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Assay Detail

CHEMBL698078

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

Binding
Ability to displace binding of [3H]AMPA to recombinant human Ionotropic glutamate receptor ionotropic kainate 1
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Ethyl (3S,4aR,6S,8aR)-6-(4-ethoxycar- bonylimidazol-1-ylmethyl)decahydroiso-quinoline-3-carboxylic ester: a prodrug of a GluR5 kainate receptor antagonist active in two animal models of acute migraine.
Filla SA, Winter MA, Johnson KW, Bleakman D, Bell MG, Bleisch TJ, Castaño AM, Clemens-Smith A, del Prado M, Dieckman DK, Dominguez E, Escribano A, Ho KH, Hudziak KJ, Katofiasc MA, Martinez-Perez JA, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Phebus LA, Stack DR, Stratford RE, Ornstein PL.
J Med Chem (2002) 45 : 4383 -4386
PubMed 12238915 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 5.71 6.81

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL542242 1 6.81
CHEMBL14935 TEZAMPANEL ANHYDROUS 2.0 1 5.38
CHEMBL222519 NBQX 1 4.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL542242 Ki = 156.0 nM 6.81
CHEMBL14935 TEZAMPANEL ANHYDROUS Ki = 4200.0 nM 5.38
CHEMBL222519 NBQX Ki = 11600.0 nM 4.94