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Assay Detail

CHEMBL872971

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Functional
Inhibitory concentration against methoxamine-induced contractions in rat aorta
14
Total Activities
13
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

Binding of ATP-sensitive potassium channel (KATP) openers to cardiac membranes: correlation of binding affinities with cardioprotective and smooth muscle relaxing potencies.
Atwal KS, Grover GJ, Lodge NJ, Normandin DE, Traeger SC, Sleph PG, Cohen RB, Bryson CC, Dickinson KE.
J Med Chem (1998) 41 : 271 -275
PubMed 9464357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 6.67 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL328308 1 8.85
CHEMBL11458 1 8.36
CHEMBL19169 1 7.52
CHEMBL11684 (-)-CROMAKALIM 2 7.40
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 7.22
CHEMBL93196 1 6.89
CHEMBL93834 1 6.72
CHEMBL328082 1 6.28
CHEMBL93835 1 6.01
CHEMBL96267 1 4.89
CHEMBL90665 1 4.72
CHEMBL90631 1 -
CHEMBL327884 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL328308 IC50 = 1.4 nM 8.85
CHEMBL11458 IC50 = 4.4 nM 8.36
CHEMBL19169 IC50 = 30.3 nM 7.52
CHEMBL11684 (-)-CROMAKALIM IC50 = 40.1 nM 7.40
CHEMBL1159 PINACIDIL ANHYDROUS IC50 = 59.6 nM 7.22
CHEMBL93196 IC50 = 130.0 nM 6.89
CHEMBL93834 IC50 = 190.0 nM 6.72
CHEMBL328082 IC50 = 530.0 nM 6.28
CHEMBL93835 IC50 = 980.0 nM 6.01
CHEMBL11684 (-)-CROMAKALIM IC50 = 6500.0 nM 5.19
CHEMBL96267 IC50 = 12800.0 nM 4.89
CHEMBL90665 IC50 = 19000.0 nM 4.72
CHEMBL90631 IC50 = 130000.0 nM -
CHEMBL327884 IC50 > 30.0 nM -