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Assay Detail

CHEMBL771616

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

Functional
Inhibition of ET-1 stimulated arachidonic acid release in rabbit renal artery vascular smooth muscle cells
14
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Oryctolagus cuniculus
Confidence 1 — Organism
Curated By Intermediate

Target

Oryctolagus cuniculus (CHEMBL374)
Type ORGANISM
Organism Oryctolagus cuniculus

Publication

Structure-activity relationships of C-terminal endothelin hexapeptide antagonists.
Doherty AM, Cody WL, DePue PL, He JX, Waite LA, Leonard DM, Leitz NL, Dudley DT, Rapundalo ST, Hingorani GP.
J Med Chem (1993) 36 : 2585 -2594
PubMed 8410970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.85 6.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL406279 1 6.48
CHEMBL85341 1 6.37
CHEMBL313056 1 6.22
CHEMBL315047 1 6.20
CHEMBL87243 1 5.82
CHEMBL2370070 1 5.70
CHEMBL313984 2 5.66
CHEMBL86814 1 5.51
CHEMBL289687 1 5.50
CHEMBL327350 1 5.35
CHEMBL431874 1 -
CHEMBL86737 1 -
CHEMBL315780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL406279 IC50 = 330.0 nM 6.48
CHEMBL85341 IC50 = 430.0 nM 6.37
CHEMBL313056 IC50 = 600.0 nM 6.22
CHEMBL315047 IC50 = 630.0 nM 6.20
CHEMBL87243 IC50 = 1500.0 nM 5.82
CHEMBL2370070 IC50 = 2000.0 nM 5.70
CHEMBL313984 IC50 = 2200.0 nM 5.66
CHEMBL313984 IC50 = 2600.0 nM 5.58
CHEMBL86814 IC50 = 3100.0 nM 5.51
CHEMBL289687 IC50 = 3200.0 nM 5.50
CHEMBL327350 IC50 = 4500.0 nM 5.35
CHEMBL431874 IC50 > 10000.0 nM -
CHEMBL86737 IC50 > 10000.0 nM -
CHEMBL315780 IC50 > 10000.0 nM -