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Assay Detail

CHEMBL884411

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

Binding
Potassium channel opening activity in vitro using LtK cells transfected with Kir6.2/SUR2B exon 17
51
Total Activities
51
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type LtK
Confidence 8 — Homologous single protein target
Curated By Expert

Target

ATP-sensitive inward rectifier potassium channel 11 (CHEMBL1886)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationship of a novel class of naphthyl amide KATP channel openers.
Turner SC, Carroll WA, White TK, Brune ME, Buckner SA, Gopalakrishnan M, Fabiyi A, Coghlan MJ, Scott VE, Castle NA, Daza AV, Milicic I, Sullivan JP.
Bioorg Med Chem Lett (2003) 13 : 1741 -1744
PubMed 12729655 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 51 6.76 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48848 1 8.05
CHEMBL49806 1 7.92
CHEMBL50374 1 7.92
CHEMBL50760 1 7.82
CHEMBL299167 1 7.75
CHEMBL300958 1 7.64
CHEMBL48797 1 7.62
CHEMBL49787 1 7.36
CHEMBL51071 1 7.36
CHEMBL47170 1 7.35
CHEMBL300969 1 7.34
CHEMBL298866 1 7.33
CHEMBL49116 1 7.31
CHEMBL49076 1 7.22
CHEMBL48291 1 7.16
CHEMBL49153 1 7.14
CHEMBL296954 1 7.12
CHEMBL298383 1 7.10
CHEMBL45937 1 7.09
CHEMBL298970 1 7.08
CHEMBL301296 1 7.01
CHEMBL295458 1 6.93
CHEMBL49797 1 6.88
CHEMBL49701 1 6.86
CHEMBL51460 1 6.81
CHEMBL48801 1 6.80
CHEMBL48765 1 6.73
CHEMBL46244 1 6.71
CHEMBL45749 1 6.67
CHEMBL48174 1 6.56

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48848 EC50 = 9.0 nM 8.05
CHEMBL49806 EC50 = 12.0 nM 7.92
CHEMBL50374 EC50 = 12.0 nM 7.92
CHEMBL50760 EC50 = 15.0 nM 7.82
CHEMBL299167 EC50 = 18.0 nM 7.75
CHEMBL300958 EC50 = 23.0 nM 7.64
CHEMBL48797 EC50 = 24.0 nM 7.62
CHEMBL49787 EC50 = 44.0 nM 7.36
CHEMBL51071 EC50 = 44.0 nM 7.36
CHEMBL47170 EC50 = 45.0 nM 7.35
CHEMBL300969 EC50 = 46.0 nM 7.34
CHEMBL298866 EC50 = 47.0 nM 7.33
CHEMBL49116 EC50 = 49.0 nM 7.31
CHEMBL49076 EC50 = 60.0 nM 7.22
CHEMBL48291 EC50 = 70.0 nM 7.16
CHEMBL49153 EC50 = 72.0 nM 7.14
CHEMBL296954 EC50 = 76.0 nM 7.12
CHEMBL298383 EC50 = 80.0 nM 7.10
CHEMBL45937 EC50 = 81.0 nM 7.09
CHEMBL298970 EC50 = 84.0 nM 7.08
CHEMBL301296 EC50 = 98.0 nM 7.01
CHEMBL295458 EC50 = 117.0 nM 6.93
CHEMBL49797 EC50 = 131.0 nM 6.88
CHEMBL49701 EC50 = 137.0 nM 6.86
CHEMBL51460 EC50 = 154.0 nM 6.81
CHEMBL48801 EC50 = 160.0 nM 6.80
CHEMBL48765 EC50 = 185.0 nM 6.73
CHEMBL46244 EC50 = 194.0 nM 6.71
CHEMBL45749 EC50 = 213.0 nM 6.67
CHEMBL48174 EC50 = 276.0 nM 6.56
CHEMBL49348 EC50 = 306.0 nM 6.51
CHEMBL301591 EC50 = 317.0 nM 6.50
CHEMBL48615 EC50 = 417.0 nM 6.38
CHEMBL49191 EC50 = 495.0 nM 6.30
CHEMBL296931 EC50 = 570.0 nM 6.24
CHEMBL296840 EC50 = 751.0 nM 6.12
CHEMBL45645 EC50 = 1160.0 nM 5.94
CHEMBL48755 EC50 = 1750.0 nM 5.76
CHEMBL49551 EC50 = 2040.0 nM 5.69
CHEMBL49321 EC50 = 2220.0 nM 5.65
CHEMBL299166 EC50 = 4340.0 nM 5.36
CHEMBL48890 EC50 = 4840.0 nM 5.32
CHEMBL50501 EC50 = 5310.0 nM 5.28
CHEMBL46435 EC50 = 5550.0 nM 5.26
CHEMBL49070 EC50 = 6630.0 nM 5.18
CHEMBL296879 EC50 = 177000.0 nM -
CHEMBL46245 EC50 > 10000.0 nM -
CHEMBL49549 EC50 > 10000.0 nM -
CHEMBL47061 EC50 > 10000.0 nM -
CHEMBL52283 EC50 > 10000.0 nM -