Assay Detail
Binding
CHEMBL5385450
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human recombinant N-terminal IgG tagged and C-terminal His tagged C1S (358 to 688 aa residues) expressed in HEK293 cells using Z-Lys-SBzl peptide as substrate pretreated with compound followed by substrate addition incubated for 60 mins
20
Total Activities
20
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of a Novel Series of Potent, Selective, Orally Available, and Brain-Penetrable C1s Inhibitors for Modulation of the Complement Pathway.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 6.05 | 8.15 |
| INH | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5435382 | — | — | 1 | 8.15 |
| CHEMBL5417464 | — | — | 1 | 7.44 |
| CHEMBL5418327 | — | — | 1 | 6.77 |
| CHEMBL5407328 | — | — | 1 | 6.43 |
| CHEMBL5410431 | — | — | 1 | 6.41 |
| CHEMBL5418278 | — | — | 1 | 6.25 |
| CHEMBL5437582 | — | — | 1 | 6.24 |
| CHEMBL5432292 | — | — | 1 | 6.09 |
| CHEMBL5398476 | — | — | 1 | 5.92 |
| CHEMBL5439103 | — | — | 1 | 5.85 |
| CHEMBL5437882 | — | — | 1 | 5.85 |
| CHEMBL5411534 | — | — | 1 | 5.60 |
| CHEMBL5398549 | — | — | 1 | 5.38 |
| CHEMBL5411177 | — | — | 1 | 5.29 |
| CHEMBL5412594 | — | — | 1 | 5.17 |
| CHEMBL5410965 | — | — | 1 | 4.02 |
| CHEMBL5424714 | — | — | 1 | - |
| CHEMBL5431053 | — | — | 1 | - |
| CHEMBL5413734 | — | — | 1 | - |
| CHEMBL5418024 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5435382 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5417464 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5418327 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5407328 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL5410431 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL5418278 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL5437582 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL5432292 | — | IC50 | = | 820.0 | nM | 6.09 |
| CHEMBL5398476 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5439103 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5437882 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL5411534 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL5398549 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL5411177 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL5412594 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL5410965 | — | IC50 | = | 96000.0 | nM | 4.02 |
| CHEMBL5424714 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL5431053 | — | INH | = | 4.5 | uM | - |
| CHEMBL5413734 | — | IC50 | > | 300000.0 | nM | - |
| CHEMBL5418024 | — | IC50 | > | 300000.0 | nM | - |