# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA3816166 | Binding | Inhibition of recombinant PI3Kalpha (unknown origin) using dioctanoylglycerol-PIP2 as substrate incubated for 30 mins in presence of TAMRA-PIP3 by fluorescence polarization assay | Homo sapiens | 11 | ALA3813614 | single protein format | Scientific Literature | |
2. | ALA3816167 | Binding | Inhibition of human recombinant mTOR (1360 to 2549 residues) expressed in insect cells assessed as inhibition of GFP-labeled 4-EBP1 phosphorylation at Thr-37/46 residues incubated for 30 mins by FRET assay | Homo sapiens | 6 | ALA3813614 | cell-based format | Scientific Literature | |
3. | ALA3816168 | Functional | Antiproliferative activity against human PC3 cells after 3 days by CellTitre-Glo assay | Homo sapiens | 11 | ALA3813614 | cell-based format | Scientific Literature | |
4. | ALA3816169 | ADME | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in MDCK1 cells expressing human MDR1 at 5 uM incubated for 2 hrs by LC-MS/MS analysis | Canis lupus familiaris | 10 | ALA3813614 | cell-based format | Scientific Literature | |
5. | ALA3816170 | ADME | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral side in MDCK2 cells expressing mouse BCRP1 at 5 uM incubated for 2 hrs by LC-MS/MS analysis | Canis lupus familiaris | 11 | ALA3813614 | cell-based format | Scientific Literature | |
6. | ALA3816172 | ADME | Ratio of unbound fraction in CD1 mouse brain to plasma at 50 mg/kg, po after 6 hrs by LC-MS/MS analysis | Mus musculus | 1 | ALA3813614 | organism-based format | Scientific Literature | |
7. | ALA2185131 | Functional | Inhibition of PI3Kalpha in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as reduction in S6RP phosphorylation at 10 mg/kg, po qd for 24 days measured 1 to 4 hrs post last dose by electrochemiluminescence assay | Mus musculus | 2 | ALA2177093 | organism-based format | Scientific Literature | |
8. | ALA2185132 | Functional | Inhibition of PI3Kalpha in PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as reduction in S6RP phosphorylation at 40 mg/kg, po qd for 24 days measured 1 to 4 hrs post last dose by electrochemiluminescence assay | Mus musculus | 2 | ALA2177093 | organism-based format | Scientific Literature | |
9. | ALA2185133 | ADME | Drug uptake in NCr nude mouse brain xenografted with PTEN deficient human U87MG cells at 40 mg/kg after 1 hr | Mus musculus | 1 | ALA2177093 | organism-based format | Scientific Literature | |
10. | ALA2185134 | ADME | Drug uptake in healthy mouse brain at 50 mg/kg after 1 hr | Mus musculus | 1 | ALA2177093 | organism-based format | Scientific Literature | |
11. | ALA2185825 | Binding | Inhibition of PI3KC2beta at 1 uM | 1 | ALA2177093 | single protein format | Scientific Literature | ||
12. | ALA2185828 | Functional | Antitumor activity against PTEN deficient human U87MG cells xenografted in NCr nude mouse assessed as inhibition of tumor growth at 3 to 14 mg/kg, po qd for 24 days | Homo sapiens | 2 | ALA2177093 | organism-based format | Scientific Literature | |
13. | ALA2185829 | ADME | Fraction unbound in CD-1 mouse brain at 50 mg/kg, po administered as single dose measured after 6 hrs post dose | Mus musculus | 1 | ALA2177093 | organism-based format | Scientific Literature | |
14. | ALA2185830 | ADME | Fraction unbound in CD-1 mouse brain at 50 mg/kg, po administered as single dose measured after 1 hr post dose | Mus musculus | 1 | ALA2177093 | organism-based format | Scientific Literature | |
15. | ALA2185833 | ADME | Drug level in CD-1 mouse brain at 50 mg/kg, po administered as single dose measured after 6 hrs post dose | Mus musculus | 1 | ALA2177093 | organism-based format | Scientific Literature | |
16. | ALA2185835 | ADME | Drug level in CD-1 mouse brain at 50 mg/kg, po administered as single dose measured after 1 hr post dose | Mus musculus | 1 | ALA2177093 | organism-based format | Scientific Literature | |
17. | ALA2185837 | Binding | Inhibition of PI3Kalpha in human PC3 cells assessed as reduction in pAKT level by immunoblotting method | Homo sapiens | 2 | ALA2177093 | cell-based format | Scientific Literature | |
18. | ALA2185839 | ADME | Efflux ratio of apparent permeability from basolateral to apical over apical to basolateral in mouse Bcrp1 transfected MDCK2 cells at 5 uM after 2 hrs by LC-MS/MS analysis | Canis lupus familiaris | 16 | ALA2177093 | cell-based format | Scientific Literature | |
19. | ALA2186306 | Binding | Inhibition of human recombinant mTOR (1360 to 2549 amino acids) assessed as reduction in phosphorylation of (GFP)-4-EBP1 after 30 mins by FRET assay | Homo sapiens | 5 | ALA2177093 | single protein format | Scientific Literature | |
20. | ALA2186307 | ADME | Clearance in po dosed CD-1 mouse | Mus musculus | 4 | ALA2177093 | organism-based format | Scientific Literature |