Assay Detail
Binding
CHEMBL5739055
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Enzymatic Assay for MASP-2: The assay was run at room temperature in an assay buffer containing 20 mM Hepes, pH 7.4, 140 mM NaCl and 0.1% Tween 20. Assay parameters were adjusted such that the assay was linear with respect to time, enzyme and substrate concentrations. Under these optimized assays conditions, IC50 values were equivalent to Ki values, except in a few cases of tight binding inhibitors. Cases of tight binding or possible slow binding inhibitors were handled by the methods described in Copeland R. A. (2013) Evaluation of Enzyme Inhibitors in Drug Discovery. 2nd Ed., John Wiley and Sons, Inc., Chapters 5-7.
1458
Total Activities
478
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Target
Mannan-binding lectin serine protease 2 (CHEMBL4295646) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
MASP-2 inhibitors and methods of use
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 486 | 5.30 | 5.82 |
| kon | 486 | - | - |
| k_off | 486 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5898891 | — | — | 3 | 5.82 |
| CHEMBL5959785 | — | — | 3 | 5.82 |
| CHEMBL6060939 | — | — | 3 | 5.82 |
| CHEMBL5878347 | — | — | 3 | 5.82 |
| CHEMBL5801451 | — | — | 3 | 5.82 |
| CHEMBL5795459 | — | — | 3 | 5.82 |
| CHEMBL6038164 | — | — | 3 | 5.82 |
| CHEMBL5909043 | — | — | 3 | 5.82 |
| CHEMBL5827423 | — | — | 3 | 5.82 |
| CHEMBL5761304 | — | — | 3 | 5.82 |
| CHEMBL6010482 | — | — | 3 | 5.82 |
| CHEMBL5925225 | — | — | 3 | 5.82 |
| CHEMBL5890770 | — | — | 3 | 5.82 |
| CHEMBL5897239 | — | — | 6 | 5.82 |
| CHEMBL5866429 | — | — | 12 | 5.82 |
| CHEMBL5804052 | — | — | 3 | 5.82 |
| CHEMBL5941141 | — | — | 3 | 5.82 |
| CHEMBL5801221 | — | — | 3 | 5.82 |
| CHEMBL5864485 | — | — | 3 | 5.82 |
| CHEMBL5768713 | — | — | 3 | 5.82 |
| CHEMBL5963602 | — | — | 3 | 5.82 |
| CHEMBL6022164 | — | — | 9 | 5.82 |
| CHEMBL5902541 | — | — | 3 | 5.82 |
| CHEMBL6054572 | — | — | 3 | 5.82 |
| CHEMBL5870074 | — | — | 3 | 5.82 |
| CHEMBL5937862 | — | — | 3 | 5.82 |
| CHEMBL5751330 | — | — | 3 | 5.82 |
| CHEMBL5882970 | — | — | 3 | 5.82 |
| CHEMBL5888856 | — | — | 3 | 5.82 |
| CHEMBL5863724 | — | — | 3 | 5.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5855854 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5795459 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5785262 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5827391 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5801221 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5941141 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL6038164 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5877185 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5898891 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5863724 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5866429 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL6010482 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5927041 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5789492 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5827423 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL6054835 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5905312 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL6045678 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5792291 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5761304 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5990247 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5925225 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5890770 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5782844 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5945368 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5917654 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5751330 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL6022164 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5937862 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL6040016 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5870074 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL6054572 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5902541 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5853214 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5938937 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5963602 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5882970 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5905306 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5762749 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5768713 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5799168 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL6060939 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5922982 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5878347 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5955689 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5851869 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5864485 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5888856 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5801451 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL5926181 | — | Ki | = | 1500.0 | nM | 5.82 |