Assay Detail
Binding
CHEMBL5733554
Review assay metadata, readout intent, target linkage, and publication context from the same page.
In Vitro Assay: ADAMTS-4:The basis for the assay is the cleavage of the substrate TBIS-1 (5-FAM-TEGEARGSVILLK (5TAMRA)K-NH2) (SEQ ID No 2) by human ADAMTS4For 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 Hepes pH7.5, 100 mM NaCl, 5 mM CaCl2, 0.1% CHAPS, 5% glycerol) containing hADAMTS4 (0.325 ng/L) (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 TBIS-1 (10 μL, 4.5 μM, Anaspec) 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 535).
528
Total Activities
175
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| 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 | 176 | 7.00 | 8.30 |
| kon | 176 | - | - |
| k_off | 176 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4874034 | — | — | 3 | 8.30 |
| CHEMBL5851590 | — | — | 3 | 8.30 |
| CHEMBL5769726 | — | — | 3 | 8.22 |
| CHEMBL6023444 | — | — | 3 | 8.22 |
| CHEMBL5845522 | — | — | 3 | 8.15 |
| CHEMBL5806226 | — | — | 3 | 8.15 |
| CHEMBL5982976 | — | — | 3 | 8.00 |
| CHEMBL6040418 | — | — | 3 | 7.96 |
| CHEMBL6012959 | — | — | 3 | 7.96 |
| CHEMBL5932436 | — | — | 3 | 7.96 |
| CHEMBL5996710 | — | — | 3 | 7.82 |
| CHEMBL6036847 | — | — | 3 | 7.77 |
| CHEMBL6016907 | — | — | 3 | 7.77 |
| CHEMBL5839480 | — | — | 3 | 7.75 |
| CHEMBL6053977 | — | — | 3 | 7.75 |
| CHEMBL5913296 | — | — | 3 | 7.70 |
| CHEMBL5742640 | — | — | 3 | 7.70 |
| CHEMBL6059207 | — | — | 3 | 7.68 |
| CHEMBL5869212 | — | — | 3 | 7.68 |
| CHEMBL5872666 | — | — | 3 | 7.68 |
| CHEMBL6010345 | — | — | 3 | 7.66 |
| CHEMBL5849058 | — | — | 3 | 7.66 |
| CHEMBL5816915 | — | — | 3 | 7.64 |
| CHEMBL4650334 | ALDUMASTAT | 2.0 | 3 | 7.64 |
| CHEMBL5949991 | — | — | 3 | 7.62 |
| CHEMBL6036614 | — | — | 3 | 7.62 |
| CHEMBL6055505 | — | — | 3 | 7.58 |
| CHEMBL6056403 | — | — | 3 | 7.57 |
| CHEMBL5924924 | — | — | 3 | 7.57 |
| CHEMBL4854306 | — | — | 3 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5851590 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4874034 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5769726 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL6023444 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5806226 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5845522 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5982976 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5932436 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL6012959 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL6040418 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5996710 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL6016907 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL6036847 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5839480 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL6053977 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5742640 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5913296 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5872666 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5869212 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL6059207 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5849058 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL6010345 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5816915 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4650334 | ALDUMASTAT | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL6036614 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5949991 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL6055505 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL6056403 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5924924 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL6002399 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4854306 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5913647 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5935305 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL5777064 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5786978 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5801234 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5872368 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL5894569 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5904713 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL4864100 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL5873922 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5909928 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5818101 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL5891470 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5872970 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5922080 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5992754 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL5866536 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4877087 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL6061166 | — | IC50 | = | 42.0 | nM | 7.38 |