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Assay Detail

CHEMBL1947669

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

Binding
Activation of KATP channel in K+-depolarized rat aortic rings assessed as relaxation of KCl-induced contraction
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Aorta
Confidence 3 — Cell-line / Tissue
Curated By Autocuration

Publication

Hydroxylated analogues of ATP-sensitive potassium channel openers belonging to the group of 6- and/or 7-substituted 3-isopropylamino-4H-1,2,4-benzothiadiazine 1,1-dioxides: toward an improvement in sulfonylurea receptor 1 selectivity and metabolism stability.
de Tullio P, Servais AC, Fillet M, Gillotin F, Somers F, Chiap P, Lebrun P, Pirotte B.
J Med Chem (2011) 54 : 8353 -8361
PubMed 22077416 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 28 4.56 5.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1946140 1 5.12
CHEMBL1946270 1 4.76
CHEMBL1946139 1 4.75
CHEMBL191539 1 4.43
CHEMBL115565 1 4.36
CHEMBL1946759 1 4.28
CHEMBL1946412 1 4.25
CHEMBL1946135 1 -
CHEMBL1945809 1 -
CHEMBL1945806 1 -
CHEMBL1946760 1 -
CHEMBL1944656 1 -
CHEMBL1946413 1 -
CHEMBL1946411 1 -
CHEMBL1946274 1 -
CHEMBL1946138 1 -
CHEMBL1946136 1 -
CHEMBL1946137 1 -
CHEMBL1946271 1 -
CHEMBL1946272 1 -
CHEMBL1945808 1 -
CHEMBL1946414 1 -
CHEMBL1946134 1 -
CHEMBL1945810 1 -
CHEMBL189093 1 -
CHEMBL1946410 1 -
CHEMBL1945807 1 -
CHEMBL1946273 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1946140 EC50 = 7500.0 nM 5.12
CHEMBL1946270 EC50 = 17400.0 nM 4.76
CHEMBL1946139 EC50 = 17600.0 nM 4.75
CHEMBL191539 EC50 = 37000.0 nM 4.43
CHEMBL115565 EC50 = 43300.0 nM 4.36
CHEMBL1946759 EC50 = 53100.0 nM 4.28
CHEMBL1946412 EC50 = 55700.0 nM 4.25
CHEMBL1946135 EC50 > 300000.0 nM -
CHEMBL1945809 EC50 - -
CHEMBL1945806 EC50 > 300000.0 nM -
CHEMBL1946760 EC50 - -
CHEMBL1944656 EC50 - -
CHEMBL1946413 EC50 - -
CHEMBL1946411 EC50 - -
CHEMBL1946274 EC50 - -
CHEMBL1946138 EC50 - -
CHEMBL1946136 EC50 - -
CHEMBL1946137 EC50 > 300000.0 nM -
CHEMBL1946271 EC50 > 200000.0 nM -
CHEMBL1946272 EC50 > 200000.0 nM -
CHEMBL1945808 EC50 - -
CHEMBL1946414 EC50 > 300000.0 nM -
CHEMBL1946134 EC50 = 124000.0 nM -
CHEMBL1945810 EC50 = 189000.0 nM -
CHEMBL189093 EC50 = 274000.0 nM -
CHEMBL1946410 EC50 = 241000.0 nM -
CHEMBL1945807 EC50 = 230000.0 nM -
CHEMBL1946273 EC50 > 200000.0 nM -