 IC50 = 53000.0 nM 4.28
CHEMBL315203 IC50 > 100000.0 nM -