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Assay Detail

CHEMBL672283

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

Binding
Binding affinity to CHO cells stably expressing human Endothelin B 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 receptor type B (CHEMBL1785)
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 4.62 5.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL149232 1 5.20
CHEMBL148719 1 5.03
CHEMBL359273 1 4.80
CHEMBL24461 1 4.73
CHEMBL149763 1 4.70
CHEMBL345951 1 4.70
CHEMBL147340 1 4.66
CHEMBL147238 1 4.51
CHEMBL149592 1 4.41
CHEMBL147365 1 4.32
CHEMBL150260 1 4.28
CHEMBL357077 1 4.12
CHEMBL149010 1 -
CHEMBL148855 1 -
CHEMBL149778 1 -
CHEMBL346862 1 -
CHEMBL149340 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL149232 Ki = 6300.0 nM 5.20
CHEMBL148719 Ki = 9400.0 nM 5.03
CHEMBL359273 Ki = 16000.0 nM 4.80
CHEMBL24461 Ki = 18700.0 nM 4.73
CHEMBL149763 Ki = 20000.0 nM 4.70
CHEMBL345951 Ki = 20000.0 nM 4.70
CHEMBL147340 Ki = 22000.0 nM 4.66
CHEMBL147238 Ki = 30800.0 nM 4.51
CHEMBL149592 Ki = 39000.0 nM 4.41
CHEMBL147365 Ki = 48000.0 nM 4.32
CHEMBL150260 Ki = 52000.0 nM 4.28
CHEMBL357077 Ki = 75000.0 nM 4.12
CHEMBL149010 Ki = 120000.0 nM -
CHEMBL148855 Ki = 150000.0 nM -
CHEMBL149778 Ki > 200000.0 nM -
CHEMBL346862 Ki = 130000.0 nM -
CHEMBL149340 Ki = 170000.0 nM -