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Assay Detail

CHEMBL699703

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

Binding
Ability to inhibit the binding of [3H]-kainic acid radioligand to Ionotropic glutamate receptor kainate in rat brain membranes.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Glutamate receptor ionotropic, kainate (CHEMBL2094119)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

Heteroaryl analogues of AMPA. 2. Synthesis, absolute stereochemistry, photochemistry, and structure-activity relationships.
Falch E, Brehm L, Mikkelsen I, Johansen TN, Skjaerbaek N, Nielsen B, Stensbøl TB, Ebert B, Krogsgaard-Larsen P.
J Med Chem (1998) 41 : 2513 -2523
PubMed 9651156 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.73 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL275040 KAINIC ACID 2.0 1 8.15
CHEMBL310897 1 5.31
CHEMBL85331 1 -
CHEMBL316225 1 -
CHEMBL315416 1 -
CHEMBL83720 1 -
CHEMBL313039 1 -
CHEMBL86216 1 -
CHEMBL312860 1 -
CHEMBL315906 1 -
CHEMBL84114 1 -
CHEMBL82406 1 -
CHEMBL85688 1 -
CHEMBL315203 1 -
CHEMBL276815 (S)-AMPA 1 -
CHEMBL84132 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL275040 KAINIC ACID IC50 = 7.0 nM 8.15
CHEMBL310897 IC50 = 4900.0 nM 5.31
CHEMBL85331 IC50 > 100000.0 nM -
CHEMBL316225 IC50 > 100000.0 nM -
CHEMBL315416 IC50 > 100000.0 nM -
CHEMBL83720 IC50 > 100000.0 nM -
CHEMBL313039 IC50 > 100000.0 nM -
CHEMBL86216 IC50 > 100000.0 nM -
CHEMBL312860 IC50 > 100000.0 nM -
CHEMBL315906 IC50 > 100000.0 nM -
CHEMBL84114 IC50 > 100000.0 nM -
CHEMBL82406 IC50 > 100000.0 nM -
CHEMBL85688 IC50 > 100000.0 nM -
CHEMBL315203 IC50 > 100000.0 nM -
CHEMBL276815 (S)-AMPA IC50 > 100000.0 nM -
CHEMBL84132 IC50 > 100000.0 nM -