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Assay Detail

CHEMBL4013311

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

Binding
Inhibition of complement factor D in human whole blood assessed as decrease in zymosan-induced AP activation mediated soluble MAC complex formation preincubated for 15 mins followed by zymosan addition measured after 40 mins by ELISA
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Complement factor D (CHEMBL2176771)
Type SINGLE PROTEIN
Organism Homo sapiens

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
IC50 14 6.93 8.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3683737 1 8.05
CHEMBL3683753 1 7.96
CHEMBL4098439 1 7.66
CHEMBL4081888 1 7.46
CHEMBL3678882 1 6.82
CHEMBL4094108 1 6.60
CHEMBL4070311 1 6.23
CHEMBL4065529 1 5.90
CHEMBL3683729 1 5.73
CHEMBL4075355 1 -
CHEMBL4075037 1 -
CHEMBL4095470 1 -
CHEMBL4061643 1 -
CHEMBL4076955 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3683737 IC50 = 9.0 nM 8.05
CHEMBL3683753 IC50 = 11.0 nM 7.96
CHEMBL4098439 IC50 = 22.0 nM 7.66
CHEMBL4081888 IC50 = 35.0 nM 7.46
CHEMBL3678882 IC50 = 150.0 nM 6.82
CHEMBL4094108 IC50 = 250.0 nM 6.60
CHEMBL4070311 IC50 = 587.0 nM 6.23
CHEMBL4065529 IC50 = 1250.0 nM 5.90
CHEMBL3683729 IC50 = 1860.0 nM 5.73
CHEMBL4075355 IC50 - -
CHEMBL4075037 IC50 - -
CHEMBL4095470 IC50 - -
CHEMBL4061643 IC50 - -
CHEMBL4076955 IC50 - -