Assay Detail
Binding
CHEMBL4013288
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Inhibition of recombinant human complement factor D catalytic domain using Z-Lys-thiobenzylester as substrate preincubated for 1 hr followed by substrate addition by 2,4-dinitrobenzenesulfonyl-2,7-desmethyl-fluorecein probe based spectrofluorimetric assay
25
Total Activities
25
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 |
Publication
Discovery of Highly Potent and Selective Small-Molecule Reversible Factor D Inhibitors Demonstrating Alternative Complement Pathway Inhibition in Vivo.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 6.81 | 8.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3683753 | — | — | 1 | 8.30 |
| CHEMBL3683737 | — | — | 1 | 8.22 |
| CHEMBL3678882 | — | — | 1 | 8.00 |
| CHEMBL4094108 | — | — | 1 | 7.92 |
| CHEMBL4098439 | — | — | 1 | 7.85 |
| CHEMBL4081888 | — | — | 1 | 7.82 |
| CHEMBL4070311 | — | — | 1 | 7.64 |
| CHEMBL4061643 | — | — | 1 | 7.35 |
| CHEMBL4065529 | — | — | 1 | 7.30 |
| CHEMBL3668698 | — | — | 1 | 7.30 |
| CHEMBL3683729 | — | — | 1 | 7.18 |
| CHEMBL4095470 | — | — | 1 | 6.82 |
| CHEMBL4075355 | — | — | 1 | 6.82 |
| CHEMBL3668644 | — | — | 1 | 6.52 |
| CHEMBL4075037 | — | — | 1 | 6.50 |
| CHEMBL4076955 | — | — | 1 | 6.43 |
| CHEMBL3673764 | — | — | 1 | 6.35 |
| CHEMBL3908849 | — | — | 1 | 6.30 |
| CHEMBL3673825 | — | — | 1 | 6.30 |
| CHEMBL4068741 | — | — | 1 | 6.19 |
| CHEMBL3668730 | — | — | 1 | 6.16 |
| CHEMBL3668664 | — | — | 1 | 6.07 |
| CHEMBL3668755 | — | — | 1 | 5.85 |
| CHEMBL3668694 | — | — | 1 | 4.66 |
| CHEMBL3668647 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3683753 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3683737 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3678882 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4094108 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4098439 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4081888 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4070311 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4061643 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL4065529 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3668698 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3683729 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4095470 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4075355 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3668644 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4075037 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL4076955 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3673764 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL3908849 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL3673825 | — | IC50 | = | 500.0 | nM | 6.30 |
| CHEMBL4068741 | — | IC50 | = | 650.0 | nM | 6.19 |
| CHEMBL3668730 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL3668664 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL3668755 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3668694 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL3668647 | — | IC50 | = | 30000.0 | nM | 4.52 |