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Assay Detail

CHEMBL3889157

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

Binding
ELISA Assay: CVF-Bb complex prepared from purified cobra venom factor (1 μM), recombinant human complement factor B (expressed in drosophila cells and purified using standard methods) and human complement factor D (expressed in E. Coli, refolded and purified using standard methods). CVF-Bb complex at 3 nM concentration was incubated with test compound at various concentrations for 1 hour at room temperature in PBS pH 7.4 containing 10 mM MgCl2 and 0.05% (w/v) CHAPS. Human complement C3 substrate purified from plasma was added to a final concentration of 1 μM. After 1 hour incubation at room temperature, the enzyme reaction was stopped by addition of a cocktail of concentrated pan-protease inhibitors. The product of the reaction, C3a, was quantified by means of an enzyme-linked-immunosorbent assay.
131
Total Activities
130
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Plasma
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Complement pathway modulators and uses thereof
(2016)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 131 7.02 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4106993 1 9.00
CHEMBL4114217 1 9.00
CHEMBL4107243 1 8.52
CHEMBL4113469 1 8.52
CHEMBL4108959 1 8.40
CHEMBL4111681 1 8.40
CHEMBL4114574 1 8.30
CHEMBL4107774 1 8.22
CHEMBL3928150 1 8.22
CHEMBL4114991 1 8.22
CHEMBL4114221 1 8.22
CHEMBL4107659 1 8.22
CHEMBL4109971 1 8.22
CHEMBL4115570 1 8.22
CHEMBL4110511 1 8.15
CHEMBL3943926 1 8.15
CHEMBL4111301 1 8.10
CHEMBL3957678 1 8.05
CHEMBL4112178 1 8.00
CHEMBL3981421 1 8.00
CHEMBL4114531 1 8.00
CHEMBL4113781 1 8.00
CHEMBL3952833 1 7.96
CHEMBL3905588 1 7.96
CHEMBL4113062 1 7.96
CHEMBL4112415 1 7.92
CHEMBL4113623 1 7.89
CHEMBL4113997 1 7.85
CHEMBL3923445 1 7.82
CHEMBL4108762 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4114217 IC50 = 1.0 nM 9.00
CHEMBL4106993 IC50 = 1.0 nM 9.00
CHEMBL4107243 IC50 = 3.0 nM 8.52
CHEMBL4113469 IC50 = 3.0 nM 8.52
CHEMBL4111681 IC50 = 4.0 nM 8.40
CHEMBL4108959 IC50 = 4.0 nM 8.40
CHEMBL4114574 IC50 = 5.0 nM 8.30
CHEMBL4115570 IC50 = 6.0 nM 8.22
CHEMBL4109971 IC50 = 6.0 nM 8.22
CHEMBL4107774 IC50 = 6.0 nM 8.22
CHEMBL4107659 IC50 = 6.0 nM 8.22
CHEMBL4114221 IC50 = 6.0 nM 8.22
CHEMBL4114991 IC50 = 6.0 nM 8.22
CHEMBL3928150 IC50 = 6.0 nM 8.22
CHEMBL4110511 IC50 = 7.0 nM 8.15
CHEMBL3943926 IC50 = 7.0 nM 8.15
CHEMBL4111301 IC50 = 8.0 nM 8.10
CHEMBL3957678 IC50 = 9.0 nM 8.05
CHEMBL4113781 IC50 = 10.0 nM 8.00
CHEMBL4114531 IC50 = 10.0 nM 8.00
CHEMBL3981421 IC50 = 10.0 nM 8.00
CHEMBL4112178 IC50 = 10.0 nM 8.00
CHEMBL3952833 IC50 = 11.0 nM 7.96
CHEMBL4113062 IC50 = 11.0 nM 7.96
CHEMBL3905588 IC50 = 11.0 nM 7.96
CHEMBL4112415 IC50 = 12.0 nM 7.92
CHEMBL4113623 IC50 = 13.0 nM 7.89
CHEMBL4113997 IC50 = 14.0 nM 7.85
CHEMBL4108762 IC50 = 15.0 nM 7.82
CHEMBL3923445 IC50 = 15.0 nM 7.82
CHEMBL3975396 IC50 = 16.0 nM 7.80
CHEMBL3898919 IC50 = 17.0 nM 7.77
CHEMBL3929496 IC50 = 20.0 nM 7.70
CHEMBL4107253 IC50 = 20.0 nM 7.70
CHEMBL3890117 IC50 = 20.0 nM 7.70
CHEMBL3978495 IC50 = 20.0 nM 7.70
CHEMBL3953356 IC50 = 20.0 nM 7.70
CHEMBL3968840 IC50 = 20.0 nM 7.70
CHEMBL4107492 IC50 = 30.0 nM 7.52
CHEMBL3973437 IC50 = 30.0 nM 7.52
CHEMBL4109043 IC50 = 30.0 nM 7.52
CHEMBL4110121 IC50 = 30.0 nM 7.52
CHEMBL4109775 IC50 = 40.0 nM 7.40
CHEMBL3957065 IC50 = 40.0 nM 7.40
CHEMBL4111694 IC50 = 40.0 nM 7.40
CHEMBL4115080 IC50 = 40.0 nM 7.40
CHEMBL4115621 IC50 = 40.0 nM 7.40
CHEMBL4110860 IC50 = 40.0 nM 7.40
CHEMBL4113394 IC50 = 50.0 nM 7.30
CHEMBL4108466 IC50 = 50.0 nM 7.30