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Assay Detail

CHEMBL641504

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

Binding
Binding affinity against AMPA receptor in rat brain membrane using [3H]-AMPA as radioligand
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Glutamate receptor ionotropic, AMPA (CHEMBL2093871)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

6-(1H-imidazol-1-yl)-7-nitro-2,3(1H,4H)-quinoxalinedione hydrochloride (YM90K) and related compounds: structure-activity relationships for the AMPA-type non-NMDA receptor.
Ohmori J, Sakamoto S, Kubota H, Shimizu-Sasamata M, Okada M, Kawasaki S, Hidaka K, Togami J, Furuya T, Murase K.
J Med Chem (1994) 37 : 467 -475
PubMed 8120865 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 22 6.31 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL222519 NBQX 1 7.22
CHEMBL13260 YM-90K 1 7.08
CHEMBL357841 1 7.00
CHEMBL129227 1 6.75
CHEMBL142005 1 6.70
CHEMBL62431 1 6.70
CHEMBL155265 DNQX 1 6.70
CHEMBL142391 1 6.64
CHEMBL128118 1 6.62
CHEMBL9790 1 6.57
CHEMBL142233 1 6.41
CHEMBL294540 1 6.37
CHEMBL410513 1 6.21
CHEMBL142872 1 6.16
CHEMBL345094 1 6.09
CHEMBL142804 1 5.89
CHEMBL145604 1 5.85
CHEMBL27715 1 5.80
CHEMBL337747 1 5.72
CHEMBL23044 1 5.70
CHEMBL142157 1 5.32
CHEMBL342289 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL222519 NBQX Ki = 60.0 nM 7.22
CHEMBL13260 YM-90K Ki = 84.0 nM 7.08
CHEMBL357841 Ki = 100.0 nM 7.00
CHEMBL129227 Ki = 180.0 nM 6.75
CHEMBL142005 Ki = 200.0 nM 6.70
CHEMBL62431 Ki = 200.0 nM 6.70
CHEMBL155265 DNQX Ki = 200.0 nM 6.70
CHEMBL142391 Ki = 230.0 nM 6.64
CHEMBL128118 Ki = 240.0 nM 6.62
CHEMBL9790 Ki = 270.0 nM 6.57
CHEMBL142233 Ki = 390.0 nM 6.41
CHEMBL294540 Ki = 430.0 nM 6.37
CHEMBL410513 Ki = 620.0 nM 6.21
CHEMBL142872 Ki = 690.0 nM 6.16
CHEMBL345094 Ki = 820.0 nM 6.09
CHEMBL142804 Ki = 1300.0 nM 5.89
CHEMBL145604 Ki = 1400.0 nM 5.85
CHEMBL27715 Ki = 1600.0 nM 5.80
CHEMBL337747 Ki = 1900.0 nM 5.72
CHEMBL23044 Ki = 2000.0 nM 5.70
CHEMBL142157 Ki = 4800.0 nM 5.32
CHEMBL342289 Ki = 5000.0 nM 5.30