| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA2090836 | B | Tight binding inhibition of human hepsin expressed in Drosophila melanogaster S2 cells using Boc-QAR-AMC as substrate incubated for 15 mins prior to substrate addition measured for 30 mins by fluorimetric analysis | Homo sapiens | 1 | ALA2086329 | cell-based format | Scientific Literature | |
| 2. | ALA3389936 | B | Inhibition of recombinant hepsin (unknown origin) using Boc-QAR-AMC as substrate by fluorescence assay | Homo sapiens | 20 | ALA3352254 | single protein format | Scientific Literature | |
| 3. | ALA3404297 | B | Inhibition of hepsin (unknown origin) using Boc-QAR-AMC as substrate after 30 mins prior to substrate addition by fluorescence assay | Homo sapiens | 17 | ALA3400148 | single protein format | Scientific Literature | |
| 4. | ALA3404298 | B | Inhibition of hepsin (unknown origin) | Homo sapiens | 1 | ALA3400148 | single protein format | Scientific Literature | |
| 5. | ALA3637191 | B | Inhibition of human recombinant hepsin by fluorescence based assay using 65 uM BOC-Gln-Arg-Arg -AMC as substrate | Homo sapiens | 10 | ALA3632605 | single protein format | Scientific Literature | |
| 6. | ALA3748443 | B | Inhibition of human recombinant hepsin using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition measured for 15 to 120 mins by plate reader analysis | Homo sapiens | 12 | ALA3745608 | single protein format | Scientific Literature | |
| 7. | ALA3782551 | B | Inhibition of human recombinant hepsin using H2N(EEdansyl)GKQLRVVNGG (KDabcyl)-NH2 as substrate by fluorometric analysis | Homo sapiens | 19 | ALA3779883 | single protein format | Scientific Literature | |
| 8. | ALA3830286 | B | Inhibition of recombinant human hepsin using Boc-QAR-AMC as substrate preincubated for 30 mins followed by substrate addition by fluorescence assay | Homo sapiens | 11 | ALA3826925 | single protein format | Scientific Literature | |
| 9. | ALA3887550 | B | High-Throughput Screening Assay: To identify novel inhibitors of hepsin, the Chembridge DIVERSet 10,000 compound high-diversity library was screened using an assay based on the cleavage of the chromogenic peptide. In addition, the NINDS II library of 1040 compounds (MicroSource Discovery) was screened to identify hepsin inhibitors among established drugs and known bioactive molecules. Screens were performed in a 96-well format at a final compound concentration of 2 uM. To minimize false positives, positions 1 and 12 of each row contained DMSO/buffer controls. As a measure of reproducibility, the Z' score for this assay was 0.78 (Zhang et al., 1999 J Biomol Screen 4:67). | Homo sapiens | 16 | ALA3886357 | single protein format | BindingDB Database | |
| 10. | ALA4122262 | B | Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells using Boc-QRR-AMC as substrate after 15 mins by automated fluorescence assay | Homo sapiens | 35 | ALA4118144 | cell-based format | Scientific Literature | |
| 11. | ALA4122265 | B | Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells using Boc-QRR-AMC as substrate after 15 mins by manual fluorescence assay | Homo sapiens | 8 | ALA4118144 | cell-based format | Scientific Literature | |
| 12. | ALA4122270 | B | Inhibition of doxycycline induced Hepsin in human MCF10A cells using Boc-QRR-AMC as substrate preincubated for 24 hrs followed by doxycycline induction for 24 hrs and subsequent addition of substrate by fluorescence assay | Homo sapiens | 5 | ALA4118144 | cell-based format | Scientific Literature | |
| 13. | ALA4122271 | B | Inhibition of doxycycline induced Hepsin in human MCF10A cells assessed as prevention in loss of HAI-1 level at 10 uM preincubated for 30 mins followed by doxycycline addition measured after 6 hrs by Immunoblot assay | Homo sapiens | 5 | ALA4118144 | cell-based format | Scientific Literature | |
| 14. | ALA4122273 | B | Inhibition of doxycycline induced hepsin-mediated conversion of Pro-HGF into active form in human MCF10A cells assessed as decrease in MET phosphorylation (Tyr1243/1245) at 1 to 10 uM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot method | Homo sapiens | 1 | ALA4118144 | cell-based format | Scientific Literature | |
| 15. | ALA4122274 | B | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human Hs578T cells assessed as decrease in MET phosphorylation at 1 to 10 uM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot method | Homo sapiens | 5 | ALA4118144 | cell-based format | Scientific Literature | |
| 16. | ALA4122275 | B | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human Hs578T cells assessed as decrease in MET phosphorylation at 1 uM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot method | Homo sapiens | 1 | ALA4118144 | cell-based format | Scientific Literature | |
| 17. | ALA4122276 | B | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human HCC1937 cells assessed as decrease in MET phosphorylation at 1 uM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot method | Homo sapiens | 1 | ALA4118144 | cell-based format | Scientific Literature | |
| 18. | ALA4122277 | B | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human Hs578T cells assessed as decrease in MET phosphorylation at 100 nM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot method | Homo sapiens | 1 | ALA4118144 | cell-based format | Scientific Literature | |
| 19. | ALA4122278 | B | Inhibition of hepsin-mediated conversion of Pro-HGF into active form in human HCC1937 cells assessed as decrease in MET phosphorylation at 100 nM preincubated for 30 mins followed by recombinant human pro-HGF addition measured after 30 mins by immunoblot method | Homo sapiens | 1 | ALA4118144 | cell-based format | Scientific Literature | |
| 20. | ALA4122279 | B | Inhibition of recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant expressed in mouse NS0 cells assessed as decrease in HGF alpha chain formation at 1 uM incubated for 30 mins in presence of recombinant human pro-HGF by immunoblot method | Homo sapiens | 1 | ALA4118144 | cell-based format | Scientific Literature |
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