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Assay Detail

CHEMBL697882

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

Binding
Binding affinity for Ionotropic glutamate receptor AMPA using [3H]- AMPA
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Novel 1-hydroxyazole bioisosteres of glutamic acid. Synthesis, protolytic properties, and pharmacology.
Stensbøl TB, Uhlmann P, Morel S, Eriksen BL, Felding J, Kromann H, Hermit MB, Greenwood JR, Braüner-Osborne H, Madsen U, Junager F, Krogsgaard-Larsen P, Begtrup M, Vedsø P.
J Med Chem (2002) 45 : 19 -31
PubMed 11754576 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.47 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL13378 (R,S)-AMPA 1 7.40
CHEMBL104208 1 6.89
CHEMBL321164 1 6.82
CHEMBL317234 1 6.57
CHEMBL107160 1 5.58
CHEMBL320290 1 5.57
CHEMBL104197 1 -
CHEMBL104065 1 -
CHEMBL102612 1 -
CHEMBL323289 1 -
CHEMBL104039 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL13378 (R,S)-AMPA IC50 = 40.0 nM 7.40
CHEMBL104208 IC50 = 130.0 nM 6.89
CHEMBL321164 IC50 = 150.0 nM 6.82
CHEMBL317234 IC50 = 270.0 nM 6.57
CHEMBL107160 IC50 = 2600.0 nM 5.58
CHEMBL320290 IC50 = 2700.0 nM 5.57
CHEMBL104197 IC50 > 100000.0 nM -
CHEMBL104065 IC50 > 100000.0 nM -
CHEMBL102612 IC50 > 100000.0 nM -
CHEMBL323289 IC50 > 100000.0 nM -
CHEMBL104039 IC50 > 100000.0 nM -