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Assay Detail

CHEMBL866639

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Functional
Repolarization of beta-TC3 cells
22
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type Beta-TC3
Confidence 1 — Organism
Curated By Expert

Target

Beta-TC3 (CHEMBL614063)
Type CELL-LINE
Organism Mus musculus

Publication

New 3-alkylamino-4H-thieno-1,2,4-thiadiazine 1,1-dioxide derivatives activate ATP-sensitive potassium channels of pancreatic beta cells.
Nielsen FE, Ebdrup S, Jensen AF, Ynddal L, Bodvarsdottir TB, Stidsen C, Worsaae A, Boonen HC, Arkhammar PO, Fremming T, Wahl P, Kornø HT, Hansen JB.
J Med Chem (2006) 49 : 4127 -4139
PubMed 16821773 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 20 6.14 7.70
Emax 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134168 1 7.70
CHEMBL212041 1 6.89
CHEMBL210749 1 6.85
CHEMBL383992 1 6.80
CHEMBL212479 1 6.40
CHEMBL379292 1 6.32
CHEMBL210864 1 6.30
CHEMBL135191 TIFENAZOXIDE 2.0 1 6.30
CHEMBL208928 1 6.30
CHEMBL209313 1 5.70
CHEMBL445321 1 5.51
CHEMBL210948 2 5.46
CHEMBL378871 2 5.44
CHEMBL210673 1 5.30
CHEMBL181 DIAZOXIDE 4.0 1 4.86
CHEMBL438967 1 -
CHEMBL210419 1 -
CHEMBL210210 1 -
CHEMBL212476 1 -
CHEMBL441686 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134168 EC50 = 20.0 nM 7.70
CHEMBL212041 EC50 = 130.0 nM 6.89
CHEMBL210749 EC50 = 140.0 nM 6.85
CHEMBL383992 EC50 = 160.0 nM 6.80
CHEMBL212479 EC50 = 400.0 nM 6.40
CHEMBL379292 EC50 = 480.0 nM 6.32
CHEMBL135191 TIFENAZOXIDE EC50 = 500.0 nM 6.30
CHEMBL208928 EC50 = 500.0 nM 6.30
CHEMBL210864 EC50 = 500.0 nM 6.30
CHEMBL209313 EC50 = 2000.0 nM 5.70
CHEMBL445321 EC50 = 3100.0 nM 5.51
CHEMBL210948 EC50 = 3500.0 nM 5.46
CHEMBL378871 EC50 = 3600.0 nM 5.44
CHEMBL210673 EC50 = 5000.0 nM 5.30
CHEMBL181 DIAZOXIDE EC50 = 13700.0 nM 4.86
CHEMBL438967 EC50 > 30000.0 nM -
CHEMBL210419 EC50 - -
CHEMBL378871 Emax < 60.0 % -
CHEMBL210948 Emax < 60.0 % -
CHEMBL210210 EC50 - -
CHEMBL212476 EC50 - -
CHEMBL441686 EC50 - -