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Assay Detail

CHEMBL655070

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Functional
Changes in potassium fluxes assessed in the glucose responsive insulin-producing murine cell line beta-TC3
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Murine cell line
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 30 5.95 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134168 1 7.85
CHEMBL336621 1 7.10
CHEMBL341410 1 7.00
CHEMBL442023 1 6.70
CHEMBL135091 1 6.70
CHEMBL3350271 1 6.52
CHEMBL2111887 1 6.52
CHEMBL336586 1 6.40
CHEMBL134255 1 6.40
CHEMBL132075 1 6.40
CHEMBL134253 1 6.30
CHEMBL135191 TIFENAZOXIDE 2.0 1 6.22
CHEMBL131971 1 6.22
CHEMBL335640 1 6.22
CHEMBL3350270 1 6.10
CHEMBL135145 1 6.00
CHEMBL134220 1 5.89
CHEMBL133663 1 5.85
CHEMBL133596 1 5.70
CHEMBL134254 1 5.70
CHEMBL337442 1 5.10
CHEMBL335477 1 5.05
CHEMBL2111888 1 4.85
CHEMBL134039 1 4.77
CHEMBL135240 1 4.70
CHEMBL134120 1 4.39
CHEMBL181 DIAZOXIDE 4.0 1 4.11
CHEMBL133699 1 -
CHEMBL334826 1 -
CHEMBL341435 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134168 EC50 = 14.0 nM 7.85
CHEMBL336621 EC50 = 80.0 nM 7.10
CHEMBL341410 EC50 = 100.0 nM 7.00
CHEMBL442023 EC50 = 200.0 nM 6.70
CHEMBL135091 EC50 = 200.0 nM 6.70
CHEMBL3350271 EC50 = 300.0 nM 6.52
CHEMBL2111887 EC50 = 300.0 nM 6.52
CHEMBL336586 EC50 = 400.0 nM 6.40
CHEMBL134255 EC50 = 400.0 nM 6.40
CHEMBL132075 EC50 = 400.0 nM 6.40
CHEMBL134253 EC50 = 500.0 nM 6.30
CHEMBL135191 TIFENAZOXIDE EC50 = 600.0 nM 6.22
CHEMBL131971 EC50 = 600.0 nM 6.22
CHEMBL335640 EC50 = 600.0 nM 6.22
CHEMBL3350270 EC50 = 800.0 nM 6.10
CHEMBL135145 EC50 = 1000.0 nM 6.00
CHEMBL134220 EC50 = 1300.0 nM 5.89
CHEMBL133663 EC50 = 1400.0 nM 5.85
CHEMBL133596 EC50 = 2000.0 nM 5.70
CHEMBL134254 EC50 = 2000.0 nM 5.70
CHEMBL337442 EC50 = 8000.0 nM 5.10
CHEMBL335477 EC50 = 9000.0 nM 5.05
CHEMBL2111888 EC50 = 14000.0 nM 4.85
CHEMBL134039 EC50 = 17000.0 nM 4.77
CHEMBL135240 EC50 = 20000.0 nM 4.70
CHEMBL134120 EC50 = 41000.0 nM 4.39
CHEMBL181 DIAZOXIDE EC50 = 77400.0 nM 4.11
CHEMBL133699 EC50 > 30000.0 nM -
CHEMBL334826 EC50 > 100000.0 nM -
CHEMBL341435 EC50 > 100000.0 nM -