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Assay Detail

CHEMBL702865

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

Binding
In vitro binding affinity against Ionotropic glutamate receptor kainate (kainic acid) using [3H]KAIN as radioligand
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 kainate (CHEMBL2109241)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Heteroaryl analogues of AMPA. Synthesis and quantitative structure-activity relationships.
Bang-Andersen B, Lenz SM, Skjaerbaek N, Søby KK, Hansen HO, Ebert B, Bøgesø KP, Krogsgaard-Larsen P.
J Med Chem (1997) 40 : 2831 -2842
PubMed 9288165 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 4.51 5.31

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL310897 1 5.31
CHEMBL328310 1 4.80
CHEMBL94859 1 4.39
CHEMBL318467 1 4.24
CHEMBL13378 (R,S)-AMPA 1 4.17
CHEMBL98723 1 4.13
CHEMBL317790 1 -
CHEMBL97742 1 -
CHEMBL94860 1 -
CHEMBL441460 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL310897 IC50 = 4900.0 nM 5.31
CHEMBL328310 IC50 = 16000.0 nM 4.80
CHEMBL94859 IC50 = 41000.0 nM 4.39
CHEMBL318467 IC50 = 58000.0 nM 4.24
CHEMBL13378 (R,S)-AMPA IC50 = 68000.0 nM 4.17
CHEMBL98723 IC50 = 74000.0 nM 4.13
CHEMBL317790 IC50 > 100000.0 nM -
CHEMBL97742 IC50 > 100000.0 nM -
CHEMBL94860 IC50 > 100000.0 nM -
CHEMBL441460 IC50 > 100000.0 nM -