| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3706078 | B | In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498). Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series to generate a 10-point curve. | 1 | cell-based format | BindingDB Database | |||
| 2. | ALA3706135 | B | ADP-Glo Kinase Assay: In this assay, the inhibitory activity of a test substance against the tyrosine kinase activity of FGFR1 protein is measured.To each well of a flat bottom 96 well white plate (Sumitomo Bakelite Co., Ltd., MS-8496W), 10 ul of FGFR1 protein (Cama Biosciences, Inc., 08-133) solution diluted to 1 ug/mL with an assay buffer (20 mM HEPES NaOH, 0.01% Triton X-100, 2 mM DTT, and 5 mM MgCl2), 10 ul, of an assay buffer solution containing CSK-tide substrate (Ana Spec Inc., 63843) in a final concentration of 1000 nM and ATP (Promega Corporation, V9102) in a final concentration of 58.3 uM, and 5 ul of a test substance diluted with the assay buffer were added, and the reaction was performed at room temperature for 1 hour (kinase reaction). For measuring kinase activity, ADP-Glo Kinase Assay (Promega Corporation, V9102) was used. After the reaction, 25 uL of ADP-Glo reagent was added to each well of the plate, and the reaction was performed at morn temperature for 40 minutes. | Homo sapiens | 128 | single protein format | BindingDB Database | ||
| 3. | ALA3707869 | B | In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498). Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series to generate a 10-point curve. | Homo sapiens | 1 | cell-based format | BindingDB Database | ||
| 4. | ALA3707870 | B | In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498). Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series to generate a 10-point curve. | Homo sapiens | 1 | cell-based format | BindingDB Database | ||
| 5. | ALA3707913 | B | In Vitro Binding Assay: hEP1 and hEP4 membranes are prepared from recombinant HEK293 cells stably expressing human EP1 (Genbank accession number AY275470) or EP4 (Genbank accession number AY429109) receptors. hEP2 and hEP3 membranes are prepared from HEK293 cells transiently transfected with EP2 (Genbank accession number AY275471) or EP3 (isoform VI: Genbank accession number AY429108) receptor plasmids. Frozen cell pellets are homogenized in homogenization buffer using a Teflon/glass homogenizer. Membrane protein is aliquoted and quick frozen on dry ice prior to storage at -80 C. Homogenization buffer contained 10 mM Tris-HCl, pH 7.4, 250 mM sucrose, 1 mM EDTA, 0.3 mM indomethacin and plus Complete, with EDTA, obtained from Roche Molecular Biochemicals (Catalog Number 1 697 498). Kd values for [3H]-PGE2 binding to each receptor are determined by saturation binding studies or homologous competition. Compounds are tested in a 96-well format using a three-fold dilution series to generate a 10-point curve. | 1 | cell-based format | BindingDB Database | |||
| 6. | ALA3796825 | P | Aqueous solubility of compound at pH 6 at 2 mM after 20 hrs by HPLC | 5 | small-molecule physicochemical format | Scientific Literature | |||
| 7. | ALA3796826 | A | Clearance in rat at 1 mg/kg, iv | Rattus norvegicus | 2 | organism-based format | Scientific Literature | ||
| 8. | ALA3796827 | A | AUC in rat at 5 mg/kg, po | Rattus norvegicus | 2 | organism-based format | Scientific Literature | ||
| 9. | ALA3796828 | A | Cmax in rat at 5 mg/kg, po | Rattus norvegicus | 2 | organism-based format | Scientific Literature | ||
| 10. | ALA3796829 | A | Half life in rat at 5 mg/kg, po | Rattus norvegicus | 2 | organism-based format | Scientific Literature | ||
| 11. | ALA3796830 | A | Oral bioavailability in rat at 5 mg/kg | Rattus norvegicus | 2 | organism-based format | Scientific Literature | ||
| 12. | ALA3796831 | A | Volume of distribution at steady state in rat at 1 mg/kg, iv or 5 mg/kg, po | Rattus norvegicus | 1 | organism-based format | Scientific Literature | ||
| 13. | ALA3796832 | A | AUC in dog at 5 mg/kg, po | Canis lupus familiaris | 1 | organism-based format | Scientific Literature | ||
| 14. | ALA3796833 | A | Cmax in dog at 5 mg/kg, po | Canis lupus familiaris | 1 | organism-based format | Scientific Literature | ||
| 15. | ALA3796834 | A | Half life in dog at 5 mg/kg, po | Canis lupus familiaris | 1 | organism-based format | Scientific Literature | ||
| 16. | ALA3796835 | A | Clearance in dog at 1 mg/kg, iv | Canis lupus familiaris | 1 | organism-based format | Scientific Literature | ||
| 17. | ALA3796836 | A | Volume of distribution at steady state in dog at 1 mg/kg, iv or 5 mg/kg, po | Canis lupus familiaris | 1 | organism-based format | Scientific Literature | ||
| 18. | ALA3796837 | A | Oral bioavailability in dog at 5 mg/kg | Canis lupus familiaris | 1 | organism-based format | Scientific Literature | ||
| 19. | ALA3795702 | A | Inhibition of CYP1A2 (unknown origin) | Homo sapiens | 1 | single protein format | Scientific Literature | ||
| 20. | ALA3795703 | A | Inhibition of CYP2B6 (unknown origin) | Homo sapiens | 1 | single protein format | Scientific Literature |
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