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

CHEMBL678556

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

Binding
Binding affinity towards human ETA receptor expressed in CHO-K1 cells in the presence of 0.05 nM [125I]-labeled endothelin 1
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO-K1
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Discovery of 4'-[(imidazol-1-yl)methyl]biphenyl-2-sulfonamides as dual endothelin/angiotensin II receptor antagonists.
Tellew JE, Baska RA, Beyer SM, Carlson KE, Cornelius LA, Fadnis L, Gu Z, Kunst BL, Kowala MC, Monshizadegan H, Murugesan N, Ryan CS, Valentine MT, Yang Y, Macor JE.
Bioorg Med Chem Lett (2003) 13 : 1093 -1096
PubMed 12643919 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 25 7.69 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12703 1 9.00
CHEMBL11706 BMS-248360 1 8.70
CHEMBL11840 1 8.40
CHEMBL12106 1 8.30
CHEMBL266628 1 8.30
CHEMBL275545 1 8.15
CHEMBL12233 1 8.15
CHEMBL12588 1 8.10
CHEMBL12013 1 7.89
CHEMBL11528 1 7.85
CHEMBL12144 1 7.82
CHEMBL275523 1 7.80
CHEMBL268706 1 7.77
CHEMBL429037 1 7.70
CHEMBL12175 1 7.70
CHEMBL12590 1 7.70
CHEMBL12557 1 7.66
CHEMBL12333 1 7.40
CHEMBL274154 1 7.40
CHEMBL12592 1 7.26
CHEMBL12102 1 7.26
CHEMBL12779 1 6.98
CHEMBL417429 1 6.38
CHEMBL12172 1 6.34
CHEMBL12348 1 6.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12703 Ki = 1.0 nM 9.00
CHEMBL11706 BMS-248360 Ki = 2.0 nM 8.70
CHEMBL11840 Ki = 4.0 nM 8.40
CHEMBL12106 Ki = 5.0 nM 8.30
CHEMBL266628 Ki = 5.0 nM 8.30
CHEMBL275545 Ki = 7.0 nM 8.15
CHEMBL12233 Ki = 7.0 nM 8.15
CHEMBL12588 Ki = 8.0 nM 8.10
CHEMBL12013 Ki = 13.0 nM 7.89
CHEMBL11528 Ki = 14.0 nM 7.85
CHEMBL12144 Ki = 15.0 nM 7.82
CHEMBL275523 Ki = 16.0 nM 7.80
CHEMBL268706 Ki = 17.0 nM 7.77
CHEMBL429037 Ki = 20.0 nM 7.70
CHEMBL12175 Ki = 20.0 nM 7.70
CHEMBL12590 Ki = 20.0 nM 7.70
CHEMBL12557 Ki = 22.0 nM 7.66
CHEMBL12333 Ki = 40.0 nM 7.40
CHEMBL274154 Ki = 40.0 nM 7.40
CHEMBL12592 Ki = 55.0 nM 7.26
CHEMBL12102 Ki = 55.0 nM 7.26
CHEMBL12779 Ki = 105.0 nM 6.98
CHEMBL417429 Ki = 415.0 nM 6.38
CHEMBL12172 Ki = 460.0 nM 6.34
CHEMBL12348 Ki = 700.0 nM 6.16