Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL832384

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

Functional
Inhibition of after hyperpolarization (AHP) of cultured rat sympathetic neurons as SKCa channel blocking activity
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Sympathetic neuron
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Small conductance calcium-activated potassium channel (CHEMBL2096673)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Bis-quinolinium cyclophanes: toward a pharmacophore model for the blockade of apamin-sensitive SKCa channels in sympathetic neurons.
Galanakis D, Ganellin CR, Chen JQ, Gunasekera D, Dunn PM.
Bioorg Med Chem Lett (2004) 14 : 4231 -4235
PubMed 15261276 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 7.31 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL420873 1 8.70
CHEMBL117908 1 8.52
CHEMBL184300 1 8.05
CHEMBL185146 1 8.00
CHEMBL181911 1 7.92
CHEMBL183644 1 7.82
CHEMBL184858 1 7.80
CHEMBL181912 1 7.60
CHEMBL430146 1 7.55
CHEMBL184891 1 7.52
CHEMBL182716 1 7.51
CHEMBL360624 1 7.46
CHEMBL1180184 1 7.40
CHEMBL186139 1 7.22
CHEMBL360621 1 7.22
CHEMBL185258 1 7.19
CHEMBL137175 1 7.16
CHEMBL185106 1 6.89
CHEMBL341700 1 6.89
CHEMBL185137 1 6.82
CHEMBL425707 1 6.82
CHEMBL119859 1 6.72
CHEMBL185230 1 6.58
CHEMBL185006 2 6.42
CHEMBL121663 DEQUALINIUM CHLORIDE 4.0 1 6.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL420873 IC50 = 2.0 nM 8.70
CHEMBL117908 IC50 = 3.0 nM 8.52
CHEMBL184300 IC50 = 9.0 nM 8.05
CHEMBL185146 IC50 = 10.0 nM 8.00
CHEMBL181911 IC50 = 12.0 nM 7.92
CHEMBL183644 IC50 = 15.0 nM 7.82
CHEMBL184858 IC50 = 16.0 nM 7.80
CHEMBL181912 IC50 = 25.0 nM 7.60
CHEMBL430146 IC50 = 28.0 nM 7.55
CHEMBL184891 IC50 = 30.0 nM 7.52
CHEMBL182716 IC50 = 31.0 nM 7.51
CHEMBL360624 IC50 = 35.0 nM 7.46
CHEMBL1180184 IC50 = 40.0 nM 7.40
CHEMBL186139 IC50 = 60.0 nM 7.22
CHEMBL360621 IC50 = 60.0 nM 7.22
CHEMBL185258 IC50 = 65.0 nM 7.19
CHEMBL137175 IC50 = 70.0 nM 7.16
CHEMBL341700 IC50 = 130.0 nM 6.89
CHEMBL185106 IC50 = 130.0 nM 6.89
CHEMBL185137 IC50 = 150.0 nM 6.82
CHEMBL425707 IC50 = 150.0 nM 6.82
CHEMBL119859 IC50 = 190.0 nM 6.72
CHEMBL185230 IC50 = 260.0 nM 6.58
CHEMBL185006 IC50 = 380.0 nM 6.42
CHEMBL185006 IC50 = 630.0 nM 6.20
CHEMBL121663 DEQUALINIUM CHLORIDE IC50 = 900.0 nM 6.05