Assay Detail
Binding
CHEMBL5730586
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 uM), 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 uM. 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
86
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 | 9.20 | 11.00 |
| kon | 110 | - | - |
| k_off | 110 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6043471 | — | — | 3 | 11.00 |
| CHEMBL4594448 | IPTACOPAN | 4.0 | 3 | 11.00 |
| CHEMBL6024618 | — | — | 6 | 11.00 |
| CHEMBL5778053 | — | — | 6 | 11.00 |
| CHEMBL5932429 | — | — | 6 | 11.00 |
| CHEMBL5804420 | — | — | 6 | 11.00 |
| CHEMBL5981804 | — | — | 3 | 11.00 |
| CHEMBL5867904 | — | — | 6 | 10.70 |
| CHEMBL4632794 | — | — | 3 | 10.70 |
| CHEMBL6009765 | — | — | 3 | 10.70 |
| CHEMBL5786380 | — | — | 6 | 10.70 |
| CHEMBL5885876 | — | — | 3 | 10.70 |
| CHEMBL5742644 | — | — | 3 | 10.70 |
| CHEMBL5759287 | — | — | 3 | 10.70 |
| CHEMBL5877871 | — | — | 6 | 10.70 |
| CHEMBL5746213 | — | — | 3 | 10.52 |
| CHEMBL6000572 | — | — | 3 | 10.52 |
| CHEMBL6014350 | — | — | 3 | 10.52 |
| CHEMBL5839570 | — | — | 3 | 10.40 |
| CHEMBL6026552 | — | — | 3 | 10.40 |
| CHEMBL5746835 | — | — | 3 | 10.40 |
| CHEMBL6011435 | — | — | 3 | 10.30 |
| CHEMBL4644994 | — | — | 6 | 10.30 |
| CHEMBL5818564 | — | — | 3 | 10.22 |
| CHEMBL6031306 | — | — | 3 | 10.22 |
| CHEMBL6003272 | — | — | 3 | 10.15 |
| CHEMBL5903309 | — | — | 3 | 10.05 |
| CHEMBL5909868 | — | — | 3 | 10.00 |
| CHEMBL5994439 | — | — | 3 | 10.00 |
| CHEMBL5909766 | — | — | 3 | 9.92 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL6043471 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL5778053 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL5981804 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL6024618 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL5932429 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL5804420 | — | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL4594448 | IPTACOPAN | IC50 | = | 0.01 | nM | 11.00 |
| CHEMBL5885876 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5742644 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5759287 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5877871 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL6009765 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5867904 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL4632794 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL5786380 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL6024618 | — | IC50 | = | 0.02 | nM | 10.70 |
| CHEMBL6000572 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL6014350 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL5746213 | — | IC50 | = | 0.03 | nM | 10.52 |
| CHEMBL6026552 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL5746835 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL5839570 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL6011435 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL4644994 | — | IC50 | = | 0.05 | nM | 10.30 |
| CHEMBL5818564 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL6031306 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL6003272 | — | IC50 | = | 0.07 | nM | 10.15 |
| CHEMBL5903309 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL5909868 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5994439 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL5909766 | — | IC50 | = | 0.12 | nM | 9.92 |
| CHEMBL6064397 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL6010962 | — | IC50 | = | 0.14 | nM | 9.85 |
| CHEMBL5831878 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL5833948 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL6014967 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL5864470 | — | IC50 | = | 0.23 | nM | 9.64 |
| CHEMBL5968743 | — | IC50 | = | 0.24 | nM | 9.62 |
| CHEMBL5862159 | — | IC50 | = | 0.28 | nM | 9.55 |
| CHEMBL5847273 | — | IC50 | = | 0.29 | nM | 9.54 |
| CHEMBL5869243 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL5823358 | — | IC50 | = | 0.34 | nM | 9.47 |
| CHEMBL6016984 | — | IC50 | = | 0.45 | nM | 9.35 |
| CHEMBL5929526 | — | IC50 | = | 0.65 | nM | 9.19 |
| CHEMBL5839517 | — | IC50 | = | 0.64 | nM | 9.19 |
| CHEMBL5890193 | — | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL4647418 | — | IC50 | = | 0.71 | nM | 9.15 |
| CHEMBL4633437 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL5778053 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL6060716 | — | IC50 | = | 0.84 | nM | 9.08 |