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Assay Detail

CHEMBL770812

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

Functional
Compound was evaluated for the functional assay performed by obtaining ET-1 concentration-response curves [pA2(ETB)] in isolated rabbit jugularis vein
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 1 — Organism
Curated By Intermediate

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Endothelin antagonists: discovery of EMD 122946, a highly potent and orally active ETA selective antagonist.
Mederski WW, Dorsch D, Osswald M, Anzali S, Christadler M, Schmitges CJ, Schelling P, Wilm C, Fluck M.
Bioorg Med Chem Lett (1998) 8 : 1771 -1776
PubMed 9873432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 6.07 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL48907 1 6.10
CHEMBL9194 ATRASENTAN 3.0 1 6.10
CHEMBL298725 1 6.00
CHEMBL25438 PD-156707 SODIUM 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL48907 Kd = 794.33 nM 6.10
CHEMBL9194 ATRASENTAN Kd = 794.33 nM 6.10
CHEMBL298725 Kd = 1000.0 nM 6.00
CHEMBL25438 PD-156707 SODIUM Kd > 3162.28 nM -