| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA2327470 | F | Inhibition of VAP1-mediated ocular permeability in streptozotocin-induced Sprague-Dawley rat diabetic model assessed as fluorescein leakage in vitreous at 1 to 10 mg/kg, sc administered daily for 4 weeks post streptozotocin challenge measured 24 hrs post last dose by fluorescence assay | Rattus norvegicus | 1 | organism-based format | Scientific Literature | ||
| 2. | ALA2327663 | A | Plasma concentration in Wistar rat at 0.1 mg/kg, sc after 0.5 to 6 hrs by LC-MS analysis | Rattus norvegicus | 1 | organism-based format | Scientific Literature | ||
| 3. | ALA2327664 | F | Inhibition of VAP1 in streptozotocin-induced Wistar rat diabetic model using [14C]-benzylamine as substrate assessed as [14C]-benzylaldehyde formation in plasma at >/= 0.1 mg/kg, sc after 1 hr by liquid scintillation counting analysis | Rattus norvegicus | 1 | organism-based format | Scientific Literature | ||
| 4. | ALA2327665 | A | Plasma concentration in sc dosed Wistar rat after 0.5 to 6 hrs by LC-MS analysis | Rattus norvegicus | 1 | organism-based format | Scientific Literature | ||
| 5. | ALA2327666 | B | Selectivity ratio of IC50 for human MAOB to IC50 for human VAP1 | Homo sapiens | 1 | assay format | Scientific Literature | ||
| 6. | ALA2327667 | B | Selectivity ratio of IC50 for human DAO to IC50 for human VAP1 | Homo sapiens | 1 | assay format | Scientific Literature | ||
| 7. | ALA2327668 | B | Selectivity ratio of IC50 for human VAP1 to IC50 for rat VAP1 | 1 | assay format | Scientific Literature | |||
| 8. | ALA2327669 | B | Inhibition of human DAO expressed in CHO cells using putrescine as substrate after 1 hr by fluorometric assay | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 9. | ALA2327670 | B | Inhibition of rat liver DAO using putrescine as substrate after 1 hr by fluorometric assay | Rattus norvegicus | 1 | assay format | Scientific Literature | ||
| 10. | ALA2327671 | B | Inhibition of rat VAP1 expressed in CHO cells using [14C]-benzylamine as substrate incubated for 30 mins prior to substrate addition measured after 1 hr by scintillation spectrophotometric analysis | Rattus norvegicus | 1 | cell-based format | Scientific Literature | ||
| 11. | ALA2327672 | B | Inhibition of human VAP1 expressed in CHO cells using [14C]-benzylamine as substrate incubated for 30 mins prior to substrate addition measured after 1 hr by scintillation spectrophotometric analysis | Homo sapiens | 20 | cell-based format | Scientific Literature | ||
| 12. | ALA2327673 | B | Inhibition of human MAOB expressed in CHO cells using benzylamine as substrate after 1 hr by fluorometric assay | Homo sapiens | 1 | cell-based format | Scientific Literature | ||
| 13. | ALA2393848 | B | Inhibition of human recombinant MAO-B using benzylamine as substrate after 1 hr by fluorometric assay | Homo sapiens | 2 | single protein format | Scientific Literature | ||
| 14. | ALA2393850 | B | Inhibition of rat VAP-1 expressed in CHO cells using [14C]-benzylamine as substrate preincubated for 30 mins prior to substrate addition measured after 1 hr by scintillation spectrometric analysis | Rattus norvegicus | 20 | cell-based format | Scientific Literature | ||
| 15. | ALA2393975 | B | Inhibition of human recombinant MAO-A using 5-hydroxytryptamine as substrate after 1 hr by fluorometric assay | Homo sapiens | 2 | single protein format | Scientific Literature | ||
| 16. | ALA2393976 | B | Inhibition of human VAP-1 expressed in CHO cells using [14C]-benzylamine as substrate preincubated for 30 mins prior to substrate addition measured after 1 hr by scintillation spectrometric analysis | Homo sapiens | 20 | cell-based format | Scientific Literature | ||
| 17. | ALA3301363 | P | ASTRAZENECA: Octan-1-ol/water (pH7.4) distribution coefficent measured by a shake flask method described in J. Biomol. Screen. 2011, 16, 348-355. Experimental range -1.5 to 4.5 | 4,197 | small-molecule physicochemical format | AstraZeneca Deposited Data | |||
| 18. | ALA3301365 | A | ASTRAZENECA: % bound to plasma by equilibrium dialysis. Compound is incubated with whole human plasma at 37C for >5hrs. Method described in B. Testa et al (Eds.), Pharmacokinetic Profiling in Drug Research: Biological, Physicochemical, and Computational Strategies, Wiley-VCH, Weinheim, 2006, pp.119-141. Experimental range 10% to 99.95% bound. | Homo sapiens | 1,614 | cell-free format | AstraZeneca Deposited Data | ||
| 19. | ALA3301370 | A | ASTRAZENECA: Intrinsic clearance measured in human liver microsomes following incubation at 37C. Experimental range <3 to >150 microL/min/mg. Rapid Commun. Mass Spectrom. 2010, 24, 1730-1736. | Homo sapiens | 1,102 | microsome format | AstraZeneca Deposited Data | ||
| 20. | ALA3301371 | A | ASTRAZENECA: Intrinsic clearance measured in rat hepatocytes following incubation at 37C. Experimental range <3 to >150 microL/min/1E6 cells. Rapid Commun. Mass Spectrom. 2010, 24, 1730-1736 | Rattus norvegicus | 837 | cell-based format | AstraZeneca Deposited Data |
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