Assay Detail
Binding
CHEMBL5733563
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Assay: MMP-14:The basis for the assay is the cleavage of the substrate 390 MMP FRET Substrate I (Anaspec Cat # AS-27076) by human MMP14 (Biomol, Cat #SE-259).For the dose response (10 point), 4 μL of a dilution series of compound 2 mM highest concentration, 1/5 dilution in DMSO further diluted 1 in 10 in water, corresponding to a final highest concentration of 20 μM), is transferred to 384 well Fluotrac 200 plate (Greiner, cat #781076) and incubated at room temperature for 30 min with a 26 μL buffer solution (50 mM MOPS pH7, 5 mM CaCl2, 1 μM ZnCl2, 0.1% Brij-35) containing MMP14 (0.05 ng/μL) (it will be appreciated by the skilled person that the potency read out is independent of the enzyme concentration).The reaction is initiated by adding to the assay plate 390 MMP FRET Substrate I (10 μL, 2.5 μM) in the same buffer.Finally, the fluorescence is read on the Envision (Perkin Elmer) after an incubation of 60 min at room temperature (Excitation 485 nm, Emission 530).
384
Total Activities
117
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
5-[(piperazin-1-yl)-3-oxo-propyl]-imidazolidine-2,4-dione derivatives as ADAMTS inhibitors for the treatment of osteoarthritis
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 128 | 6.09 | 8.15 |
| kon | 128 | - | - |
| k_off | 128 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL6024784 | — | — | 3 | 8.15 |
| CHEMBL5859458 | — | — | 3 | 8.15 |
| CHEMBL5831615 | — | — | 3 | 7.58 |
| CHEMBL5961990 | — | — | 3 | 7.58 |
| CHEMBL5802716 | — | — | 6 | 7.51 |
| CHEMBL5962730 | — | — | 3 | 7.28 |
| CHEMBL5970747 | — | — | 6 | 6.68 |
| CHEMBL4874034 | — | — | 3 | 6.42 |
| CHEMBL5954577 | — | — | 3 | 6.42 |
| CHEMBL5913296 | — | — | 3 | 6.42 |
| CHEMBL5899647 | — | — | 3 | 6.42 |
| CHEMBL5829727 | — | — | 3 | 6.41 |
| CHEMBL6054615 | — | — | 3 | 6.30 |
| CHEMBL5837951 | — | — | 3 | 6.28 |
| CHEMBL5962512 | — | — | 6 | 6.26 |
| CHEMBL5969470 | — | — | 3 | 6.26 |
| CHEMBL5769726 | — | — | 6 | 6.26 |
| CHEMBL5742640 | — | — | 6 | 6.24 |
| CHEMBL5880676 | — | — | 3 | 6.17 |
| CHEMBL6006530 | — | — | 3 | 6.17 |
| CHEMBL5793217 | — | — | 3 | 6.15 |
| CHEMBL5795237 | — | — | 3 | 6.13 |
| CHEMBL5813943 | — | — | 3 | 6.08 |
| CHEMBL6007842 | — | — | 3 | 6.07 |
| CHEMBL6053977 | — | — | 6 | 6.06 |
| CHEMBL6053142 | — | — | 3 | 6.03 |
| CHEMBL5831090 | — | — | 3 | 6.01 |
| CHEMBL5861219 | — | — | 3 | 6.01 |
| CHEMBL6023444 | — | — | 6 | 6.00 |
| CHEMBL5862883 | — | — | 3 | 5.99 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5859458 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL6024784 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5831615 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5961990 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL5802716 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5962730 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL5970747 | — | IC50 | = | 209.0 | nM | 6.68 |
| CHEMBL4874034 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL5954577 | — | IC50 | = | 378.0 | nM | 6.42 |
| CHEMBL5913296 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL5899647 | — | IC50 | = | 384.0 | nM | 6.42 |
| CHEMBL5829727 | — | IC50 | = | 387.0 | nM | 6.41 |
| CHEMBL6054615 | — | IC50 | = | 501.0 | nM | 6.30 |
| CHEMBL5837951 | — | IC50 | = | 520.0 | nM | 6.28 |
| CHEMBL5962512 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL5969470 | — | IC50 | = | 549.0 | nM | 6.26 |
| CHEMBL5769726 | — | IC50 | = | 547.0 | nM | 6.26 |
| CHEMBL5742640 | — | IC50 | = | 581.0 | nM | 6.24 |
| CHEMBL6006530 | — | IC50 | = | 682.0 | nM | 6.17 |
| CHEMBL5880676 | — | IC50 | = | 682.0 | nM | 6.17 |
| CHEMBL5793217 | — | IC50 | = | 701.0 | nM | 6.15 |
| CHEMBL5795237 | — | IC50 | = | 740.0 | nM | 6.13 |
| CHEMBL5813943 | — | IC50 | = | 823.0 | nM | 6.08 |
| CHEMBL5769726 | — | IC50 | = | 823.0 | nM | 6.08 |
| CHEMBL6007842 | — | IC50 | = | 848.0 | nM | 6.07 |
| CHEMBL6053977 | — | IC50 | = | 879.0 | nM | 6.06 |
| CHEMBL6053142 | — | IC50 | = | 945.0 | nM | 6.03 |
| CHEMBL5831090 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL5861219 | — | IC50 | = | 978.0 | nM | 6.01 |
| CHEMBL6023444 | — | IC50 | = | 990.0 | nM | 6.00 |
| CHEMBL5862883 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL5926301 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5935305 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL5902596 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL5801234 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL6024813 | — | IC50 | = | 1230.0 | nM | 5.91 |
| CHEMBL5760423 | — | IC50 | = | 1220.0 | nM | 5.91 |
| CHEMBL6016907 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL6065607 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL5864271 | — | IC50 | = | 1310.0 | nM | 5.88 |
| CHEMBL5742640 | — | IC50 | = | 1345.0 | nM | 5.87 |
| CHEMBL5912335 | — | IC50 | = | 1380.0 | nM | 5.86 |
| CHEMBL5973514 | — | IC50 | = | 1440.0 | nM | 5.84 |
| CHEMBL5802577 | — | IC50 | = | 1530.0 | nM | 5.82 |
| CHEMBL6046223 | — | IC50 | = | 1540.0 | nM | 5.81 |
| CHEMBL5962512 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL5941233 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL4859812 | — | IC50 | = | 2053.0 | nM | 5.69 |
| CHEMBL5849058 | — | IC50 | = | 2295.0 | nM | 5.64 |
| CHEMBL5760423 | — | IC50 | = | 2590.0 | nM | 5.59 |