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Assay Detail

CHEMBL5340647

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

Functional
Vasorelaxant activity in New Zealand White rabbits aortic rings assessed as reduction in phenylephrine-induced contraction measured after 30 mins
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Tissue Aorta
Confidence 1 — Organism
Curated By Autocuration

Target

Aorta (CHEMBL4651286)
Type TISSUE
Organism Oryctolagus cuniculus

Publication

New Generation of sGC Stimulators: Discovery of Imidazo[1,2-<i>a</i>]pyridine Carboxamide BAY 1165747 (BAY-747), a Long-Acting Soluble Guanylate Cyclase Stimulator for the Treatment of Resistant Hypertension.
Vakalopoulos A, Wunder F, Hartung IV, Redlich G, Jautelat R, Buchgraber P, Hassfeld J, Gromov AV, Lindner N, Bierer D, Gries J, Kroh W, Paulsen H, Mittendorf J, Lang D, Becker-Pelster E, Brockschnieder D, Geiss V, Li V, Straub A, Knorr A, Mondritzki T, Trübel H, Raschke M, Schaefer M, Thomas D, Sandner P, Stasch JP, Follmann M.
J Med Chem (2023) 66 : 7280 -7303
PubMed 37040336 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.62 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5425229 1 7.57
CHEMBL5415811 1 6.20
CHEMBL5435708 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5425229 IC50 = 27.0 nM 7.57
CHEMBL5415811 IC50 = 625.0 nM 6.20
CHEMBL5435708 IC50 = 840.0 nM 6.08