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Assay Detail

CHEMBL677307

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

Binding
Compound was tested for binding affinity against Endothelin A receptor
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-1 receptor (CHEMBL252)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Thiophenesulfonamides as endothelin receptor antagonists
Raju B, Wu C, Kois A, Verner E, Okun I, Stavros F, Chan MF
Bioorg Med Chem Lett (1996) 6 : 2651 -2656
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.36 7.79

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL80857 1 7.79
CHEMBL316012 1 7.37
CHEMBL432815 1 7.32
CHEMBL328517 1 7.08
CHEMBL329890 1 7.06
CHEMBL89688 1 7.00
CHEMBL313801 1 6.94
CHEMBL329560 1 6.80
CHEMBL89203 1 6.74
CHEMBL314307 1 6.74
CHEMBL330674 1 6.66
CHEMBL313551 1 6.51
CHEMBL91073 1 6.50
CHEMBL89689 1 6.48
CHEMBL293232 1 6.22
CHEMBL88506 1 6.09
CHEMBL328089 1 6.08
CHEMBL329861 1 5.88
CHEMBL89457 1 5.84
CHEMBL330003 1 5.77
CHEMBL91470 1 5.72
CHEMBL78080 1 5.60
CHEMBL92318 1 5.58
CHEMBL265290 1 5.56
CHEMBL329375 1 5.47
CHEMBL314320 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL80857 IC50 = 16.2 nM 7.79
CHEMBL316012 IC50 = 42.85 nM 7.37
CHEMBL432815 IC50 = 47.9 nM 7.32
CHEMBL328517 IC50 = 82.3 nM 7.08
CHEMBL329890 IC50 = 87.3 nM 7.06
CHEMBL89688 IC50 = 100.2 nM 7.00
CHEMBL313801 IC50 = 115.0 nM 6.94
CHEMBL329560 IC50 = 159.6 nM 6.80
CHEMBL89203 IC50 = 184.0 nM 6.74
CHEMBL314307 IC50 = 182.0 nM 6.74
CHEMBL330674 IC50 = 217.5 nM 6.66
CHEMBL313551 IC50 = 306.0 nM 6.51
CHEMBL91073 IC50 = 315.5 nM 6.50
CHEMBL89689 IC50 = 334.0 nM 6.48
CHEMBL293232 IC50 = 603.0 nM 6.22
CHEMBL88506 IC50 = 819.0 nM 6.09
CHEMBL328089 IC50 = 832.0 nM 6.08
CHEMBL329861 IC50 = 1320.0 nM 5.88
CHEMBL89457 IC50 = 1450.0 nM 5.84
CHEMBL330003 IC50 = 1710.0 nM 5.77
CHEMBL91470 IC50 = 1910.0 nM 5.72
CHEMBL78080 IC50 = 2510.0 nM 5.60
CHEMBL92318 IC50 = 2603.0 nM 5.58
CHEMBL265290 IC50 = 2750.0 nM 5.56
CHEMBL329375 IC50 = 3390.0 nM 5.47
CHEMBL314320 IC50 = 36600.0 nM 4.44