Assay Detail
Binding
CHEMBL5731431
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Human Complement Factor B TR-FRET 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. IC50 values were calculated from percentage of inhibition of CVF-Bb activity as a function of test compound concentration.
330
Total Activities
89
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Piperidinyl-indole derivatives complement factor B inhibitors and uses thereof
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 110 | 6.67 | 8.05 |
| kon | 110 | - | - |
| k_off | 110 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6043471 | — | — | 3 | 8.05 |
| CHEMBL5922859 | — | — | 3 | 8.05 |
| CHEMBL5981804 | — | — | 3 | 7.96 |
| CHEMBL5992968 | — | — | 3 | 7.89 |
| CHEMBL6024618 | — | — | 6 | 7.89 |
| CHEMBL5749220 | — | — | 3 | 7.85 |
| CHEMBL6009765 | — | — | 3 | 7.82 |
| CHEMBL5865752 | — | — | 3 | 7.82 |
| CHEMBL5759287 | — | — | 3 | 7.72 |
| CHEMBL5936315 | — | — | 3 | 7.72 |
| CHEMBL4632794 | — | — | 3 | 7.72 |
| CHEMBL5885876 | — | — | 3 | 7.66 |
| CHEMBL5982712 | — | — | 3 | 7.66 |
| CHEMBL6000572 | — | — | 3 | 7.57 |
| CHEMBL5781952 | — | — | 6 | 7.52 |
| CHEMBL6026552 | — | — | 3 | 7.46 |
| CHEMBL5746835 | — | — | 3 | 7.43 |
| CHEMBL5980756 | — | — | 3 | 7.42 |
| CHEMBL6011435 | — | — | 3 | 7.35 |
| CHEMBL4644994 | — | — | 6 | 7.33 |
| CHEMBL5818564 | — | — | 3 | 7.26 |
| CHEMBL6031306 | — | — | 3 | 7.20 |
| CHEMBL5823445 | — | — | 3 | 7.06 |
| CHEMBL5904269 | — | — | 3 | 6.78 |
| CHEMBL5750743 | — | — | 6 | 6.64 |
| CHEMBL5919413 | — | — | 3 | 6.13 |
| CHEMBL4594448 | IPTACOPAN | 4.0 | 6 | 5.96 |
| CHEMBL5859255 | — | — | 3 | 5.77 |
| CHEMBL5958669 | — | — | 3 | 5.75 |
| CHEMBL5870859 | — | — | 3 | 5.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5922859 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL6043471 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5981804 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL6024618 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5992968 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5749220 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL6009765 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5865752 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5759287 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4632794 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5936315 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5982712 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5885876 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL6024618 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL6000572 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5781952 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL6026552 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5746835 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5980756 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL6011435 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4644994 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL5818564 | — | IC50 | = | 55.0 | nM | 7.26 |
| CHEMBL6031306 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL5823445 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL5781952 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5904269 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL5750743 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL5919413 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4594448 | IPTACOPAN | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5859255 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL5870859 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5958669 | — | IC50 | = | 1800.0 | nM | 5.75 |
| CHEMBL5879188 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL5902722 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL6029491 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL5900106 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL5900320 | — | IC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL5830458 | — | IC50 | = | 29000.0 | nM | 4.54 |
| CHEMBL5769081 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL4635047 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL5818097 | — | IC50 | = | 36000.0 | nM | 4.44 |
| CHEMBL4633437 | — | IC50 | = | 67000.0 | nM | 4.17 |
| CHEMBL5865752 | — | k_off | = | - | s-1 | - |
| CHEMBL5982712 | — | k_off | = | - | s-1 | - |
| CHEMBL4644994 | — | kon | = | - | — | - |
| CHEMBL5865752 | — | kon | = | - | — | - |
| CHEMBL5900106 | — | kon | = | - | — | - |
| CHEMBL4644994 | — | IC50 | = | 15000.0 | nM | - |
| CHEMBL4644994 | — | kon | = | - | — | - |
| CHEMBL5982712 | — | kon | = | - | — | - |