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Assay Detail

CHEMBL972281

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

Functional
Inhibition of glucose-induced insulin secretion in Wistar rat pancreatic beta islets assessed as residual insulin secretion relative to control
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers.
Sebille S, de Tullio P, Florence X, Becker B, Antoine MH, Michaux C, Wouters J, Pirotte B, Lebrun P.
Bioorg Med Chem (2008) 16 : 5704 -5719
PubMed 18406154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.53 6.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112668 1 6.14
CHEMBL447283 1 5.65
CHEMBL497955 1 5.64
CHEMBL497954 1 5.59
CHEMBL497956 1 5.56
CHEMBL526087 1 5.51
CHEMBL451698 1 5.49
CHEMBL181 DIAZOXIDE 4.0 1 4.65
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 -
CHEMBL49035 CROMAKALIM 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112668 IC50 = 730.0 nM 6.14
CHEMBL447283 IC50 = 2260.0 nM 5.65
CHEMBL497955 IC50 = 2300.0 nM 5.64
CHEMBL497954 IC50 = 2590.0 nM 5.59
CHEMBL497956 IC50 = 2750.0 nM 5.56
CHEMBL526087 IC50 = 3120.0 nM 5.51
CHEMBL451698 IC50 = 3250.0 nM 5.49
CHEMBL181 DIAZOXIDE IC50 = 22600.0 nM 4.65
CHEMBL1159 PINACIDIL ANHYDROUS IC50 > 100000.0 nM -
CHEMBL49035 CROMAKALIM IC50 > 100000.0 nM -