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Assay Detail

CHEMBL779272

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

Functional
Vasodilation effects on Wistar rat mesenteric arteries precontracted with phenylephrine
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 1 — Organism
Curated By Intermediate

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

6-Chloro-3-alkylamino-4H-thieno[3,2-e]-1,2,4-thiadiazine 1,1-dioxide derivatives potently and selectively activate ATP sensitive potassium channels of pancreatic beta-cells.
Nielsen FE, Bodvarsdottir TB, Worsaae A, MacKay P, Stidsen CE, Boonen HC, Pridal L, Arkhammar PO, Wahl P, Ynddal L, Junager F, Dragsted N, Tagmose TM, Mogensen JP, Koch A, Treppendahl SP, Hansen JB.
J Med Chem (2002) 45 : 4171 -4187
PubMed 12213059 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 4.72 5.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL131971 1 5.21
CHEMBL134168 1 5.14
CHEMBL132075 1 4.97
CHEMBL135191 TIFENAZOXIDE 2.0 1 4.84
CHEMBL3350270 1 4.72
CHEMBL181 DIAZOXIDE 4.0 1 4.68
CHEMBL133596 1 4.63
CHEMBL2111887 1 4.60
CHEMBL135091 1 4.53
CHEMBL133663 1 4.41
CHEMBL336586 1 4.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL131971 EC50 = 6200.0 nM 5.21
CHEMBL134168 EC50 = 7200.0 nM 5.14
CHEMBL132075 EC50 = 10800.0 nM 4.97
CHEMBL135191 TIFENAZOXIDE EC50 = 14300.0 nM 4.84
CHEMBL3350270 EC50 = 19200.0 nM 4.72
CHEMBL181 DIAZOXIDE EC50 = 20800.0 nM 4.68
CHEMBL133596 EC50 = 23300.0 nM 4.63
CHEMBL2111887 EC50 = 25200.0 nM 4.60
CHEMBL135091 EC50 = 29400.0 nM 4.53
CHEMBL133663 EC50 = 38600.0 nM 4.41
CHEMBL336586 EC50 = 60600.0 nM 4.22