Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL677439

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

Binding
Binding affinity against human Endothelin B receptor in transfected COS 7 cell membrane preparation
ChEMBL ↗
56
Total Activities
56
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type COS 7
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Halogen substitution at the isoxazole ring enhances the activity of N-(isoxazolyl)sulfonamide endothelin antagonists
Ming Fai Chan, Raju B, Kois A, Castillo RS, Verner EJ, Chengde Wu, Emily Hwang, Okun I, Stavros F, Balaji V
Bioorg Med Chem Lett (1996) 6 : 2393 -2398
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 56 4.80 6.03

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL78563 — — 1 6.03
CHEMBL80538 — — 1 5.96
CHEMBL311510 — — 1 5.92
CHEMBL430822 — — 1 5.47
CHEMBL79080 — — 1 5.42
CHEMBL76438 — — 1 5.40
CHEMBL311742 — — 1 5.33
CHEMBL417651 — — 1 5.31
CHEMBL309692 — — 1 5.28
CHEMBL311138 — — 1 5.28
CHEMBL312187 — — 1 5.28
CHEMBL80342 — — 1 5.18
CHEMBL80507 — — 1 5.17
CHEMBL78552 — — 1 5.16
CHEMBL80857 — — 1 5.10
CHEMBL79031 — — 1 5.03
CHEMBL311216 — — 1 4.96
CHEMBL310739 — — 1 4.89
CHEMBL420029 — — 1 4.89
CHEMBL312685 — — 1 4.89
CHEMBL80808 — — 1 4.89
CHEMBL311461 — — 1 4.85
CHEMBL80129 — — 1 4.85
CHEMBL78734 — — 1 4.85
CHEMBL80484 — — 1 4.82
CHEMBL78952 — — 1 4.82
CHEMBL79066 — — 1 4.77
CHEMBL76779 — — 1 4.70
CHEMBL78080 — — 1 4.70
CHEMBL78669 — — 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL78563 — IC50 = 930.0 nM 6.03
CHEMBL80538 — IC50 = 1100.0 nM 5.96
CHEMBL311510 — IC50 = 1200.0 nM 5.92
CHEMBL430822 — IC50 = 3400.0 nM 5.47
CHEMBL79080 — IC50 = 3800.0 nM 5.42
CHEMBL76438 — IC50 = 4000.0 nM 5.40
CHEMBL311742 — IC50 = 4700.0 nM 5.33
CHEMBL417651 — IC50 = 4900.0 nM 5.31
CHEMBL309692 — IC50 = 5200.0 nM 5.28
CHEMBL311138 — IC50 = 5200.0 nM 5.28
CHEMBL312187 — IC50 = 5300.0 nM 5.28
CHEMBL80342 — IC50 = 6600.0 nM 5.18
CHEMBL80507 — IC50 = 6700.0 nM 5.17
CHEMBL78552 — IC50 = 7000.0 nM 5.16
CHEMBL80857 — IC50 = 7900.0 nM 5.10
CHEMBL79031 — IC50 = 9400.0 nM 5.03
CHEMBL311216 — IC50 = 11000.0 nM 4.96
CHEMBL310739 — IC50 = 13000.0 nM 4.89
CHEMBL420029 — IC50 = 13000.0 nM 4.89
CHEMBL312685 — IC50 = 13000.0 nM 4.89
CHEMBL80808 — IC50 = 13000.0 nM 4.89
CHEMBL311461 — IC50 = 14000.0 nM 4.85
CHEMBL80129 — IC50 = 14000.0 nM 4.85
CHEMBL78734 — IC50 = 14000.0 nM 4.85
CHEMBL78952 — IC50 = 15000.0 nM 4.82
CHEMBL80484 — IC50 = 15000.0 nM 4.82
CHEMBL79066 — IC50 = 17000.0 nM 4.77
CHEMBL76779 — IC50 = 20000.0 nM 4.70
CHEMBL78080 — IC50 = 20000.0 nM 4.70
CHEMBL78669 — IC50 = 22000.0 nM 4.66
CHEMBL78830 — IC50 = 23000.0 nM 4.64
CHEMBL453 SULFISOXAZOLE IC50 = 24000.0 nM 4.62
CHEMBL421523 — IC50 = 24000.0 nM 4.62
CHEMBL78853 — IC50 = 24000.0 nM 4.62
CHEMBL309397 — IC50 = 25000.0 nM 4.60
CHEMBL76576 — IC50 = 25000.0 nM 4.60
CHEMBL311781 — IC50 = 26000.0 nM 4.58
CHEMBL80807 — IC50 = 27000.0 nM 4.57
CHEMBL78601 — IC50 = 29000.0 nM 4.54
CHEMBL80945 — IC50 = 30000.0 nM 4.52
CHEMBL80317 — IC50 = 33000.0 nM 4.48
CHEMBL310361 — IC50 = 35000.0 nM 4.46
CHEMBL80438 — IC50 = 37000.0 nM 4.43
CHEMBL79030 — IC50 = 38000.0 nM 4.42
CHEMBL312266 — IC50 = 39000.0 nM 4.41
CHEMBL78929 — IC50 = 45000.0 nM 4.35
CHEMBL76949 — IC50 = 47000.0 nM 4.33
CHEMBL81593 — IC50 = 49000.0 nM 4.31
CHEMBL80532 — IC50 = 58000.0 nM 4.24
CHEMBL26522 — IC50 = 57000.0 nM 4.24