# | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
---|---|---|---|---|---|---|---|---|---|
1. | ALA4015867 | Binding | Inhibition of human TMEM16A expressed in FRT cells co-expressing iodide sensitive fluorescent protein YFP-H148Q/I152L/F46L assessed as reduction in ATP-induced Ca2+ activation-mediated chloride current by measuring decrease in iodide influx preincubated for 10 mins followed by ATP/iodide addition by fluorescence assay | Homo sapiens | 50 | ALA4014325 | cell-based format | Scientific Literature | |
2. | ALA4015868 | Binding | Inhibition of human TMEM16A expressed in FRT cells assessed as reduction of ATP-induced in chloride conductance preincubated for 5 mins followed by ATP addition by short-circuit current assay | Homo sapiens | 9 | ALA4014325 | cell-based format | Scientific Literature | |
3. | ALA4015869 | Binding | Inhibition of human TMEM16B expressed in FRT cells co-expressing iodide sensitive fluorescent protein YFP-H148Q/I152L/F46L assessed as reduction in ATP-induced Ca2+ activation-mediated chloride current by measuring decrease in iodide influx preincubated for 10 mins followed by ATP/iodide addition by fluorescence assay | Homo sapiens | 8 | ALA4014325 | cell-based format | Scientific Literature | |
4. | ALA4015871 | ADME | Cytotoxicity against human HT-29 cells assessed as cell survival at 5 uM after 8 hrs by alamar blue assay relative to control | Homo sapiens | 9 | ALA4014325 | cell-based format | Scientific Literature | |
5. | ALA4015872 | Binding | Inhibition of human wild type CFTR expressed in FRT cells co-expressing halide sensitive YFP-H148Q assessed as reduction in forskolin induced cAMP activated chloride conductance by measuring decrease in iodide influx after 15 mins by fluorescence assay | Homo sapiens | 9 | ALA4014325 | cell-based format | Scientific Literature | |
6. | ALA4015874 | Binding | Inhibition of calcium activated chloride channel in ATP-activated human HT-29 cells expressing YFP-H148Q/152L assessed as reduction in iodide influx preincubated for 10 mins followed by ATP addition by fluorescence assay | Homo sapiens | 9 | ALA4014325 | assay format | Scientific Literature | |
7. | ALA4015875 | Binding | Inhibition of human TMEM16A expressed in FRT cells assessed as reduction in Ca2+ activated chloride current at 250 nM at -60 mV holding potential by inside-out patch-clamp method | Homo sapiens | 1 | ALA4014325 | cell-based format | Scientific Literature | |
8. | ALA4015876 | Binding | Reversible inhibition of human TMEM16A expressed in FRT cells assessed as recovery of Ca2+ activated chloride current at 250 nM preincubated with cells followed by compound washout at -60 mV holding potential by inside-out patch-clamp method | Homo sapiens | 1 | ALA4014325 | cell-based format | Scientific Literature | |
9. | ALA4015877 | Binding | Inhibition of human TMEM16A expressed in FRT cells assessed as reduction in ionomycin activated chloride conductance at 1 uM preincubated for 5 mins followed by ionomycin addition by short-circuit current assay | Homo sapiens | 1 | ALA4014325 | cell-based format | Scientific Literature | |
10. | ALA4015879 | Binding | Inhibition of human TMEM16A expressed in FRT cells assessed as alteration of ATP stimulated cytoplasmic calcium elevation at 1 uM preincubated for 3 mins followed by ATP addition by Fluo-4 fluorescence assay | Homo sapiens | 1 | ALA4014325 | cell-based format | Scientific Literature | |
11. | ALA4015880 | ADME | Metabolic stability in rat liver microsomes assessed as compound remaining in presence of NADPH at 10 uM after 180 mins by LC/MS analysis | Rattus norvegicus | 1 | ALA4014325 | assay format | Scientific Literature | |
12. | ALA4015881 | Physicochemical | Kinetic aqueous solubility of compound in PBS by titration method | 1 | ALA4014325 | small-molecule physicochemical format | Scientific Literature | ||
13. | ALA4015882 | Binding | Inhibition of TMEM16A in CD1 mouse ileum assessed as reduction in intestinal smooth muscle contraction | Mus musculus | 1 | ALA4014325 | assay format | Scientific Literature | |
14. | ALA4015883 | Physicochemical | Stability of compound in aqueous solution at 100 uM after 1 day by ESI-LCMS analysis | 1 | ALA4014325 | small-molecule physicochemical format | Scientific Literature | ||
15. | ALA4015884 | Physicochemical | Stability of compound in aqueous solution at 100 uM after 2 days by ESI-LCMS analysis | 1 | ALA4014325 | small-molecule physicochemical format | Scientific Literature | ||
16. | ALA4015885 | Physicochemical | Drug metabolism in aqueous solution assessed as 2-oxo-2-(3-(o-tolylcarbamoyl)-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophen-2-ylamino)acetyl fluoride formation after 3 days by ESI-LCMS analysis | 1 | ALA4014325 | small-molecule physicochemical format | Scientific Literature | ||
17. | ALA4015886 | Physicochemical | Drug metabolism in aqueous solution assessed as 2-(2,2-difluoro-2-hydroxyacetamido)-N-o-tolyl-5,6,7,8-tetrahydro-4H-cyclohepta[b]thiophene-3-carboxamide formation after 3 days by ESI-LCMS analysis | 1 | ALA4014325 | small-molecule physicochemical format | Scientific Literature | ||
18. | ALA4015889 | Binding | Selectivity ratio of IC50 for human TMEM16B expressed in FRT cells co-expressing iodide sensitive fluorescent protein YFP-H148Q/I152L/F46L to IC50 for human TMEM16A expressed in FRT cells co-expressing iodide sensitive fluorescent protein YFP-H148Q/I152L/F46L | Homo sapiens | 2 | ALA4014325 | cell-based format | Scientific Literature | |
19. | ALA4015890 | Binding | Inhibition of human TMEM16A expressed in FRT cells assessed as reduction in carbachol activated chloride conductance at 1 uM preincubated for 5 mins followed by carbachol addition by short-circuit current assay | Homo sapiens | 1 | ALA4014325 | cell-based format | Scientific Literature | |
20. | ALA4015891 | Physicochemical | Stability of compound in DMSO | 1 | ALA4014325 | small-molecule physicochemical format | Scientific Literature |