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Assay Detail

CHEMBL658321

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

Functional
Antagonistic activity was measured by ET receptor mediated hydrolysis of inositol phosphates
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cricetulus griseus
Cell Type CHO
Confidence 1 — Organism
Curated By Intermediate

Target

CHO (CHEMBL613853)
Type CELL-LINE
Organism Cricetulus griseus

Publication

Pyrrolidine-3-carboxylic acids as endothelin antagonists. 4. Side chain conformational restriction leads to ET(B) selectivity.
von Geldern TW, Tasker AS, Sorensen BK, Winn M, Szczepankiewicz BG, Dixon DB, Chiou WJ, Wang L, Wessale JL, Adler A, Marsh KC, Nguyen B, Opgenorth TJ.
J Med Chem (1999) 42 : 3668 -3678
PubMed 10479298 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.65 9.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL332794 A-192621 1 9.19
CHEMBL435385 1 8.10

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL332794 A-192621 IC50 = 0.65 nM 9.19
CHEMBL435385 IC50 = 7.9 nM 8.10