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Assay Detail

CHEMBL954137

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

Binding
Activation of BK channel-mediated vasorelaxation activity assessed as reduction in KCl-induced contractile tone
ChEMBL ↗
69
Total Activities
69
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Calcium-activated potassium channel subunit alpha-1 (CHEMBL4304) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

QSAR studies on BK channel activators.
Coi A, Fiamingo FL, Livi O, Calderone V, Martelli A, Massarelli I, Bianucci AM.
Bioorg Med Chem (2009) 17 : 319 -325
PubMed 19026552 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 69 5.32 8.49

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL445346 — — 1 8.49
CHEMBL448335 — — 1 7.56
CHEMBL465922 — — 1 7.56
CHEMBL524902 — — 1 6.87
CHEMBL504160 — — 1 6.84
CHEMBL511200 — — 1 6.75
CHEMBL506373 — — 1 6.72
CHEMBL464057 — — 1 6.60
CHEMBL517012 — — 1 6.55
CHEMBL455306 — — 1 6.43
CHEMBL453712 — — 1 6.35
CHEMBL465950 — — 1 6.19
CHEMBL464249 — — 1 6.16
CHEMBL465109 — — 1 5.84
CHEMBL465454 — — 1 5.81
CHEMBL512408 — — 1 5.67
CHEMBL465455 — — 1 5.61
CHEMBL499800 — — 1 5.60
CHEMBL465456 — — 1 5.58
CHEMBL526140 — — 1 5.52
CHEMBL481576 — — 1 5.51
CHEMBL481577 — — 1 5.51
CHEMBL481578 — — 1 5.48
CHEMBL519785 — — 1 5.46
CHEMBL480795 — — 1 5.39
CHEMBL297914 — — 1 5.28
CHEMBL482376 — — 1 5.23
CHEMBL384903 — — 1 5.23
CHEMBL482377 — — 1 5.16
CHEMBL482378 — — 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL445346 — IC50 = 3.236 nM 8.49
CHEMBL448335 — IC50 = 27.54 nM 7.56
CHEMBL465922 — IC50 = 27.54 nM 7.56
CHEMBL524902 — IC50 = 134.9 nM 6.87
CHEMBL504160 — IC50 = 144.54 nM 6.84
CHEMBL511200 — IC50 = 177.83 nM 6.75
CHEMBL506373 — IC50 = 190.55 nM 6.72
CHEMBL464057 — IC50 = 251.19 nM 6.60
CHEMBL517012 — IC50 = 281.84 nM 6.55
CHEMBL455306 — IC50 = 371.54 nM 6.43
CHEMBL453712 — IC50 = 446.68 nM 6.35
CHEMBL465950 — IC50 = 645.65 nM 6.19
CHEMBL464249 — IC50 = 691.83 nM 6.16
CHEMBL465109 — IC50 = 1445.44 nM 5.84
CHEMBL465454 — IC50 = 1548.82 nM 5.81
CHEMBL512408 — IC50 = 2137.96 nM 5.67
CHEMBL465455 — IC50 = 2454.71 nM 5.61
CHEMBL499800 — IC50 = 2511.89 nM 5.60
CHEMBL465456 — IC50 = 2630.27 nM 5.58
CHEMBL526140 — IC50 = 3019.95 nM 5.52
CHEMBL481576 — IC50 = 3090.3 nM 5.51
CHEMBL481577 — IC50 = 3090.3 nM 5.51
CHEMBL481578 — IC50 = 3311.31 nM 5.48
CHEMBL519785 — IC50 = 3467.37 nM 5.46
CHEMBL480795 — IC50 = 4073.8 nM 5.39
CHEMBL297914 — IC50 = 5248.07 nM 5.28
CHEMBL384903 — IC50 = 5888.44 nM 5.23
CHEMBL482376 — IC50 = 5888.44 nM 5.23
CHEMBL482377 — IC50 = 6918.31 nM 5.16
CHEMBL482378 — IC50 = 7762.47 nM 5.11
CHEMBL481781 — IC50 = 8128.31 nM 5.09
CHEMBL480414 — IC50 = 8709.64 nM 5.06
CHEMBL443975 — IC50 = 9332.54 nM 5.03
CHEMBL480413 — IC50 = 10232.93 nM 4.99
CHEMBL480300 — IC50 = 10964.78 nM 4.96
CHEMBL480415 — IC50 = 11220.18 nM 4.95
CHEMBL501138 — IC50 = 11220.18 nM 4.95
CHEMBL465926 — IC50 = 11748.98 nM 4.93
CHEMBL463870 — IC50 = 11748.98 nM 4.93
CHEMBL447035 — IC50 = 11748.98 nM 4.93
CHEMBL504665 — IC50 = 12302.69 nM 4.91
CHEMBL464033 — IC50 = 12589.25 nM 4.90
CHEMBL464051 — IC50 = 13489.63 nM 4.87
CHEMBL506149 — IC50 = 13489.63 nM 4.87
CHEMBL464052 — IC50 = 13803.84 nM 4.86
CHEMBL463882 — IC50 = 15135.61 nM 4.82
CHEMBL465376 — IC50 = 15135.61 nM 4.82
CHEMBL468265 — IC50 = 15848.93 nM 4.80
CHEMBL501328 — IC50 = 17378.01 nM 4.76
CHEMBL467019 — IC50 = 17782.79 nM 4.75