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Assay Detail

CHEMBL1008047

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

Binding
Inhibition of Wistar rat recombinant SK3 channel expressed in HEK293 cells by whole cell patch clamp technique
44
Total Activities
44
Compounds Tested
3
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
Kd 40 6.65 9.37
Activity 3 - -
IC50 1 5.16 5.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420873 1 9.37
CHEMBL117908 1 8.57
CHEMBL511710 1 8.04
CHEMBL504041 1 7.96
CHEMBL458836 1 7.77
CHEMBL463987 1 7.70
CHEMBL463373 1 7.57
CHEMBL453140 1 7.51
CHEMBL463189 1 7.50
CHEMBL463986 1 7.48
CHEMBL511681 1 7.47
CHEMBL457743 1 7.36
CHEMBL511709 1 7.21
CHEMBL510780 1 7.11
CHEMBL457744 1 6.92
CHEMBL458755 1 6.89
CHEMBL487165 1 6.89
CHEMBL444117 1 6.77
CHEMBL121663 DEQUALINIUM CHLORIDE 4.0 1 6.75
CHEMBL456444 1 6.70
CHEMBL486156 1 6.35
CHEMBL487166 1 6.27
CHEMBL458754 1 6.23
CHEMBL519876 1 6.22
CHEMBL456445 1 6.19
CHEMBL507161 1 6.12
CHEMBL458756 1 6.10
CHEMBL515502 1 5.80
CHEMBL453486 1 5.77
CHEMBL457972 1 5.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420873 Kd = 0.43 nM 9.37
CHEMBL117908 Kd = 2.7 nM 8.57
CHEMBL511710 Kd = 9.1 nM 8.04
CHEMBL504041 Kd = 11.0 nM 7.96
CHEMBL458836 Kd = 17.0 nM 7.77
CHEMBL463987 Kd = 20.0 nM 7.70
CHEMBL463373 Kd = 27.0 nM 7.57
CHEMBL453140 Kd = 31.0 nM 7.51
CHEMBL463189 Kd = 32.0 nM 7.50
CHEMBL463986 Kd = 33.0 nM 7.48
CHEMBL511681 Kd = 34.0 nM 7.47
CHEMBL457743 Kd = 44.0 nM 7.36
CHEMBL511709 Kd = 61.0 nM 7.21
CHEMBL510780 Kd = 77.0 nM 7.11
CHEMBL457744 Kd = 120.0 nM 6.92
CHEMBL458755 Kd = 130.0 nM 6.89
CHEMBL487165 Kd = 130.0 nM 6.89
CHEMBL444117 Kd = 170.0 nM 6.77
CHEMBL121663 DEQUALINIUM CHLORIDE Kd = 180.0 nM 6.75
CHEMBL456444 Kd = 200.0 nM 6.70
CHEMBL486156 Kd = 450.0 nM 6.35
CHEMBL487166 Kd = 540.0 nM 6.27
CHEMBL458754 Kd = 590.0 nM 6.23
CHEMBL519876 Kd = 600.0 nM 6.22
CHEMBL456445 Kd = 640.0 nM 6.19
CHEMBL507161 Kd = 750.0 nM 6.12
CHEMBL458756 Kd = 790.0 nM 6.10
CHEMBL515502 Kd = 1600.0 nM 5.80
CHEMBL453486 Kd = 1700.0 nM 5.77
CHEMBL457972 Kd = 2000.0 nM 5.70
CHEMBL215370 LAUDANOSINE METHIODIDE Kd = 2600.0 nM 5.58
CHEMBL456446 Kd = 2700.0 nM 5.57
CHEMBL1360 ATRACURIUM Kd = 6400.0 nM 5.19
CHEMBL455001 Kd = 6500.0 nM 5.19
CHEMBL558625 IC50 = 7000.0 nM 5.16
CHEMBL539935 Kd = 14000.0 nM 4.85
CHEMBL1687 Kd = 16000.0 nM 4.80
CHEMBL554917 PENUCURONIUM Kd = 21000.0 nM 4.68
CHEMBL502867 Kd > 10000.0 nM -
CHEMBL453730 Activity - -
CHEMBL499968 Activity - -
CHEMBL452887 Activity - -
CHEMBL171596 Kd > 10000.0 nM -
CHEMBL486569 Kd > 10000.0 nM -