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Assay Detail

CHEMBL5258680

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

Binding
Activation of human Kir6.2/SUR1 channel outward current expressed in HEK293 cells at -70 mV holding potential by EPC9 patch-clamp amplifier based assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Sulfonylurea receptor 1, Kir6.2 (CHEMBL2096972)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and SAR of a novel Kir6.2/SUR1 channel opener scaffold identified by HTS.
Dodd CJ, Chronister KS, Rathnayake U, Parr LC, Li K, Chang S, Mi D, Days EL, Bauer JA, Cho HP, Boutaud O, Denton JS, Lindsley CW, Han C.
Bioorg Med Chem Lett (2023) 87 : 129256 -129256
PubMed 36966977 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 6.35 6.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135191 TIFENAZOXIDE 2.0 1 6.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135191 TIFENAZOXIDE EC50 = 450.0 nM 6.35