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Assay Detail

CHEMBL679830

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

Binding
Binding affinity to CHO cells stably expressing human Endothelin A receptor.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biphenylsulfonamide endothelin receptor antagonists. Part 3: structure-activity relationship of 4'-heterocyclic biphenylsulfonamides.
Murugesan N, Gu Z, Stein PD, Spergel S, Bisaha S, Liu EC, Zhang R, Webb ML, Moreland S, Barrish JC.
Bioorg Med Chem Lett (2002) 12 : 517 -520
PubMed 11844662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.69 9.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL359273 1 9.05
CHEMBL24461 1 8.85
CHEMBL149232 1 8.64
CHEMBL345951 1 8.48
CHEMBL357077 1 8.40
CHEMBL150260 1 8.25
CHEMBL147340 1 8.21
CHEMBL148719 1 8.17
CHEMBL149010 1 7.72
CHEMBL346862 1 7.60
CHEMBL147238 1 7.43
CHEMBL149763 1 7.42
CHEMBL148855 1 7.36
CHEMBL147365 1 6.66
CHEMBL149592 1 6.57
CHEMBL149340 1 6.52
CHEMBL149778 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL359273 Ki = 0.9 nM 9.05
CHEMBL24461 Ki = 1.4 nM 8.85
CHEMBL149232 Ki = 2.3 nM 8.64
CHEMBL345951 Ki = 3.3 nM 8.48
CHEMBL357077 Ki = 4.0 nM 8.40
CHEMBL150260 Ki = 5.6 nM 8.25
CHEMBL147340 Ki = 6.2 nM 8.21
CHEMBL148719 Ki = 6.7 nM 8.17
CHEMBL149010 Ki = 19.0 nM 7.72
CHEMBL346862 Ki = 25.0 nM 7.60
CHEMBL147238 Ki = 37.0 nM 7.43
CHEMBL149763 Ki = 38.0 nM 7.42
CHEMBL148855 Ki = 44.0 nM 7.36
CHEMBL147365 Ki = 220.0 nM 6.66
CHEMBL149592 Ki = 270.0 nM 6.57
CHEMBL149340 Ki = 300.0 nM 6.52
CHEMBL149778 Ki = 3800.0 nM 5.42