# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA4189777 | Binding | Displacement of fluorescein-labeled MLL4-43 from full length human menin expressed in Escherichia coli BL21 (DE3) cells after 3 hrs by fluorescence polarization assay | Homo sapiens | 29 | ALA4184328 | cell-based format | Scientific Literature | |
2. | ALA4189778 | Binding | Binding affinity to menin in mouse bone marrow cells harboring MLL-AF9 fusion protein assessed as inhibition of protein interaction with MLL by measuring cell growth inhibition after 7 days by MTT assay | Mus musculus | 29 | ALA4184328 | cell-based format | Scientific Literature | |
3. | ALA4189779 | ADME | Half life in CD-1 mouse liver microsomes at 1 uM after 3 to 60 mins by LC-MS/MS method | Mus musculus | 29 | ALA4184328 | microsome format | Scientific Literature | |
4. | ALA4189780 | Unassigned | Selectivity index, ratio of GI50 for mouse bone marrow cells transformed with control oncogenes Hoxa9/Meis1 to GI50 for binding affinity to menin in mouse bone marrow cells harboring MLL-AF9 fusion protein assessed as inhibition of protein interaction with MLL by measuring cell growth inhibition | Mus musculus | 3 | ALA4184328 | cell-based format | Scientific Literature | |
5. | ALA4189781 | Binding | Binding affinity to human C-terminal Avi-tagged menin expressed in Escherichia coli BL21 (DE3) cells by bio-layer interferometry | Homo sapiens | 2 | ALA4184328 | cell-based format | Scientific Literature | |
6. | ALA4189782 | ADME | Cytotoxicity against mouse bone marrow cells transformed with control oncogenes Hoxa9/Meis1 assessed as cell growth inhibition after 7 days by MTT assay | Mus musculus | 1 | ALA4184328 | cell-based format | Scientific Literature | |
7. | ALA4189783 | Functional | Cytotoxicity against human MV411 cells harboring MLL-AF4 fusion protein assessed as cell growth inhibition after 7 days by MTT assay | Homo sapiens | 2 | ALA4184328 | cell-based format | Scientific Literature | |
8. | ALA4189784 | Functional | Cytotoxicity against human MOLM13 cells harboring MLL-AF9 fusion protein assessed as cell growth inhibition after 7 days by MTT assay | Homo sapiens | 2 | ALA4184328 | cell-based format | Scientific Literature | |
9. | ALA4189785 | ADME | Cytotoxicity against human K562 cells assessed as cell growth inhibition after 7 days by MTT assay | Homo sapiens | 1 | ALA4184328 | cell-based format | Scientific Literature | |
10. | ALA4189786 | ADME | Cytotoxicity against human U937 cells assessed as cell growth inhibition after 7 days by MTT assay | Homo sapiens | 1 | ALA4184328 | cell-based format | Scientific Literature | |
11. | ALA4189787 | Binding | Binding affinity to menin in human MV411 cells assessed as inhibition of protein interaction with AF4-fused MLL by measuring downregulation of HOXA9 gene expression at 100 nM after 6 days by qRT-PCR method | Homo sapiens | 1 | ALA4184328 | cell-based format | Scientific Literature | |
12. | ALA4189788 | Binding | Binding affinity to menin in human MV411 cells assessed as inhibition of protein interaction with AF4-fused MLL by measuring downregulation of MEIS1 gene expression at 100 nM after 6 days by qRT-PCR method | Homo sapiens | 1 | ALA4184328 | cell-based format | Scientific Literature | |
13. | ALA4189789 | Binding | Binding affinity to menin in human MV411 cells assessed as inhibition of protein interaction with AF4-fused MLL by measuring downregulation of DLX2 gene expression at 100 nM after 6 days by qRT-PCR method | Homo sapiens | 1 | ALA4184328 | cell-based format | Scientific Literature | |
14. | ALA4189790 | Binding | Binding affinity to menin in human MV411 cells assessed as inhibition of protein interaction with AF4-fused MLL by measuring upregulation of ITGAM gene expression at 50 to 200 nM after 6 days by qRT-PCR method | Homo sapiens | 1 | ALA4184328 | cell-based format | Scientific Literature | |
15. | ALA4189791 | ADME | Oral bioavailability in C57BL/6 mouse at 30 mg/kg by LC-MS/MS method | Mus musculus | 1 | ALA4184328 | organism-based format | Scientific Literature | |
16. | ALA4189792 | Toxicity | Toxicity in NSG mouse xenografted with luciferase expressing human MV411 cells assessed as reduction in body weight at 80 mg/kg, ip administered for 21 consecutive days measured during compound dosing | Mus musculus | 1 | ALA4184328 | organism-based format | Scientific Literature | |
17. | ALA4189793 | Functional | In vivo inhibition of menin interaction with MLL in luciferase expressing human MV411 cells xenografted in NSG mouse at 80 mg/kg, ip administered for 21 consecutive days measured at days 7, 14, 21 during compound dosing by bioluminescence method relative to vehicle-treated control | Mus musculus | 1 | ALA4184328 | organism-based format | Scientific Literature | |
18. | ALA4189794 | Functional | Antileukemia activity against luciferase expressing human MV411 cells xenografted in NSG mouse assessed as reduction in spleen weight at 80 mg/kg, ip administered for 6 consecutive days | Homo sapiens | 1 | ALA4184328 | organism-based format | Scientific Literature | |
19. | ALA4189795 | Functional | Antileukemia activity against luciferase expressing human MV411 cells xenografted in NSG mouse assessed as reduction in spleen size at 80 mg/kg, ip administered for 6 consecutive days | Homo sapiens | 1 | ALA4184328 | organism-based format | Scientific Literature | |
20. | ALA4189796 | Functional | Antileukemia activity against luciferase expressing human MV411 cells xenografted in NSG mouse assessed as levels of human CD45positive cells at 80 mg/kg, ip administered for 6 consecutive days by flow cytometric method (Rvb = 75%) | Homo sapiens | 1 | ALA4184328 | organism-based format | Scientific Literature |