Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL676101

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

Binding
Binding affinity towards Endothelin A receptor in A10 rat thoracic aorta smooth muscle cells using [125I]ET1 as radioligand
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Tissue Thoracic aorta
Cell Type A10
Confidence 9 — Direct single protein target
Curated By Expert

Target

Endothelin-1 receptor (CHEMBL4566)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Structure-activity relationships of monocyclic endothelin analogs
Hunt JT, Lee VG, Stein PD, Hedberg A, Liu EC, McMullen D, Moreland S
Bioorg Med Chem Lett (1991) 1 : 33 -38
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 11 6.79 9.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437472 ENDOTHELIN 2.0 1 9.82
CHEMBL263581 1 8.68
CHEMBL412346 1 7.29
CHEMBL438470 1 6.89
CHEMBL386629 1 6.73
CHEMBL268318 1 6.19
CHEMBL407887 1 6.03
CHEMBL410001 1 5.51
CHEMBL125377 1 5.41
CHEMBL409578 1 5.32
CHEMBL1790883 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437472 ENDOTHELIN Kd = 0.15 nM 9.82
CHEMBL263581 Kd = 2.109 nM 8.68
CHEMBL412346 Kd = 51.9 nM 7.29
CHEMBL438470 Kd = 130.0 nM 6.89
CHEMBL386629 Kd = 188.0 nM 6.73
CHEMBL268318 Kd = 646.0 nM 6.19
CHEMBL407887 Kd = 929.0 nM 6.03
CHEMBL410001 Kd = 3074.0 nM 5.51
CHEMBL125377 Kd = 3920.0 nM 5.41
CHEMBL409578 Kd = 4778.0 nM 5.32
CHEMBL1790883 Kd > 20000.0 nM -