# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA4353688 | Binding | Inhibition of N-terminal His-tagged recombinant human KDM4A (1 to 359 residues) expressed in Escherichia coli assessed as decrease in demethylation of substrate using peptide (ARTKQTARK(Me3)STGGKAPRKQLA-GGKbiotin) as substrate and 2OG as cosubstrate pre-incubated for 10 mins before substrate addition followed by centrifugation for 1 min and measured after 20 mins by AlphaScreen assay | Homo sapiens | 33 | ALA4350996 | assay format | Scientific Literature | |
2. | ALA4353689 | Binding | Inhibition of N-terminal GST-tagged recombinant human KDM4B (1 to 500 residues) expressed in baculovirus infected Sf9 insect cells assessed as decrease in demethylation of substrate using peptide (ARTKQTARK(Me3)STGGKAPRKQLA-GGKbiotin) as substrate and 2OG as cosubstrate pre-incubated for 10 mins before substrate addition followed by centrifugation for 1 min and measured after 20 mins by AlphaScreen assay | Homo sapiens | 33 | ALA4350996 | cell-based format | Scientific Literature | |
3. | ALA4353690 | Binding | Inhibition of KDM5B (unknown origin) assessed as decrease in demethylation of substrate using peptide (H3(1-21)K4-Me3-GGKBiotin) as substrate and 2OG as cosubstrate pre-incubated for 15 mins before substrate addition followed by centrifugation for 15 secs and measured after 20 mins by Alphascreen assay | Homo sapiens | 33 | ALA4350996 | single protein format | Scientific Literature | |
4. | ALA4353691 | Binding | Inhibition of KDM5C (unknown origin) assessed as decrease in demethylation of substrate using peptide (H3(1-21)K4-Me3-GGKBiotin) as substrate and 2OG as cosubstrate pre-incubated for 15 mins before substrate addition followed by centrifugation for 15 secs and measured after 20 mins by Alphascreen assay | Homo sapiens | 33 | ALA4350996 | single protein format | Scientific Literature | |
5. | ALA4353692 | Binding | Inhibition of KDM2A (unknown origin) by Alphascreen assay | Homo sapiens | 6 | ALA4350996 | single protein format | Scientific Literature | |
6. | ALA4353693 | Binding | Inhibition of KDM3A (unknown origin) by Alphascreen assay | Homo sapiens | 6 | ALA4350996 | single protein format | Scientific Literature | |
7. | ALA4353694 | Binding | Inhibition of KDM6B (unknown origin) by Alphascreen assay | Homo sapiens | 5 | ALA4350996 | single protein format | Scientific Literature | |
8. | ALA4353730 | Binding | Binding affinity to KDM4A (unknown origin) | Homo sapiens | 8 | ALA4350996 | single protein format | Scientific Literature | |
9. | ALA4353731 | Binding | Binding affinity to KDM5B (unknown origin) | Homo sapiens | 8 | ALA4350996 | single protein format | Scientific Literature | |
10. | ALA4353732 | ADME | Apparent permeability of the compound in human Caco2 cells from apical to basolateral side at 10 uM after 2 hr by LC/MS/MS analysis | Homo sapiens | 33 | ALA4350996 | cell-based format | Scientific Literature | |
11. | ALA4353733 | Binding | Binding affinity to recombinant human N-terminal KDM4B (1 to 348 residues) fused upstream with E31G-R71G-K105E/ePL-tagged C-terminal transfected in HEK293T cells measured after 30 mins by chemiluminescence based cellular target engagement assay | Homo sapiens | 8 | ALA4350996 | cell-based format | Scientific Literature | |
12. | ALA4353734 | Binding | Binding affinity to recombinant human N-terminal KDM5B (26 to 772 residues) fused with ePL-tagged C-terminal transfected in HEK293T cells measured after 30 mins by chemiluminescence based cellular target engagement assay | Homo sapiens | 8 | ALA4350996 | cell-based format | Scientific Literature | |
13. | ALA4353735 | Binding | Inhibition of FLAG tagged full length wild type human KDM4A transfected in HeLa cells assessed as decrease in demethylation of H3K9Me3 measured after 24 hrs by cell analyser based immunofluorescence assay | Homo sapiens | 7 | ALA4350996 | cell-based format | Scientific Literature | |
14. | ALA4353737 | Binding | Inhibition of full length human wild type KDM5B transfected in HeLa cells assessed as decrease in demethylation of H3K4Me3 measured after 24 hrs by cell analyser based immunofluorescence assay | Homo sapiens | 8 | ALA4350996 | cell-based format | Scientific Literature |