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Assay Detail

CHEMBL687336

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

Functional
Contraction and relaxation of guinea pig portal vein with KCl and glibenclamide respectively
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Tissue Portal vein
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Sulfonylurea receptors; K-ATP channels (CHEMBL2095152)
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

N-aryl-3,3,3-trifluoro-2-hydroxy-2-methylpropanamides: KATP potassium channel openers. Modifications on the western region.
Ohnmacht CJ, Russell K, Empfield JR, Frank CA, Gibson KH, Mayhugh DR, McLaren FM, Shapiro HS, Brown FJ, Trainor DA, Ceccarelli C, Lin MM, Masek BB, Forst JM, Harris RJ, Hulsizer JM, Lewis JJ, Silverman SM, Smith RW, Warwick PJ, Kau ST, Chun AL, Grant TL, Howe BB, Neilson KL.
J Med Chem (1996) 39 : 4592 -4601
PubMed 8917648 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.38 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL49035 CROMAKALIM 2.0 1 7.70
CHEMBL143181 1 7.36
CHEMBL70996 1 7.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL49035 CROMAKALIM IC50 = 20.0 nM 7.70
CHEMBL143181 IC50 = 44.0 nM 7.36
CHEMBL70996 IC50 = 82.0 nM 7.09