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Assay Detail

CHEMBL679113

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Binding
Concentration required to inhibit 50% Et-1 binding to endothelin A receptor in rat A-10 cells.
29
Total Activities
29
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type A10
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Selective endothelin A receptor antagonists. 4. Discovery and structure-activity relationships of stilbene acid and alcohol derivatives.
Astles PC, Brown TJ, Halley F, Handscombe CM, Harris NV, McCarthy C, McLay IM, Lockey P, Majid T, Porter B, Roach AG, Smith C, Walsh R.
J Med Chem (1998) 41 : 2745 -2753
PubMed 9667965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 6.11 8.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL90320 1 8.10
CHEMBL328600 1 7.10
CHEMBL92842 1 6.82
CHEMBL330255 1 6.70
CHEMBL433201 1 6.70
CHEMBL91810 1 6.52
CHEMBL90191 1 6.52
CHEMBL93411 1 6.40
CHEMBL328786 1 6.30
CHEMBL90666 1 6.22
CHEMBL330543 1 6.22
CHEMBL328580 1 6.22
CHEMBL328057 1 6.16
CHEMBL328464 1 6.16
CHEMBL419694 1 6.10
CHEMBL92446 1 6.05
CHEMBL328964 1 6.00
CHEMBL327861 1 5.96
CHEMBL328444 1 5.89
CHEMBL91741 1 5.89
CHEMBL93596 1 5.85
CHEMBL91965 1 5.70
CHEMBL92570 1 5.70
CHEMBL92876 1 5.68
CHEMBL90094 1 5.52
CHEMBL92092 1 5.51
CHEMBL92402 1 5.28
CHEMBL92607 1 5.22
CHEMBL96836 1 4.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL90320 IC50 = 8.0 nM 8.10
CHEMBL328600 IC50 = 80.0 nM 7.10
CHEMBL92842 IC50 = 150.0 nM 6.82
CHEMBL330255 IC50 = 200.0 nM 6.70
CHEMBL433201 IC50 = 200.0 nM 6.70
CHEMBL91810 IC50 = 300.0 nM 6.52
CHEMBL90191 IC50 = 300.0 nM 6.52
CHEMBL93411 IC50 = 400.0 nM 6.40
CHEMBL328786 IC50 = 500.0 nM 6.30
CHEMBL90666 IC50 = 600.0 nM 6.22
CHEMBL330543 IC50 = 600.0 nM 6.22
CHEMBL328580 IC50 = 600.0 nM 6.22
CHEMBL328057 IC50 = 700.0 nM 6.16
CHEMBL328464 IC50 = 700.0 nM 6.16
CHEMBL419694 IC50 = 800.0 nM 6.10
CHEMBL92446 IC50 = 900.0 nM 6.05
CHEMBL328964 IC50 = 1000.0 nM 6.00
CHEMBL327861 IC50 = 1100.0 nM 5.96
CHEMBL328444 IC50 = 1300.0 nM 5.89
CHEMBL91741 IC50 = 1300.0 nM 5.89
CHEMBL93596 IC50 = 1400.0 nM 5.85
CHEMBL91965 IC50 = 2000.0 nM 5.70
CHEMBL92570 IC50 = 2000.0 nM 5.70
CHEMBL92876 IC50 = 2100.0 nM 5.68
CHEMBL90094 IC50 = 3000.0 nM 5.52
CHEMBL92092 IC50 = 3100.0 nM 5.51
CHEMBL92402 IC50 = 5300.0 nM 5.28
CHEMBL92607 IC50 = 6000.0 nM 5.22
CHEMBL96836 IC50 = 20000.0 nM 4.70