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Assay Detail

CHEMBL4013329

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

Functional
In vivo inhibition of complement factor D in cynomolgus monkey assessed as decrease in zymosan-induced AP activation by measuring soluble MAC complex deposition in serum administered as single dose via oral gavage measured at 4 to 24 hrs post dose
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Macaca fascicularis
Confidence 1 — Organism
Curated By Autocuration

Target

Cynomolgus monkey (CHEMBL613847)
Type ORGANISM
Organism Macaca fascicularis

Publication

Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Lorthiois E, Anderson K, Vulpetti A, Rogel O, Cumin F, Ostermann N, Steinbacher S, Mac Sweeney A, Delgado O, Liao SM, Randl S, Rüdisser S, Dussauge S, Fettis K, Kieffer L, de Erkenez A, Yang L, Hartwieg C, Argikar UA, La Bonte LR, Newton R, Kansara V, Flohr S, Hommel U, Jaffee B, Maibaum J.
J Med Chem (2017) 60 : 5717 -5735
PubMed 28621538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.42 7.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3683753 1 7.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3683753 EC50 = 38.0 nM 7.42