# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA2384327 | B | Ratio of IWR1 EC50 to compound EC50 for tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method | Homo sapiens | 2 | cell-based format | Scientific Literature | ||
2. | ALA2384331 | F | Unbound Cmax in po dosed CD-1 mouse to EC50 for tankyrase in human SW480 cells | 3 | organism-based format | Scientific Literature | |||
3. | ALA2384332 | B | Activation of rat PXR at 10 uM relative to control | Rattus norvegicus | 3 | single protein format | Scientific Literature | ||
4. | ALA2384333 | A | Inhibition of CYP3A4 (unknown origin) | Homo sapiens | 3 | single protein format | Scientific Literature | ||
5. | ALA2384334 | B | Inhibition of tankyrase in human SW480 cells assessed as accumulation of Axin2 after 24 hrs by Hoechst dye-based method in presence of FBA | Homo sapiens | 3 | cell-based format | Scientific Literature | ||
6. | ALA2384339 | A | AUCt in CD-1 mouse at 30 mg/kg, po | Mus musculus | 16 | organism-based format | Scientific Literature | ||
7. | ALA2384340 | A | Cmax in CD-1 mouse at 30 mg/kg, po | Mus musculus | 16 | organism-based format | Scientific Literature | ||
8. | ALA2384341 | A | Plasma protein binding in mouse | Mus musculus | 8 | cell-free format | Scientific Literature | ||
9. | ALA2384345 | P | Solubility of the compound in PBS at pH 7.4 | 8 | small-molecule physicochemical format | Scientific Literature | |||
10. | ALA2384346 | P | Solubility of the compound in 0.01N HCl | 8 | small-molecule physicochemical format | Scientific Literature | |||
11. | ALA2384347 | P | Solubility of the compound in simulated intestinal fluid at pH 6.8 | 8 | small-molecule physicochemical format | Scientific Literature | |||
12. | ALA2384480 | A | Intrinsic clearance in rat liver microsomes | Rattus norvegicus | 30 | microsome format | Scientific Literature | ||
13. | ALA2384481 | A | Intrinsic clearance in human liver microsomes | Homo sapiens | 30 | microsome format | Scientific Literature | ||
14. | ALA2384482 | B | Inhibition of tankyrase in human SW480 cells assessed as degradation of beta catenin after 40 to 48 hrs | Homo sapiens | 31 | cell-based format | Scientific Literature | ||
15. | ALA2384483 | B | Inhibition of tankyrase in human SW480 cells assessed as accumulation of axin2 after 24 hrs by Hoechst dye-based method | Homo sapiens | 30 | cell-based format | Scientific Literature | ||
16. | ALA2384484 | B | Inhibition of PARP2 (unknown origin) using histone as substrate after 1 hr by luminescence assay | Homo sapiens | 5 | single protein format | Scientific Literature | ||
17. | ALA2384485 | B | Inhibition of PARP1 (unknown origin) using histone as substrate after 1 hr by luminescence assay | Homo sapiens | 5 | single protein format | Scientific Literature | ||
18. | ALA2384487 | B | Inhibition of 6XHis-tagged tankyrase1 (1091 to 1325) (unknown origin) after 60 mins in presence of NAD | Homo sapiens | 32 | single protein format | Scientific Literature | ||
19. | ALA3888461 | B | Tankyrase Biochemical Assays: The tankyrase 1 biochemical activity of the compounds was assayed in the following assay buffer (50 mM MOPS pH7.5, 100 mM NaCl, 2.5 mM MgCl2, 0.01% Tween-20, 0.05% BSA, and 1 mM DTT) as follows: 0.25 nM of 6×HIS-tankyrase 1 (1091-1325) was incubated in the presence of compound (DMSO 1.85% final) in a Perkin Elmer 384 well Proxiplate Plus™ (cat. no. 6008289) with 400 nM of NAD for 60 minutes at room temperature. The assay was then stopped with the above assay buffer containing a 0.6 M inhibitor and the following detection components: 0.05 g/mL monoclonal anti-PAR antibody (Trevigen cat. no. 4335-MC-01K-AC) prebound for 60 minutes with 0.63 μg/mL protein G AlphaLisa® acceptor bead (Perkin Elmer cat. no. AL102M) and 5 μg/mL AlphaLisa® nickel chelate donor bead (Perkin Elmer cat. no. AS101M). The assay was incubated for 16 hours at room temperature in the dark and read on a Perkin Elmer Envision® multi label reader using the default program set with laser excitation at 680 nM and emission at 615 nM. The tankyrase 2 biochemical assay was performed using the procedure set forth above with respect to tankyrase 1 except that 4 nM 6×HIS-tankyrase 2 (946-1162) and 250 nM NAD were used. | 175 | single protein format | BindingDB Database |