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Assay Detail

CHEMBL2317552

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

Binding
Inhibition of rat GluA1 receptor flip form expressed in Xenopus laevis oocyte assessed as glutamate-induced current at holding potentials from -80 to -40 mV by two electrode voltage clamp analysis
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glutamate receptor 1 (CHEMBL3753)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationship studies of argiotoxins: selective and potent inhibitors of ionotropic glutamate receptors.
Poulsen MH, Lucas S, Bach TB, Barslund AF, Wenzler C, Jensen CB, Kristensen AS, Strømgaard K.
J Med Chem (2013) 56 : 1171 -1181
PubMed 23320429 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 7.11 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2314718 1 7.77
CHEMBL2314933 1 7.72
CHEMBL2314712 1 7.55
CHEMBL2314717 1 7.43
CHEMBL2314719 1 7.37
CHEMBL2314935 1 7.34
CHEMBL2314713 1 7.28
CHEMBL2311573 1 7.24
CHEMBL2314934 1 7.21
CHEMBL2314931 1 7.11
CHEMBL2314936 1 7.11
CHEMBL1098240 1 7.11
CHEMBL2314940 1 7.09
CHEMBL2314716 1 7.08
CHEMBL2314938 1 7.08
CHEMBL2314715 1 7.03
CHEMBL2314929 1 7.02
CHEMBL2314928 1 6.98
CHEMBL2314937 1 6.93
CHEMBL2314930 1 6.91
CHEMBL2314927 1 6.78
CHEMBL2314932 1 6.77
CHEMBL2314939 1 6.34
CHEMBL2314714 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2314718 IC50 = 17.0 nM 7.77
CHEMBL2314933 IC50 = 19.0 nM 7.72
CHEMBL2314712 IC50 = 28.0 nM 7.55
CHEMBL2314717 IC50 = 37.0 nM 7.43
CHEMBL2314719 IC50 = 43.0 nM 7.37
CHEMBL2314935 IC50 = 46.0 nM 7.34
CHEMBL2314713 IC50 = 52.0 nM 7.28
CHEMBL2311573 IC50 = 57.0 nM 7.24
CHEMBL2314934 IC50 = 62.0 nM 7.21
CHEMBL2314931 IC50 = 77.0 nM 7.11
CHEMBL2314936 IC50 = 78.0 nM 7.11
CHEMBL1098240 IC50 = 77.0 nM 7.11
CHEMBL2314940 IC50 = 81.0 nM 7.09
CHEMBL2314716 IC50 = 84.0 nM 7.08
CHEMBL2314938 IC50 = 83.0 nM 7.08
CHEMBL2314715 IC50 = 94.0 nM 7.03
CHEMBL2314929 IC50 = 96.0 nM 7.02
CHEMBL2314928 IC50 = 105.0 nM 6.98
CHEMBL2314937 IC50 = 118.0 nM 6.93
CHEMBL2314930 IC50 = 124.0 nM 6.91
CHEMBL2314927 IC50 = 167.0 nM 6.78
CHEMBL2314932 IC50 = 171.0 nM 6.77
CHEMBL2314939 IC50 = 454.0 nM 6.34
CHEMBL2314714 IC50 = 466.0 nM 6.33