Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4048606

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

Binding
Displacement of [3H]SYM2081 from recombinant homomeric rat GluK1 receptor expressed in baculovirus infected Sf9 insect cell membranes
5
Total Activities
5
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 ionotropic, kainate 1 (CHEMBL2919)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

( S)-2-Amino-3-(5-methyl-3-hydroxyisoxazol-4-yl)propanoic Acid (AMPA) and Kainate Receptor Ligands: Further Exploration of Bioisosteric Replacements and Structural and Biological Investigation.
Brogi S, Brindisi M, Butini S, Kshirsagar GU, Maramai S, Chemi G, Gemma S, Campiani G, Novellino E, Fiorenzani P, Pinassi J, Aloisi AM, Gynther M, Venskutonytė R, Han L, Frydenvang K, Kastrup JS, Pickering DS.
J Med Chem (2018) 61 : 2124 -2130
PubMed 29451794 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.11 7.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL337577 1 7.36
CHEMBL4075364 1 6.45
CHEMBL4077177 1 6.23
CHEMBL4066795 1 6.06
CHEMBL4083716 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL337577 Ki = 44.0 nM 7.36
CHEMBL4075364 Ki = 356.0 nM 6.45
CHEMBL4077177 Ki = 586.0 nM 6.23
CHEMBL4066795 Ki = 869.0 nM 6.06
CHEMBL4083716 Ki = 36000.0 nM 4.44