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Assay Detail

CHEMBL677400

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

Binding
Inhibition of ET-1 binding to Endothelin B receptor in cultured rat cerebellar membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Subcellular Membrane
Confidence 9 — Direct single protein target
Curated By Expert

Target

Endothelin receptor type B (CHEMBL4631)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Design of a functional hexapeptide antagonist of endothelin.
Cody WL, Doherty AM, He JX, DePue PL, Rapundalo ST, Hingorani GA, Major TC, Panek RL, Dudley DT, Haleen SJ.
J Med Chem (1992) 35 : 3301 -3303
PubMed 1324321 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 5.80 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437472 ENDOTHELIN 2.0 1 8.80
CHEMBL328942 1 6.82
CHEMBL317064 1 5.75
CHEMBL86814 1 5.48
CHEMBL438194 1 5.46
CHEMBL315047 1 5.40
CHEMBL85341 1 5.16
CHEMBL289687 1 5.00
CHEMBL432091 1 4.37
CHEMBL34540 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437472 ENDOTHELIN IC50 = 1.6 nM 8.80
CHEMBL328942 IC50 = 150.0 nM 6.82
CHEMBL317064 IC50 = 1800.0 nM 5.75
CHEMBL86814 IC50 = 3300.0 nM 5.48
CHEMBL438194 IC50 = 3500.0 nM 5.46
CHEMBL315047 IC50 = 4000.0 nM 5.40
CHEMBL85341 IC50 = 7000.0 nM 5.16
CHEMBL289687 IC50 = 10000.0 nM 5.00
CHEMBL432091 IC50 = 43000.0 nM 4.37
CHEMBL34540 IC50 > 50000.0 nM -