Assay Detail
Binding
CHEMBL3705870
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Fluorometric Plate Assay: To determine the efficacy of various synthesized PAI-1 inhibitor compounds, a fluorometric plate assay was carried out to measure the half maximal inhibitory concentration (IC50) of these compounds on recombinant active human PAI-1 in vitro. An IC50 is a measure of the effectiveness of a compound in inhibiting biological or biochemical function. Stated another way, IC50 represents the concentration of a drug that is required for 50% inhibition in vitro. The IC50 of various compounds was measured using a fluorometric plate assay as set out below, and the results are shown in Table 3.Recombinant active human PAI-1 (Molecular Innovations) (final 1 nM) was incubated for 15 min at 23 C. with increasing concentrations of each compound in 100 mM NaCl, 40 mM HEPES, 0.005% Tween-20, 10% DMSO, pH 7.8. Alternately, the assay has been carried out using low concentrations of DMSO (about 0.1% DMSO or less) in the buffer. In various aspects, the invention does not require a solvent, like DMSO.
37
Total Activities
37
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
Plasminogen activator inhibitor-1 inhibitors and methods of use thereof to modulate lipid metabolism
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 6.17 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL425946 | — | — | 1 | 8.00 |
| CHEMBL3669202 | — | — | 1 | 8.00 |
| CHEMBL1224764 | — | — | 1 | 8.00 |
| CHEMBL207014 | — | — | 1 | 8.00 |
| CHEMBL377052 | — | — | 1 | 8.00 |
| CHEMBL3669191 | — | — | 1 | 7.30 |
| CHEMBL3669189 | — | — | 1 | 7.30 |
| CHEMBL3669200 | — | — | 1 | 7.16 |
| CHEMBL3669193 | — | — | 1 | 7.05 |
| CHEMBL2087115 | — | — | 1 | 6.55 |
| CHEMBL2087114 | — | — | 1 | 6.43 |
| CHEMBL2087116 | — | — | 1 | 5.93 |
| CHEMBL3669196 | — | — | 1 | 5.77 |
| CHEMBL1090448 | — | — | 1 | 5.53 |
| CHEMBL3669181 | — | — | 1 | 5.11 |
| CHEMBL599742 | — | — | 1 | 4.99 |
| CHEMBL3669187 | — | — | 1 | 4.56 |
| CHEMBL3669183 | — | — | 1 | 4.54 |
| CHEMBL3669194 | — | — | 1 | 4.49 |
| CHEMBL3669199 | — | — | 1 | 4.32 |
| CHEMBL3669197 | — | — | 1 | 4.32 |
| CHEMBL3669178 | — | — | 1 | 4.31 |
| CHEMBL3669185 | — | — | 1 | - |
| CHEMBL292067 | — | — | 1 | - |
| CHEMBL3669186 | — | — | 1 | - |
| CHEMBL606451 | — | — | 1 | - |
| CHEMBL3669188 | — | — | 1 | - |
| CHEMBL3669182 | — | — | 1 | - |
| CHEMBL3669180 | — | — | 1 | - |
| CHEMBL3669192 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL425946 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL377052 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL207014 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1224764 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3669202 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3669191 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3669189 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3669200 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3669193 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL2087115 | — | IC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2087114 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL2087116 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL3669196 | — | IC50 | = | 1710.0 | nM | 5.77 |
| CHEMBL1090448 | — | IC50 | = | 2960.0 | nM | 5.53 |
| CHEMBL3669181 | — | IC50 | = | 7850.0 | nM | 5.11 |
| CHEMBL599742 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL3669187 | — | IC50 | = | 27500.0 | nM | 4.56 |
| CHEMBL3669183 | — | IC50 | = | 28700.0 | nM | 4.54 |
| CHEMBL3669194 | — | IC50 | = | 32700.0 | nM | 4.49 |
| CHEMBL3669197 | — | IC50 | = | 47900.0 | nM | 4.32 |
| CHEMBL3669199 | — | IC50 | = | 48300.0 | nM | 4.32 |
| CHEMBL3669178 | — | IC50 | = | 49300.0 | nM | 4.31 |
| CHEMBL3669195 | — | IC50 | = | 104000.0 | nM | - |
| CHEMBL3669198 | — | IC50 | = | 146000.0 | nM | - |
| CHEMBL3669190 | — | IC50 | = | 195000.0 | nM | - |
| CHEMBL3669179 | — | IC50 | = | 196000.0 | nM | - |
| CHEMBL3669184 | — | IC50 | = | 236000.0 | nM | - |
| CHEMBL3669201 | — | IC50 | = | 246000.0 | nM | - |
| CHEMBL302625 | — | IC50 | = | 269000.0 | nM | - |
| CHEMBL3669192 | — | IC50 | = | 332000.0 | nM | - |
| CHEMBL3669180 | — | IC50 | = | 338000.0 | nM | - |
| CHEMBL3669182 | — | IC50 | = | 386000.0 | nM | - |
| CHEMBL3669188 | — | IC50 | = | 423000.0 | nM | - |
| CHEMBL606451 | — | IC50 | = | 450000.0 | nM | - |
| CHEMBL3669186 | — | IC50 | = | 562000.0 | nM | - |
| CHEMBL292067 | — | IC50 | = | 900000.0 | nM | - |
| CHEMBL3669185 | — | IC50 | = | 2204000.0 | nM | - |