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Assay Detail

CHEMBL673234

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Binding
Inhibitory activity against human endothelin B receptor expressed in CHO cells
ChEMBL ↗
42
Total Activities
42
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. 4. Discovery of N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]- 2-yl]methyl]-N,3,3-trimethylbutanamide (BMS-207940), a highly potent and orally active ET(A) selective antagonist.
Murugesan N, Gu Z, Spergel S, Young M, Chen P, Mathur A, Leith L, Hermsmeier M, Liu EC, Zhang R, Bird E, Waldron T, Marino A, Koplowitz B, Humphreys WG, Chong S, Morrison RA, Webb ML, Moreland S, Trippodo N, Barrish JC.
J Med Chem (2003) 46 : 125 -137
PubMed 12502366 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 42 5.88 7.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL957 BOSENTAN 4.0 1 7.10
CHEMBL440780 — — 1 7.06
CHEMBL29793 — — 1 6.82
CHEMBL29972 — — 1 6.57
CHEMBL281977 — — 1 6.51
CHEMBL30150 — — 1 6.50
CHEMBL283610 — — 1 6.44
CHEMBL281549 — — 1 6.42
CHEMBL28963 — — 1 6.26
CHEMBL282359 — — 1 6.24
CHEMBL27855 — — 1 6.19
CHEMBL2113316 — — 1 6.11
CHEMBL28863 — — 1 6.10
CHEMBL274489 — — 1 6.09
CHEMBL30405 — — 1 6.02
CHEMBL29464 — — 1 6.01
CHEMBL29223 — — 1 5.98
CHEMBL30215 — — 1 5.96
CHEMBL29346 — — 1 5.92
CHEMBL282628 — — 1 5.89
CHEMBL282336 — — 1 5.85
CHEMBL30092 — — 1 5.85
CHEMBL285832 — — 1 5.82
CHEMBL29775 — — 1 5.77
CHEMBL29598 — — 1 5.77
CHEMBL29313 — — 1 5.72
CHEMBL431296 — — 1 5.72
CHEMBL29502 — — 1 5.64
CHEMBL29710 — — 1 5.60
CHEMBL29420 — — 1 5.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL957 BOSENTAN Ki = 80.0 nM 7.10
CHEMBL440780 — Ki = 87.0 nM 7.06
CHEMBL29793 — Ki = 150.0 nM 6.82
CHEMBL29972 — Ki = 270.0 nM 6.57
CHEMBL281977 — Ki = 310.0 nM 6.51
CHEMBL30150 — Ki = 320.0 nM 6.50
CHEMBL283610 — Ki = 360.0 nM 6.44
CHEMBL281549 — Ki = 380.0 nM 6.42
CHEMBL28963 — Ki = 550.0 nM 6.26
CHEMBL282359 — Ki = 580.0 nM 6.24
CHEMBL27855 — Ki = 640.0 nM 6.19
CHEMBL2113316 — Ki = 770.0 nM 6.11
CHEMBL28863 — Ki = 790.0 nM 6.10
CHEMBL274489 — Ki = 810.0 nM 6.09
CHEMBL30405 — Ki = 950.0 nM 6.02
CHEMBL29464 — Ki = 980.0 nM 6.01
CHEMBL29223 — Ki = 1050.0 nM 5.98
CHEMBL30215 — Ki = 1100.0 nM 5.96
CHEMBL29346 — Ki = 1200.0 nM 5.92
CHEMBL282628 — Ki = 1300.0 nM 5.89
CHEMBL30092 — Ki = 1400.0 nM 5.85
CHEMBL282336 — Ki = 1400.0 nM 5.85
CHEMBL285832 — Ki = 1500.0 nM 5.82
CHEMBL29775 — Ki = 1700.0 nM 5.77
CHEMBL29598 — Ki = 1700.0 nM 5.77
CHEMBL29313 — Ki = 1900.0 nM 5.72
CHEMBL431296 — Ki = 1900.0 nM 5.72
CHEMBL29502 — Ki = 2300.0 nM 5.64
CHEMBL29710 — Ki = 2500.0 nM 5.60
CHEMBL29420 — Ki = 2700.0 nM 5.57
CHEMBL29652 — Ki = 2800.0 nM 5.55
CHEMBL281659 — Ki = 3360.0 nM 5.47
CHEMBL284656 — Ki = 4000.0 nM 5.40
CHEMBL30009 — Ki = 4300.0 nM 5.37
CHEMBL29422 — Ki = 4400.0 nM 5.36
CHEMBL28586 — Ki = 4600.0 nM 5.34
CHEMBL282303 — Ki = 4800.0 nM 5.32
CHEMBL281668 — Ki = 7300.0 nM 5.14
CHEMBL286279 — Ki = 9100.0 nM 5.04
CHEMBL285118 — Ki = 11000.0 nM 4.96
CHEMBL24461 — Ki = 18700.0 nM 4.73
CHEMBL281869 — Ki > 50000.0 nM -