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Assay Detail

CHEMBL780694

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

Functional
Ability to relax phenylephrine-contracted rat aorta rings
31
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 1 — Organism
Curated By Expert

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 31 4.90 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL442023 1 6.82
CHEMBL135145 1 5.85
CHEMBL134039 1 5.70
CHEMBL134255 1 5.70
CHEMBL341410 1 5.48
CHEMBL336621 1 5.21
CHEMBL134168 1 5.19
CHEMBL337442 1 5.17
CHEMBL334826 1 5.10
CHEMBL135091 1 4.93
CHEMBL335640 1 4.87
CHEMBL341435 1 4.76
CHEMBL135240 1 4.69
CHEMBL134254 1 4.60
CHEMBL133663 1 4.57
CHEMBL133699 1 4.55
CHEMBL136005 1 4.46
CHEMBL3350270 1 4.29
CHEMBL133596 1 4.19
CHEMBL134220 1 4.19
CHEMBL2111887 1 4.16
CHEMBL3350271 1 4.12
CHEMBL134120 1 4.08
CHEMBL135191 TIFENAZOXIDE 2.0 1 -
CHEMBL2111888 1 -
CHEMBL131971 1 -
CHEMBL134253 1 -
CHEMBL132075 1 -
CHEMBL336586 1 -
CHEMBL335477 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL442023 EC50 = 150.0 nM 6.82
CHEMBL135145 EC50 = 1400.0 nM 5.85
CHEMBL134039 EC50 = 2000.0 nM 5.70
CHEMBL134255 EC50 = 2000.0 nM 5.70
CHEMBL341410 EC50 = 3300.0 nM 5.48
CHEMBL336621 EC50 = 6200.0 nM 5.21
CHEMBL134168 EC50 = 6500.0 nM 5.19
CHEMBL337442 EC50 = 6800.0 nM 5.17
CHEMBL334826 EC50 = 8000.0 nM 5.10
CHEMBL135091 EC50 = 11800.0 nM 4.93
CHEMBL335640 EC50 = 13400.0 nM 4.87
CHEMBL341435 EC50 = 17300.0 nM 4.76
CHEMBL135240 EC50 = 20500.0 nM 4.69
CHEMBL134254 EC50 = 25200.0 nM 4.60
CHEMBL133663 EC50 = 27000.0 nM 4.57
CHEMBL133699 EC50 = 28200.0 nM 4.55
CHEMBL136005 EC50 = 34800.0 nM 4.46
CHEMBL3350270 EC50 = 51000.0 nM 4.29
CHEMBL133596 EC50 = 64700.0 nM 4.19
CHEMBL134220 EC50 = 65000.0 nM 4.19
CHEMBL2111887 EC50 = 70000.0 nM 4.16
CHEMBL3350271 EC50 = 75300.0 nM 4.12
CHEMBL134120 EC50 = 83000.0 nM 4.08
CHEMBL135191 TIFENAZOXIDE EC50 = 119200.0 nM -
CHEMBL2111888 EC50 > 300000.0 nM -
CHEMBL131971 EC50 = 266000.0 nM -
CHEMBL134253 EC50 = 176200.0 nM -
CHEMBL132075 EC50 > 300000.0 nM -
CHEMBL336586 EC50 = 169000.0 nM -
CHEMBL335477 EC50 = 135500.0 nM -
CHEMBL445330 EC50 = 262000.0 nM -