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Assay Detail

CHEMBL805641

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

Functional
Inhibitory concentration of compound required for SKCa blocking action was assessed from its ability to inhibit After hyperpolarisation (AHP) in cultured rat sympathetic neurons
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Sympathetic neuron
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Bis-quinolinium cyclophanes: A novel class of potent blockers of the apamin-sensitive Ca2+-activated K+ channel
Campos Rosa J, Beckwith-Hall BM, Galanakis D, Ganellin C, Dunn PM, Jenkinson DH
Bioorg Med Chem Lett (1997) 7 : 7 -10
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.66 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL446445 UCL-1530 1 7.10
CHEMBL6207 1 7.05
CHEMBL268556 1 6.96
CHEMBL258254 1 6.82
CHEMBL6266 1 6.77
CHEMBL266885 1 6.75
CHEMBL6361 1 6.72
CHEMBL6354 1 6.54
CHEMBL6356 1 6.51
CHEMBL269729 1 6.42
CHEMBL429017 1 6.39
CHEMBL6315 1 6.35
CHEMBL6212 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL446445 UCL-1530 IC50 = 80.0 nM 7.10
CHEMBL6207 IC50 = 90.0 nM 7.05
CHEMBL268556 IC50 = 110.0 nM 6.96
CHEMBL258254 IC50 = 150.0 nM 6.82
CHEMBL6266 IC50 = 170.0 nM 6.77
CHEMBL266885 IC50 = 180.0 nM 6.75
CHEMBL6361 IC50 = 190.0 nM 6.72
CHEMBL6354 IC50 = 290.0 nM 6.54
CHEMBL6356 IC50 = 310.0 nM 6.51
CHEMBL269729 IC50 = 380.0 nM 6.42
CHEMBL429017 IC50 = 410.0 nM 6.39
CHEMBL6315 IC50 = 450.0 nM 6.35
CHEMBL6212 IC50 = 700.0 nM 6.16