| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA4122259 | A | Half life in mouse liver microsomes at 3 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis | Mus musculus | 3 | microsome format | Scientific Literature | ||
| 2. | ALA4122260 | A | Half life in human liver microsomes at 3 uM preincubated for 5 mins followed by NADPH addition by LC-MS/MS analysis | Homo sapiens | 3 | microsome format | Scientific Literature | ||
| 3. | ALA4122261 | P | Kinetic solubility of the compound in PBS at pH 7.4 at 6.75 to 200 uM after 90 mins by UV absorbance based assay | 3 | small-molecule physicochemical format | Scientific Literature | |||
| 4. | 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 | cell-based format | Scientific Literature | ||
| 5. | ALA4122266 | B | Inhibition of recombinant C-terminal His10-tagged human uPA (M1 to L431 residues) expressed in mouse NS0 cells using Z-GGR-AMC as substrate after 15 mins by manual fluorescence assay | Homo sapiens | 7 | cell-based format | Scientific Literature | ||
| 6. | ALA4122267 | B | Selectivity ratio of IC50 for recombinant C-terminal His10-tagged human uPA (M1 to L431 residues) to IC50 for recombinant C-terminal His10-tagged human Hepsin (R45 to L17 residues) D161E/ R162K double mutant by manual fluorescence assay | Homo sapiens | 7 | assay format | Scientific Literature | ||
| 7. | ALA4122268 | A | Apparent permeability of the compound at 50 to 200 uM after 5 hrs by PAMPA | 3 | assay format | Scientific Literature | |||
| 8. | ALA4122269 | A | Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue/CytoTox-ONE-based assay | Homo sapiens | 3 | cell-based format | Scientific Literature | ||
| 9. | 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 | cell-based format | Scientific Literature | ||
| 10. | 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 | cell-based format | Scientific Literature | ||
| 11. | 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 | cell-based format | Scientific Literature | ||
| 12. | 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 | cell-based format | Scientific Literature | ||
| 13. | 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 | cell-based format | Scientific Literature | ||
| 14. | 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 | cell-based format | Scientific Literature | ||
| 15. | 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 | cell-based format | Scientific Literature | ||
| 16. | ALA4122280 | 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 beta chain formation at 1 uM incubated for 30 mins in presence of recombinant human pro-HGF by immunoblot method | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 17. | ALA4122281 | B | Inhibition of doxycycline induced hepsin-mediated loss of desmosomal junctions in human MCF10A cells at 1 to 10 uM preincubated for 30 mins followed by doxycycline addition measured after 6 hrs by desmoglein 2 staining-based confocal immunofluorescence microscopic analysis | Homo sapiens | 2 | cell-based format | Scientific Literature | ||
| 18. | ALA4122282 | B | Inhibition of human thrombin using Z-Gly-Pro-Arg-AMC as substrate at 1 uM after 60 mins by fluorescence spectrophotometric method relative to control | Homo sapiens | 3 | single protein format | Scientific Literature | ||
| 19. | ALA4122283 | B | Inhibition of human thrombin using Z-Gly-Pro-Arg-AMC as substrate at 10 uM after 60 mins by fluorescence spectrophotometric method relative to control | Homo sapiens | 3 | single protein format | Scientific Literature | ||
| 20. | ALA4122284 | B | Inhibition of human chymase using Suc-Ala-Ala-Pro-Phe-AMC as substrate at 1 uM after 120 mins by fluorescence spectrophotometric method relative to control | Homo sapiens | 3 | single protein format | Scientific Literature |
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