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Assay Detail

CHEMBL2411652

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

Binding
Activation of GIRK1/2 (unknown origin) by thallium flux assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Kir3.1/Kir3.2 (CHEMBL3038489)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors.
Wen W, Wu W, Romaine IM, Kaufmann K, Du Y, Sulikowski GA, Weaver CD, Lindsley CW.
Bioorg Med Chem Lett (2013) 23 : 4562 -4566
PubMed 23838260 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 6.33 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2409106 1 6.80
CHEMBL86962 1 5.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2409106 EC50 = 160.0 nM 6.80
CHEMBL86962 EC50 = 1400.0 nM 5.85