Assay Detail
Binding
CHEMBL3267156
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Inhibition of hexa-His-tagged PAI-1 N152H/K156T/Q321L/M356I mutant (unknown origin) expressed in Escherichia coli BL21(DE3) after 10 mins by uPA-based assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Design, synthesis, and SAR of embelin analogues as the inhibitors of PAI-1 (plasminogen activator inhibitor-1).
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 19 | 5.77 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3263326 | — | — | 1 | 6.75 |
| CHEMBL3263324 | — | — | 1 | 6.42 |
| CHEMBL3263334 | — | — | 1 | 6.29 |
| CHEMBL3263333 | — | — | 1 | 6.24 |
| CHEMBL3263327 | — | — | 1 | 6.20 |
| CHEMBL3263325 | — | — | 1 | 6.12 |
| CHEMBL3263329 | — | — | 1 | 6.11 |
| CHEMBL3263335 | — | — | 1 | 6.05 |
| CHEMBL3263332 | — | — | 1 | 6.04 |
| CHEMBL3263328 | — | — | 1 | 6.02 |
| CHEMBL2296057 | — | — | 1 | 5.75 |
| CHEMBL221598 | — | — | 1 | 5.73 |
| CHEMBL2296056 | — | — | 1 | 5.41 |
| CHEMBL3263323 | — | — | 1 | 5.38 |
| CHEMBL2296055 | — | — | 1 | 5.34 |
| CHEMBL221137 | EMBELIN | — | 1 | 5.31 |
| CHEMBL3263330 | — | — | 1 | 5.25 |
| CHEMBL3263331 | — | — | 1 | 5.15 |
| CHEMBL471270 | 5-O-METHYLEMBELIN | — | 1 | 4.04 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3263326 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3263324 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL3263334 | — | IC50 | = | 510.0 | nM | 6.29 |
| CHEMBL3263333 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL3263327 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3263325 | — | IC50 | = | 750.0 | nM | 6.12 |
| CHEMBL3263329 | — | IC50 | = | 770.0 | nM | 6.11 |
| CHEMBL3263335 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL3263332 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL3263328 | — | IC50 | = | 950.0 | nM | 6.02 |
| CHEMBL2296057 | — | IC50 | = | 1780.0 | nM | 5.75 |
| CHEMBL221598 | — | IC50 | = | 1870.0 | nM | 5.73 |
| CHEMBL2296056 | — | IC50 | = | 3870.0 | nM | 5.41 |
| CHEMBL3263323 | — | IC50 | = | 4180.0 | nM | 5.38 |
| CHEMBL2296055 | — | IC50 | = | 4560.0 | nM | 5.34 |
| CHEMBL221137 | EMBELIN | IC50 | = | 4940.0 | nM | 5.31 |
| CHEMBL3263330 | — | IC50 | = | 5680.0 | nM | 5.25 |
| CHEMBL3263331 | — | IC50 | = | 7110.0 | nM | 5.15 |
| CHEMBL471270 | 5-O-METHYLEMBELIN | IC50 | = | 90190.0 | nM | 4.04 |