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Assay Detail

CHEMBL697893

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

Binding
Compound was evaluated for the inhibition of [3H]AMPA binding to Ionotropic glutamate receptor AMPA from rat brain synaptic membrane.
10
Total Activities
10
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

Syntheses of trans-3-substituted-CCG-IV analogs and their characterization to ionotropic glutamate receptors
Shimamoto K, Shigeri Y, Nakajima T, Yumoto N, Yoshikawa S, Ohfune Y
Bioorg Med Chem Lett (1996) 6 : 2381 -2386
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.07 8.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL276815 (S)-AMPA 1 8.21
CHEMBL575060 GLUTAMIC ACID 3.0 1 6.82
CHEMBL282842 1 6.22
CHEMBL312192 1 5.70
CHEMBL275040 KAINIC ACID 2.0 1 5.70
CHEMBL75640 1 5.40
CHEMBL80628 1 5.40
CHEMBL80376 1 5.12
CHEMBL291278 N-METHYL-D-ASPARTIC ACID (NMDA) 2.0 1 -
CHEMBL433333 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL276815 (S)-AMPA IC50 = 6.2 nM 8.21
CHEMBL575060 GLUTAMIC ACID IC50 = 150.0 nM 6.82
CHEMBL282842 IC50 = 600.0 nM 6.22
CHEMBL312192 IC50 = 2000.0 nM 5.70
CHEMBL275040 KAINIC ACID IC50 = 2000.0 nM 5.70
CHEMBL75640 IC50 = 4000.0 nM 5.40
CHEMBL80628 IC50 = 4000.0 nM 5.40
CHEMBL80376 IC50 = 7500.0 nM 5.12
CHEMBL291278 N-METHYL-D-ASPARTIC ACID (NMDA) IC50 > 100000.0 nM -
CHEMBL433333 IC50 > 100000.0 nM -