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Assay Detail

CHEMBL701841

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

Binding
Inhibition of [3H]AMPA binding to Ionotropic glutamate receptor from rat whole brain.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

8-(1H-imidazol-1-yl)-7-nitro-4(5H)-imidazo[1,2-alpha]quinoxalinone and related compounds: synthesis and structure-activity relationships for the AMPA-type non-NMDA receptor.
Ohmori J, Shimizu-Sasamata M, Okada M, Sakamoto S.
J Med Chem (1997) 40 : 2053 -2063
PubMed 9207947 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 6.76 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294781 1 7.70
CHEMBL64772 1 7.68
CHEMBL303068 1 7.32
CHEMBL302672 1 7.24
CHEMBL294308 1 7.18
CHEMBL13260 YM-90K 1 7.08
CHEMBL292806 1 7.02
CHEMBL63656 1 6.89
CHEMBL27653 1 6.85
CHEMBL63108 1 6.82
CHEMBL64044 1 6.72
CHEMBL62842 1 6.72
CHEMBL62431 1 6.70
CHEMBL64870 1 6.48
CHEMBL294540 1 6.41
CHEMBL408393 1 6.36
CHEMBL64133 1 5.35
CHEMBL63326 1 5.18
CHEMBL294801 1 -
CHEMBL64888 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294781 Ki = 20.0 nM 7.70
CHEMBL64772 Ki = 21.0 nM 7.68
CHEMBL303068 Ki = 48.0 nM 7.32
CHEMBL302672 Ki = 57.0 nM 7.24
CHEMBL294308 Ki = 66.0 nM 7.18
CHEMBL13260 YM-90K Ki = 84.0 nM 7.08
CHEMBL292806 Ki = 96.0 nM 7.02
CHEMBL63656 Ki = 130.0 nM 6.89
CHEMBL27653 Ki = 140.0 nM 6.85
CHEMBL63108 Ki = 150.0 nM 6.82
CHEMBL64044 Ki = 190.0 nM 6.72
CHEMBL62842 Ki = 190.0 nM 6.72
CHEMBL62431 Ki = 200.0 nM 6.70
CHEMBL64870 Ki = 330.0 nM 6.48
CHEMBL294540 Ki = 390.0 nM 6.41
CHEMBL408393 Ki = 440.0 nM 6.36
CHEMBL64133 Ki = 4500.0 nM 5.35
CHEMBL63326 Ki = 6600.0 nM 5.18
CHEMBL294801 Ki > 100000.0 nM -
CHEMBL64888 Ki > 10000.0 nM -