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Assay Detail

CHEMBL1777604

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

Functional
Inhibition of glucose induced insulin secretion from rat Pancreatic islet assessed as percentage of residual insulin release
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Pancreatic islet
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Impact of the nature of the substituent at the 3-position of 4H-1,2,4-benzothiadiazine 1,1-dioxides on their opening activity toward ATP-sensitive potassium channels.
Pirotte B, de Tullio P, Boverie S, Michaux C, Lebrun P.
J Med Chem (2011) 54 : 3188 -3199
PubMed 21428460 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.05 6.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112668 1 6.26
CHEMBL1774479 1 5.24
CHEMBL181 DIAZOXIDE 4.0 1 4.74
CHEMBL1774464 1 4.72
CHEMBL1774471 1 4.30
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112668 IC50 = 550.0 nM 6.26
CHEMBL1774479 IC50 = 5800.0 nM 5.24
CHEMBL181 DIAZOXIDE IC50 = 18400.0 nM 4.74
CHEMBL1774464 IC50 = 19100.0 nM 4.72
CHEMBL1774471 IC50 = 50000.0 nM 4.30
CHEMBL1159 PINACIDIL ANHYDROUS IC50 = 202300.0 nM -