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Assay Detail

CHEMBL1008046

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

Binding
Displacement of [I125]apamine from Wistar rat recombinant SK3 channel expressed in HEK293 cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Synthesis and structure-activity relationship studies of 2-(N-substituted)-aminobenzimidazoles as potent negative gating modulators ofsmall conductance Ca2+-activated K+ channels.
Sørensen US, Strøbaek D, Christophersen P, Hougaard C, Jensen ML, Nielsen EØ, Peters D, Teuber L.
J Med Chem (2008) 51 : 7625 -7634
PubMed 18998663 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 6.34 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420873 1 8.85
CHEMBL117908 1 8.74
CHEMBL121663 DEQUALINIUM CHLORIDE 4.0 1 6.85
CHEMBL215370 LAUDANOSINE METHIODIDE 1 5.82
CHEMBL558625 1 5.36
CHEMBL1360 ATRACURIUM 4.0 1 5.23
CHEMBL1687 1 5.04
CHEMBL554917 PENUCURONIUM 1 4.80
CHEMBL452887 1 -
CHEMBL499968 1 -
CHEMBL453730 1 -
CHEMBL510780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420873 Ki = 1.4 nM 8.85
CHEMBL117908 Ki = 1.8 nM 8.74
CHEMBL121663 DEQUALINIUM CHLORIDE Ki = 140.0 nM 6.85
CHEMBL215370 LAUDANOSINE METHIODIDE Ki = 1500.0 nM 5.82
CHEMBL558625 Ki = 4400.0 nM 5.36
CHEMBL1360 ATRACURIUM Ki = 5900.0 nM 5.23
CHEMBL1687 Ki = 9200.0 nM 5.04
CHEMBL554917 PENUCURONIUM Ki = 16000.0 nM 4.80
CHEMBL452887 Ki > 50000.0 nM -
CHEMBL499968 Ki > 50000.0 nM -
CHEMBL453730 Ki > 50000.0 nM -
CHEMBL510780 Ki > 50000.0 nM -