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Assay Detail

CHEMBL680869

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

Binding
Inhibition of the (-40 mV) current elicited by 100 uM glutamate by simultaneous co-application in xenopus oocytes injected with GluR1 flop RNA.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Oocyte
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Glutamate receptor 1 (CHEMBL2009)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Solid-phase synthesis of polyamine toxin analogues: potent and selective antagonists of Ca2+-permeable AMPA receptors.
Kromann H, Krikstolaityte S, Andersen AJ, Andersen K, Krogsgaard-Larsen P, Jaroszewski JW, Egebjerg J, Strømgaard K.
J Med Chem (2002) 45 : 5745 -5754
PubMed 12477358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.30 6.87

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL152879 1 6.87
CHEMBL269192 1 6.85
CHEMBL345521 1 6.77
CHEMBL152736 1 6.77
CHEMBL152425 1 6.68
CHEMBL153995 1 6.62
CHEMBL352030 1 6.60
CHEMBL350228 1 6.60
CHEMBL154012 1 6.59
CHEMBL355977 1 6.55
CHEMBL153017 1 6.54
CHEMBL422161 1 6.52
CHEMBL153996 1 6.48
CHEMBL152410 1 6.00
CHEMBL422515 1 5.52
CHEMBL434273 1 5.21
CHEMBL147182 1 5.10
CHEMBL154184 1 5.09
CHEMBL55975 1 -
CHEMBL152153 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL152879 Ki = 135.0 nM 6.87
CHEMBL269192 Ki = 140.0 nM 6.85
CHEMBL345521 Ki = 170.0 nM 6.77
CHEMBL152736 Ki = 170.0 nM 6.77
CHEMBL152425 Ki = 210.0 nM 6.68
CHEMBL153995 Ki = 240.0 nM 6.62
CHEMBL352030 Ki = 250.0 nM 6.60
CHEMBL350228 Ki = 250.0 nM 6.60
CHEMBL154012 Ki = 254.0 nM 6.59
CHEMBL355977 Ki = 280.0 nM 6.55
CHEMBL153017 Ki = 287.0 nM 6.54
CHEMBL422161 Ki = 300.0 nM 6.52
CHEMBL153996 Ki = 330.0 nM 6.48
CHEMBL152410 Ki = 1000.0 nM 6.00
CHEMBL422515 Ki = 3000.0 nM 5.52
CHEMBL434273 Ki = 6200.0 nM 5.21
CHEMBL147182 Ki = 8000.0 nM 5.10
CHEMBL154184 Ki = 8100.0 nM 5.09
CHEMBL55975 Ki = 170000.0 nM -
CHEMBL152153 Ki > 10000.0 nM -