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Assay Detail

CHEMBL914217

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

Functional
Inhibition of insulin release from rat INS-1E cells
6
Total Activities
6
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type INS-1E
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Virtual screening for novel openers of pancreatic K(ATP) channels.
Carosati E, Mannhold R, Wahl P, Hansen JB, Fremming T, Zamora I, Cianchetta G, Baroni M.
J Med Chem (2007) 50 : 2117 -2126
PubMed 17425298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 4.91 6.03
EC50 2 5.69 6.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL135191 TIFENAZOXIDE 2.0 1 6.68
CHEMBL112668 1 6.03
CHEMBL226918 1 4.75
CHEMBL181 DIAZOXIDE 4.0 1 4.69
CHEMBL226970 1 4.60
CHEMBL223230 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL135191 TIFENAZOXIDE EC50 = 210.0 nM 6.68
CHEMBL112668 IC50 = 940.0 nM 6.03
CHEMBL226918 IC50 = 18000.0 nM 4.75
CHEMBL181 DIAZOXIDE EC50 = 20280.0 nM 4.69
CHEMBL226970 IC50 = 25000.0 nM 4.60
CHEMBL223230 IC50 = 56000.0 nM 4.25