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Assay Detail

CHEMBL702871

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

Binding
In vitro inhibition of [3H]KAIN binding to Ionotropic glutamate receptor kainate.
20
Total Activities
20
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, kainate (CHEMBL2094119)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Synthesis and pharmacology of highly selective carboxy and phosphono isoxazole amino acid AMPA receptor antagonists.
Madsen U, Bang-Andersen B, Brehm L, Christensen IT, Ebert B, Kristoffersen IT, Lang Y, Krogsgaard-Larsen P.
J Med Chem (1996) 39 : 1682 -1691
PubMed 8648608 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.81 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275040 KAINIC ACID 2.0 1 7.80
CHEMBL9790 1 5.82
CHEMBL295310 1 -
CHEMBL296705 1 -
CHEMBL298469 1 -
CHEMBL48054 1 -
CHEMBL47945 1 -
CHEMBL295692 1 -
CHEMBL297648 1 -
CHEMBL291274 1 -
CHEMBL44777 1 -
CHEMBL48037 1 -
CHEMBL48038 1 -
CHEMBL45698 1 -
CHEMBL298490 1 -
CHEMBL42885 1 -
CHEMBL44059 1 -
CHEMBL297999 1 -
CHEMBL265301 1 -
CHEMBL295778 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275040 KAINIC ACID IC50 = 16.0 nM 7.80
CHEMBL9790 IC50 = 1500.0 nM 5.82
CHEMBL295310 IC50 > 100000.0 nM -
CHEMBL296705 IC50 > 100000.0 nM -
CHEMBL298469 IC50 > 100000.0 nM -
CHEMBL48054 IC50 > 100000.0 nM -
CHEMBL47945 IC50 > 100000.0 nM -
CHEMBL295692 IC50 > 100000.0 nM -
CHEMBL297648 IC50 > 100000.0 nM -
CHEMBL291274 IC50 > 100000.0 nM -
CHEMBL44777 IC50 > 100000.0 nM -
CHEMBL48037 IC50 > 100000.0 nM -
CHEMBL48038 IC50 > 100000.0 nM -
CHEMBL45698 IC50 > 100000.0 nM -
CHEMBL298490 IC50 > 100000.0 nM -
CHEMBL42885 IC50 > 100000.0 nM -
CHEMBL44059 IC50 > 100000.0 nM -
CHEMBL297999 IC50 > 100000.0 nM -
CHEMBL265301 IC50 > 100000.0 nM -
CHEMBL295778 IC50 > 100000.0 nM -