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Assay Detail

CHEMBL673226

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

Binding
Inhibition of Human Endothelin B receptor expressed in CHO Cells.
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Endothelin receptor type B (CHEMBL1785)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Biphenylsulfonamide endothelin receptor antagonists. 2. Discovery of 4'-oxazolyl biphenylsulfonamides as a new class of potent, highly selective ET(A) antagonists.
Murugesan N, Gu Z, Stein PD, Spergel S, Mathur A, Leith L, Liu EC, Zhang R, Bird E, Waldron T, Marino A, Morrison RA, Webb ML, Moreland S, Barrish JC.
J Med Chem (2000) 43 : 3111 -3117
PubMed 10956219 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 4.64 5.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105490 1 5.77
CHEMBL29422 1 5.36
CHEMBL106749 1 4.92
CHEMBL322674 1 4.92
CHEMBL24461 1 4.73
CHEMBL104848 1 4.70
CHEMBL319924 1 4.47
CHEMBL107574 1 4.11
CHEMBL319036 1 4.03
CHEMBL104172 1 4.03
CHEMBL104223 1 4.00
CHEMBL106846 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105490 Ki = 1700.0 nM 5.77
CHEMBL29422 Ki = 4400.0 nM 5.36
CHEMBL106749 Ki = 12000.0 nM 4.92
CHEMBL322674 Ki = 12000.0 nM 4.92
CHEMBL24461 Ki = 18700.0 nM 4.73
CHEMBL104848 Ki = 20000.0 nM 4.70
CHEMBL319924 Ki = 34000.0 nM 4.47
CHEMBL107574 Ki = 78000.0 nM 4.11
CHEMBL319036 Ki = 94000.0 nM 4.03
CHEMBL104172 Ki = 94000.0 nM 4.03
CHEMBL104223 Ki = 100000.0 nM 4.00
CHEMBL106846 Ki = 110000.0 nM -