| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA4040229 | A | Drug metabolism assessed as recombinant human NEP-medited peptide proteolysis at 1 mM up to 72 hrs by LC-MS analysis | Homo sapiens | 16 | ALA4038314 | single protein format | Scientific Literature | |
| 2. | ALA4040230 | A | Drug degradation in human plasma assessed as NEP-mediated degradation by measuring amount of apelin remaining after 30 mins by RP-HPLC analysis | Homo sapiens | 16 | ALA4038314 | single protein format | Scientific Literature | |
| 3. | ALA4040231 | A | Drug degradation in human plasma assessed as NEP-mediated degradation by measuring amount of apelin remaining after 60 mins by RP-HPLC analysis | Homo sapiens | 16 | ALA4038314 | single protein format | Scientific Literature | |
| 4. | ALA4040233 | B | Displacement of [125I]-pyr-1-apelin-13 from rat C-terminal EGFP-tagged APJ receptor expressed in CHO cell membranes after 3 hrs by Wallac gamma counting | Rattus norvegicus | 16 | ALA4038314 | cell-based format | Scientific Literature | |
| 5. | ALA4040235 | F | Cardiovascular activity in anesthetized mouse assessed as decrease in blood pressure at 1.4 uM/kg, iv relative to control | Mus musculus | 8 | ALA4038314 | organism-based format | Scientific Literature | |
| 6. | ALA4040240 | T | Cardiotoxicity in anesthetized mouse assessed as induction of tachycardia at 1.4 uM/kg, iv relative to control | Mus musculus | 8 | ALA4038314 | organism-based format | Scientific Literature | |
| 7. | ALA4401027 | A | Substrate activity at KLKB1 in human plasma assessed as (S)-2-((S)-2-((S)-2,6-diaminohexanamido)-3-phenylpropanamido)-5-guanidinopentanoic acid formation at 400 uM measured after 10 to 30 mins by LC-MS analysis | Homo sapiens | 1 | ALA4400521 | cell-free format | Scientific Literature | |
| 8. | ALA4401028 | A | Substrate activity at KLKB1 in human plasma assessed as (S)-2-(2-((S)-2-((S)-1-((6S,9S,12S,15S,18S)-15-((1H-imidazol-4-yl)methyl)-1-amino-18-(4-aminobutyl)-6-((S)-1-((S)-2-((S)-2,5-diamino-5-oxopentanamido)-5-guanidinopentanoyl)pyrrolidine-2-carboxamido)-12-(hydroxymethyl)-1-imino-9-isobutyl-7,10,13,16,19-pentaoxo-2,8,11,14,17,20-hexaazadocosane)pyrrolidine-2-carboxamido)hexanamido)-2-methylpropanamido)-3-(4-bromophenyl)propanoic acid formation at 400 uM measured after 10 to 30 mins by LC-MS analysis | Homo sapiens | 1 | ALA4400521 | cell-free format | Scientific Literature | |
| 9. | ALA4401029 | A | Substrate activity at recombinant human NEP (Tyr52 to Trp750 residues) expressed in HEK293 cells assessed as enzyme-mediated degradation onset time at 1 mM by MALDI-TOF MS analysis | Homo sapiens | 7 | ALA4400521 | cell-based format | Scientific Literature | |
| 10. | ALA4401030 | A | Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as enzyme-mediated degradation onset time at 1 mM by MALDI-TOF MS analysis | Homo sapiens | 6 | ALA4400521 | assay format | Scientific Literature | |
| 11. | ALA4401034 | A | Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as Km measured after 30 to 60 mins by LC-MS analysis | Homo sapiens | 4 | ALA4400521 | assay format | Scientific Literature | |
| 12. | ALA4401035 | A | Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as Kcat measured after 30 to 60 mins by LC-MS analysis | Homo sapiens | 4 | ALA4400521 | assay format | Scientific Literature | |
| 13. | ALA4401036 | A | Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as ratio of Kcat to Km measured after 30 to 60 mins by LC-MS analysis | Homo sapiens | 4 | ALA4400521 | assay format | Scientific Literature | |
| 14. | ALA4401043 | A | Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as Vmax measured after 30 to 60 mins by LC-MS analysis | Homo sapiens | 3 | ALA4400521 | assay format | Scientific Literature | |
| 15. | ALA4401044 | A | Substrate activity at recombinant human C-terminal His6-tagged KLKB1 (Pro19 to Ser262 residues) expressed in mammalian expression system assessed as compound half life by LC-MS analysis | Homo sapiens | 7 | ALA4400521 | assay format | Scientific Literature | |
| 16. | ALA4401045 | A | Substrate activity at recombinant human NEP (Tyr52 to Trp750 residues) expressed in HEK293 cells assessed as compound half life by LC-MS analysis | Homo sapiens | 7 | ALA4400521 | cell-based format | Scientific Literature | |
| 17. | ALA4401046 | A | Substrate activity at KLKB1 in human plasma assessed as compound half life by LC-MS analysis | Homo sapiens | 7 | ALA4400521 | cell-free format | Scientific Literature | |
| 18. | ALA4401047 | B | Displacement of [125I]-(Glp1,Nle11,Try14)apelin-13 from recombinant rat EGFP-fused apelin receptor expressed in CHO cell membrane measured after 3 hrs | Rattus norvegicus | 9 | ALA4400521 | cell-based format | Scientific Literature | |
| 19. | ALA4401048 | F | Activation of recombinant human APJ expressed in rat Chem5 cells co-expressing Galpha15 by Calcium 6-QF dye based fluorescence assay | Homo sapiens | 9 | ALA4400521 | cell-based format | Scientific Literature | |
| 20. | ALA4401049 | F | Blood pressure lowering activity in anesthetized mouse assessed as change in mean arterial blood pressure at 1.4 uM/kg, iv | Mus musculus | 9 | ALA4400521 | organism-based format | Scientific Literature |
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