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Assay Detail

CHEMBL653239

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Functional
Inhibition of Beta-cell KATP channel
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Sulfonylurea receptor 1, Kir6.2 (CHEMBL2096972)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Synthesis and evaluation of 7-substituted-3-cyclobutylamino-4H-1,2,4-benzothiadiazine-1,1-dioxide derivatives as K(ATP) channel agonists.
Peat AJ, Townsend C, Worley JF, Allen SH, Garrido D, Mertz RJ, Pfohl JL, Terry CM, Truax JF, Veasey RL, Thomson SA.
Bioorg Med Chem Lett (2002) 12 : 2977 -2980
PubMed 12270187 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 5.73 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL318931 1 6.71
CHEMBL102025 1 6.45
CHEMBL100793 1 6.28
CHEMBL319596 1 5.71
CHEMBL319521 1 5.41
CHEMBL181 DIAZOXIDE 4.0 1 5.06
CHEMBL101736 1 4.51

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL318931 EC50 = 196.0 nM 6.71
CHEMBL102025 EC50 = 356.0 nM 6.45
CHEMBL100793 EC50 = 530.0 nM 6.28
CHEMBL319596 EC50 = 1960.0 nM 5.71
CHEMBL319521 EC50 = 3870.0 nM 5.41
CHEMBL181 DIAZOXIDE EC50 = 8800.0 nM 5.06
CHEMBL101736 EC50 = 31000.0 nM 4.51