Assay Detail
Binding
CHEMBL5581972
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Inhibition of human Avi-tagged MUS81 (246 to 551 residues)/2x8His-tagged EME1 (246 to 570 residues) extracted from Escherichia coli BL21 Gold (DE3) using branched DNA as substrate preincubated for 15 mins followed by substrate addition and measured after 90 mins by FRET assay
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Fragment-Based Discovery of Novel MUS81 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.80 | 6.57 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5591377 | — | — | 1 | 6.57 |
| CHEMBL5592380 | — | — | 1 | 6.50 |
| CHEMBL5594391 | — | — | 1 | 6.33 |
| CHEMBL5594260 | — | — | 1 | 6.33 |
| CHEMBL5594006 | — | — | 1 | 6.18 |
| CHEMBL5595635 | — | — | 1 | 5.96 |
| CHEMBL5594490 | — | — | 1 | 5.92 |
| CHEMBL5595627 | — | — | 1 | 5.82 |
| CHEMBL4226761 | — | — | 1 | 5.70 |
| CHEMBL5592602 | — | — | 1 | 5.70 |
| CHEMBL188448 | — | — | 1 | 5.68 |
| CHEMBL5188107 | — | — | 1 | 5.62 |
| CHEMBL203976 | — | — | 1 | 5.55 |
| CHEMBL5595231 | — | — | 1 | 5.55 |
| CHEMBL5594819 | — | — | 1 | 5.42 |
| CHEMBL440562 | — | — | 1 | 5.41 |
| CHEMBL5593401 | — | — | 1 | 5.39 |
| CHEMBL5592973 | — | — | 1 | 5.35 |
| CHEMBL4225408 | — | — | 1 | 5.25 |
| CHEMBL3617204 | — | — | 1 | - |
| CHEMBL4174171 | — | — | 1 | - |
| CHEMBL5595842 | — | — | 1 | - |
| CHEMBL5584056 | — | — | 1 | - |
| CHEMBL5595830 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5591377 | — | IC50 | = | 270.0 | nM | 6.57 |
| CHEMBL5592380 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5594391 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5594260 | — | IC50 | = | 470.0 | nM | 6.33 |
| CHEMBL5594006 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL5595635 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5594490 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL5595627 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4226761 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL5592602 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL188448 | — | IC50 | = | 2100.0 | nM | 5.68 |
| CHEMBL5188107 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL203976 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5595231 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL5594819 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL440562 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL5593401 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL5592973 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL4225408 | — | IC50 | = | 5600.0 | nM | 5.25 |
| CHEMBL3617204 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4174171 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5595842 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5584056 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL5595830 | — | IC50 | > | 100000.0 | nM | - |