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Assay Detail

CHEMBL780354

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

Functional
Compound was tested for vasorelaxant activity on the basis of ability to relax endothelium-denuded rat aortic strips toned with 20 mM KCl
11
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Rattus norvegicus (CHEMBL376)
Type ORGANISM
Organism Rattus norvegicus

Publication

Novel potassium-channel openers: preparation and pharmacological evaluation of racemic and optically active N-(6-amino-3-pyridyl)-N'-bicycloalkyl-N"-cyanoguanidine derivatives.
Eda M, Takemoto T, Ono S, Okada T, Kosaka K, Gohda M, Matzno S, Nakamura N, Fukaya C.
J Med Chem (1994) 37 : 1983 -1990
PubMed 8027980 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 6.73 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL543813 2 7.15
CHEMBL291768 1 7.05
CHEMBL49035 CROMAKALIM 2.0 1 6.96
CHEMBL62216 1 6.93
CHEMBL543576 1 6.65
CHEMBL60202 2 6.57
CHEMBL1159 PINACIDIL ANHYDROUS 4.0 1 6.42
CHEMBL542385 1 6.41
CHEMBL1202785 1 6.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL543813 IC50 = 71.0 nM 7.15
CHEMBL543813 IC50 = 79.0 nM 7.10
CHEMBL291768 IC50 = 90.0 nM 7.05
CHEMBL49035 CROMAKALIM IC50 = 110.0 nM 6.96
CHEMBL62216 IC50 = 118.0 nM 6.93
CHEMBL543576 IC50 = 223.0 nM 6.65
CHEMBL60202 IC50 = 267.0 nM 6.57
CHEMBL60202 IC50 = 278.0 nM 6.56
CHEMBL1159 PINACIDIL ANHYDROUS IC50 = 380.0 nM 6.42
CHEMBL542385 IC50 = 392.0 nM 6.41
CHEMBL1202785 IC50 = 593.0 nM 6.23