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

CHEMBL679716

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

Binding
The compound was tested for binding inhibitory activity against Endothelin A receptor from porcine aortic smooth muscle membranes.
ChEMBL ↗
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Endothelin-1 receptor (CHEMBL4130) ↗
Type SINGLE PROTEIN
Organism Sus scrofa

Publication

Structure-activity relationships of cyclic pentapeptide endothelin A receptor antagonists.
Fukami T, Nagase T, Fujita K, Hayama T, Niiyama K, Mase T, Nakajima S, Fukuroda T, Saeki T, Nishikibe M.
J Med Chem (1995) 38 : 4309 -4324
PubMed 7473559 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 6.70 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL414165 — — 1 8.52
CHEMBL133257 — — 1 8.40
CHEMBL137659 — — 1 7.92
CHEMBL2370830 — — 1 7.89
CHEMBL336563 — — 1 7.82
CHEMBL2370825 — — 1 7.75
CHEMBL343516 — — 1 7.75
CHEMBL341994 — — 1 7.72
CHEMBL343062 — — 1 7.70
CHEMBL342615 — — 1 7.68
CHEMBL336033 — — 1 7.66
CHEMBL343582 — — 1 7.62
CHEMBL137716 — — 1 7.54
CHEMBL132542 — — 1 7.50
CHEMBL422285 — — 1 7.48
CHEMBL263537 — — 1 7.47
CHEMBL138120 — — 1 7.46
CHEMBL342440 — — 1 7.33
CHEMBL433853 — — 1 7.31
CHEMBL407771 — — 1 7.21
CHEMBL1791008 — — 1 7.19
CHEMBL335143 — — 1 6.96
CHEMBL335416 — — 1 6.92
CHEMBL337567 — — 1 6.89
CHEMBL407639 — — 1 6.85
CHEMBL342617 — — 1 6.85
CHEMBL137671 — — 1 6.82
CHEMBL335128 — — 1 6.82
CHEMBL337031 — — 1 6.80
CHEMBL342840 — — 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL414165 — IC50 = 3.0 nM 8.52
CHEMBL133257 — IC50 = 4.0 nM 8.40
CHEMBL137659 — IC50 = 12.0 nM 7.92
CHEMBL2370830 — IC50 = 13.0 nM 7.89
CHEMBL336563 — IC50 = 15.0 nM 7.82
CHEMBL2370825 — IC50 = 18.0 nM 7.75
CHEMBL343516 — IC50 = 18.0 nM 7.75
CHEMBL341994 — IC50 = 19.0 nM 7.72
CHEMBL343062 — IC50 = 20.0 nM 7.70
CHEMBL342615 — IC50 = 21.0 nM 7.68
CHEMBL336033 — IC50 = 22.0 nM 7.66
CHEMBL343582 — IC50 = 24.0 nM 7.62
CHEMBL137716 — IC50 = 29.0 nM 7.54
CHEMBL132542 — IC50 = 32.0 nM 7.50
CHEMBL422285 — IC50 = 33.0 nM 7.48
CHEMBL263537 — IC50 = 34.0 nM 7.47
CHEMBL138120 — IC50 = 35.0 nM 7.46
CHEMBL342440 — IC50 = 47.0 nM 7.33
CHEMBL433853 — IC50 = 49.0 nM 7.31
CHEMBL407771 — IC50 = 62.0 nM 7.21
CHEMBL1791008 — IC50 = 64.0 nM 7.19
CHEMBL335143 — IC50 = 110.0 nM 6.96
CHEMBL335416 — IC50 = 120.0 nM 6.92
CHEMBL337567 — IC50 = 130.0 nM 6.89
CHEMBL342617 — IC50 = 140.0 nM 6.85
CHEMBL407639 — IC50 = 140.0 nM 6.85
CHEMBL137671 — IC50 = 150.0 nM 6.82
CHEMBL335128 — IC50 = 150.0 nM 6.82
CHEMBL337031 — IC50 = 160.0 nM 6.80
CHEMBL342840 — IC50 = 160.0 nM 6.80
CHEMBL136634 — IC50 = 160.0 nM 6.80
CHEMBL137361 — IC50 = 180.0 nM 6.75
CHEMBL135906 — IC50 = 190.0 nM 6.72
CHEMBL134562 — IC50 = 200.0 nM 6.70
CHEMBL136210 — IC50 = 210.0 nM 6.68
CHEMBL1791007 — IC50 = 230.0 nM 6.64
CHEMBL335780 — IC50 = 240.0 nM 6.62
CHEMBL343768 — IC50 = 240.0 nM 6.62
CHEMBL341443 — IC50 = 250.0 nM 6.60
CHEMBL137754 — IC50 = 260.0 nM 6.58
CHEMBL1791006 — IC50 = 270.0 nM 6.57
CHEMBL404763 — IC50 = 330.0 nM 6.48
CHEMBL342913 — IC50 = 390.0 nM 6.41
CHEMBL337897 — IC50 = 410.0 nM 6.39
CHEMBL135907 — IC50 = 440.0 nM 6.36
CHEMBL136583 — IC50 = 530.0 nM 6.28
CHEMBL343379 — IC50 = 1400.0 nM 5.85
CHEMBL342215 — IC50 = 1500.0 nM 5.82
CHEMBL422464 — IC50 = 1700.0 nM 5.77
CHEMBL344473 — IC50 = 2800.0 nM 5.55