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Assay Detail

CHEMBL767385

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

Functional
Tested for the ability to inhibit endothelin-1 (ET-1) induced contraction in rabbit femoral arterial rings.
4
Total Activities
4
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

-Carbamate butenolide analogues as potent ETA selective endothelin receptor antagonists and prodrugs
Patt WC, Reisdorph BR, Repine JT, Doherty AM, Haleen SJ, Walker DM, Welch KM, Flynn MA, Hallak H, Reyner EL, Stewart BH
Bioorg Med Chem Lett (1997) 7 : 297 -302
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 4 7.33 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL450337 1 7.70
CHEMBL8981 PD-156707 1 7.50
CHEMBL319452 1 7.30
CHEMBL322920 1 6.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL450337 Kd = 19.95 nM 7.70
CHEMBL8981 PD-156707 Kd = 31.62 nM 7.50
CHEMBL319452 Kd = 50.12 nM 7.30
CHEMBL322920 Kd = 158.49 nM 6.80