# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA917590 | B | Inhibition of recombinant CatA using [14C]GS-7340 substrate | Homo sapiens | 3 | ALA1142204 | single protein format | Scientific Literature | |
2. | ALA917592 | B | Activity of Cat A assessed as hydrolysis | Homo sapiens | 2 | ALA1142204 | single protein format | Scientific Literature | |
3. | ALA917596 | B | Activity of purified human PBMCs Cat A from leukopheresis patient in Con A pool | Homo sapiens | 2 | ALA1142204 | single protein format | Scientific Literature | |
4. | ALA917589 | B | Ratio of kcat to Km for Cat A activity | Homo sapiens | 2 | ALA1142204 | single protein format | Scientific Literature | |
5. | ALA2176198 | B | Inhibition of human recombinant Myc-His10-tagged cathepsin A expressed in baculovirus infected Sf9 cells using BodipyFL labeled bradykinin as substrate incubated for 15 mins prior to substrate addition measured after 15 mins by fluorimetric analysis | Homo sapiens | 33 | ALA2169867 | cell-based format | Scientific Literature | |
6. | ALA2209084 | B | Inhibition of CTSA binding to FP-biotin in [12C][14N]-lysine, arginine and [13C6][15N2]-lysine, arginine labeled HEK293T cells at 20 uM after 1 hr by isotopic activity-based protein profiling-MudPIT assay | Homo sapiens | 1 | ALA2203175 | cell-based format | Scientific Literature | |
7. | ALA3240090 | B | Inhibition of recombinant cathepsin A (unknown origin) using Mca-Arg-Pro-Pro-Gly-Phe-Ser-Ala-Phe-Lys(Dnp)-OH as substrate incubated with enzyme for 5 mins prior to substrate challenge for 2 hrs by spectrofluorometer analysis | Homo sapiens | 4 | ALA3232719 | single protein format | Scientific Literature | |
8. | ALA3578763 | B | Inhibition of cathepsin A (unknown origin) using MCA-RPPGFSAFK-Dnp as substrate preincubated for 10 mins followed by substrate addition measured for 30 mins by spectrophotometric analysis | Homo sapiens | 1 | ALA3576866 | single protein format | Scientific Literature | |
9. | ALA3705983 | B | Inhibition Assay: The activated cathepsin A was diluted in assay buffer (25 mM MES, pH 5.5, containing 5 mM DTT) and mixed with the test compound (dissolved in assay buffer containing (v/v) 3% DMSO) or, in the control experiments, with the vehicle in a multiple assay plate. After incubation for 15 min at room temperature, as substrate then bradykinin carrying an N-terminal ®Bodipy FL (4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene-3-propionyl) label (JPT Peptide Technologies GmbH; dissolved in assay buffer) was added to the mixture. The final concentration of cathepsin A was 833 ng/ml and the final concentration of labeled bradykinin 2 μM. After incubation for 15 min at room temperature the reaction was stopped by the addition of stop buffer (130 mM 2-(4-(2-hydroxy-ethyl)-piperazin-1-yl)-ethanesulfonic acid, pH 7.4, containing (v/v) 0.013% ®Triton X-100, 0.13% Coating Reagent 3 (Caliper Life Sciences), 6.5% DMSO and 20 μM ebelactone B (Sigma, #E0886)). | 500 | ALA3639381 | single protein format | BindingDB Database | ||
10. | ALA3887323 | B | Inhibition Assay: Recombinant human cathepsin A (residues 29-480, with a C-terminal 10-His tag; R&D Systems, #1049-SE) was proteolytically activated with recombinant human cathepsin L (R&D Systems, #952-CY). Briefly, cathepsin A was incubated at 10 ug/ml with cathepsin L at 1 ug/ml in activation buffer (25 mM 2-(morpholin-4-yl)-ethanesulfonic acid (MES), pH 6.0, containing 5 mM dithiothreitol (DTT)) for 15 min at 37° C. Cathepsin L activity was then stopped by the addition of the cysteine protease inhibitor E-64 (N-(trans-epoxysuccinyl)-L-leucine-4-guanidinobutylamide; Sigma-Aldrich, # E3132; dissolved in activation buffer/DMSO) to a final concentration of 10 uM.The activated cathepsin A was diluted in assay buffer (25 mM MES, pH 5.5, containing 5 mM DTT) and mixed with the test compound (dissolved in assay buffer containing (v/v) 3% DMSO) or, in the control experiments, with the vehicle in a multiple assay plate. After incubation for 15 min at room temperature. | 208 | ALA3886275 | single protein format | BindingDB Database | ||
11. | ALA3887623 | B | Inhibition Assay: The activated cathepsin A was diluted in assay buffer (25 mM MES, pH 5.5, containing 5 mM DTT) and mixed with the test compound (dissolved in assay buffer containing (v/v) 3% DMSO) or, in the control experiments, with the vehicle in a multiple assay plate. After incubation for 15 min at room temperature, as substrate then bradykinin carrying an N-terminal® Bodipy FL (4,4-difluoro-5,7-dimethyl-4-bora-3a,4a-diaza-s-indacene-3-propionyl) label (JPT Peptide Technologies GmbH; dissolved in assay buffer) was added to the mixture. The final concentration of cathepsin A was 833 ng/ml and the final concentration of labeled bradykinin 2 μM. After incubation for 15 min at room temperature the reaction was stopped by the addition of stop buffer (130 mM 2-(4-(2-hydroxy-ethyl)-piperazin-1-yl)-ethanesulfonic acid, pH 7.4, containing (v/v) 0.013%° Triton X-100, 0.13% Coating Reagent 3 (Caliper Life Sciences), 6.5% DMSO and 20 μM ebelactone B (Sigma, #E0886)). | 139 | ALA3886385 | single protein format | BindingDB Database | ||
12. | ALA4046686 | A | Drug metabolism assessed as CatA (unknown origin)-mediated monophosphate formation after 18 hrs relative to control | Homo sapiens | 3 | ALA4043192 | single protein format | Scientific Literature | |
13. | ALA4050836 | A | Drug metabolism in pH 7.4 trizma buffer assessed as cathepsin A (unknown origin)-mediated (S)-2-((((2R,3S,4R,5R)-5-(6-(furan-2-ylmethylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)oxidophosphorylamino)propanoate formation at 5.0 mg measured after 2 to 12 hrs by 31P-NMR spectroscopic analysis | Homo sapiens | 1 | ALA4049415 | single protein format | Scientific Literature | |
14. | ALA4050844 | A | Stability in pH 7.4 trizma buffer assessed as cathepsin A (unknown origin)-mediated compound hydrolysis at 5.0 mg measured after 15 mins by 31P-NMR spectroscopic analysis | Homo sapiens | 1 | ALA4049415 | single protein format | Scientific Literature | |
15. | ALA4050845 | A | Drug level in pH 7.4 trizma buffer treated with phenyl(Isopropoxy-L-alaninyl) kinetin riboside phosphoramidate assessed as cathepsin A (unknown origin)-mediated metabolite formation at 5.0 mg measured after 2 to 12 hrs by 31P-NMR spectroscopic analysis | Homo sapiens | 1 | ALA4049415 | single protein format | Scientific Literature | |
16. | ALA4050846 | A | Prodrug activation in pH 7.4 trizma buffer assessed as cathepsin A (unknown origin)-mediated kinetin riboside monophosphate metabolite formation at 5.0 mg measured after 48 hrs by 31P-NMR spectroscopic analysis | Homo sapiens | 1 | ALA4049415 | single protein format | Scientific Literature | |
17. | ALA4050847 | A | Stability in pH 7.4 trizma buffer assessed as cathepsin A (unknown origin)-mediated compound hydrolysis by measuring parent compound remaining at 5.0 mg measured after 12 hrs by 31P-NMR spectroscopic analysis | Homo sapiens | 2 | ALA4049415 | single protein format | Scientific Literature | |
18. | ALA4841950 | B | Substrate activity at cathepsin A (unknown origin) at 30 uM after 30 mins | Homo sapiens | 9 | ALA4840358 | single protein format | Scientific Literature |
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