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Assay Detail

CHEMBL680877

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

Functional
Inhibition of the current elicited by 100 uM glutamate by simultaneous co-application of the antagonist in xenopus oocytes injected with a 1:1 mixture of GluR1 flop and GluR2 flop RNA as well as GluR5(Q).
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Xenopus laevis
Cell Type Oocyte
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 8 6.46 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55975 1 7.82
CHEMBL152879 1 7.22
CHEMBL147182 1 6.60
CHEMBL422515 1 6.54
CHEMBL152153 1 6.10
CHEMBL154184 1 6.05
CHEMBL434273 1 5.68
CHEMBL153017 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55975 Ki = 15.0 nM 7.82
CHEMBL152879 Ki = 60.0 nM 7.22
CHEMBL147182 Ki = 250.0 nM 6.60
CHEMBL422515 Ki = 290.0 nM 6.54
CHEMBL152153 Ki = 800.0 nM 6.10
CHEMBL154184 Ki = 900.0 nM 6.05
CHEMBL434273 Ki = 2100.0 nM 5.68
CHEMBL153017 Ki = 2200.0 nM 5.66