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Assay Detail

CHEMBL972282

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

Functional
Myorelaxant activity in potassium depolarized Wistar rat aorta rings assessed as relaxation of KCl-induced contraction
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Aorta (CHEMBL613606)
Type TISSUE
Organism Rattus norvegicus

Publication

New R/S-3,4-dihydro-2,2-dimethyl-6-halo-4-(phenylaminothiocarbonylamino)-2H-1-benzopyrans structurally related to (+/-)-cromakalim as tissue-selective pancreatic beta-cell K(ATP) channel openers.
Sebille S, de Tullio P, Florence X, Becker B, Antoine MH, Michaux C, Wouters J, Pirotte B, Lebrun P.
Bioorg Med Chem (2008) 16 : 5704 -5719
PubMed 18406154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 34 5.16 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49035 CROMAKALIM 2.0 1 6.89
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 6.46
CHEMBL468836 1 5.54
CHEMBL502421 1 5.50
CHEMBL468387 1 5.26
CHEMBL468835 1 5.21
CHEMBL496089 1 5.19
CHEMBL468985 1 5.14
CHEMBL511582 1 5.12
CHEMBL468384 1 4.96
CHEMBL468634 1 4.96
CHEMBL513528 1 4.90
CHEMBL468973 1 4.67
CHEMBL181 DIAZOXIDE 4.0 1 4.65
CHEMBL469168 1 4.61
CHEMBL112668 1 4.44
CHEMBL448599 1 4.29
CHEMBL512113 1 -
CHEMBL468635 1 -
CHEMBL467555 1 -
CHEMBL467556 1 -
CHEMBL512264 1 -
CHEMBL468422 1 -
CHEMBL468570 1 -
CHEMBL513524 1 -
CHEMBL467766 1 -
CHEMBL501304 1 -
CHEMBL451698 1 -
CHEMBL526087 1 -
CHEMBL497954 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49035 CROMAKALIM EC50 = 130.0 nM 6.89
CHEMBL1159 PINACIDIL ANHYDROUS EC50 = 350.0 nM 6.46
CHEMBL468836 EC50 = 2900.0 nM 5.54
CHEMBL502421 EC50 = 3200.0 nM 5.50
CHEMBL468387 EC50 = 5500.0 nM 5.26
CHEMBL468835 EC50 = 6200.0 nM 5.21
CHEMBL496089 EC50 = 6500.0 nM 5.19
CHEMBL468985 EC50 = 7300.0 nM 5.14
CHEMBL511582 EC50 = 7600.0 nM 5.12
CHEMBL468384 EC50 = 11100.0 nM 4.96
CHEMBL468634 EC50 = 11100.0 nM 4.96
CHEMBL513528 EC50 = 12700.0 nM 4.90
CHEMBL468973 EC50 = 21600.0 nM 4.67
CHEMBL181 DIAZOXIDE EC50 = 22400.0 nM 4.65
CHEMBL469168 EC50 = 24400.0 nM 4.61
CHEMBL112668 EC50 = 36300.0 nM 4.44
CHEMBL448599 EC50 = 51500.0 nM 4.29
CHEMBL468986 EC50 = 137300.0 nM -
CHEMBL447283 EC50 > 10000.0 nM -
CHEMBL497956 EC50 > 10000.0 nM -
CHEMBL497955 EC50 > 10000.0 nM -
CHEMBL497954 EC50 > 10000.0 nM -
CHEMBL526087 EC50 > 10000.0 nM -
CHEMBL451698 EC50 > 10000.0 nM -
CHEMBL501304 EC50 > 10000.0 nM -
CHEMBL467766 EC50 > 10000.0 nM -
CHEMBL513524 EC50 > 10000.0 nM -
CHEMBL468570 EC50 > 10000.0 nM -
CHEMBL468422 EC50 > 30000.0 nM -
CHEMBL512264 EC50 > 30000.0 nM -
CHEMBL467556 EC50 > 30000.0 nM -
CHEMBL467555 EC50 > 30000.0 nM -
CHEMBL468635 EC50 > 30000.0 nM -
CHEMBL512113 EC50 > 30000.0 nM -