| # | Aladdin ID | Assay Type | Description | Organism | Compounds | Reference | BAO Format | Source | |
|---|---|---|---|---|---|---|---|---|---|
| 1. | ALA3705503 | B | Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4. | Homo sapiens | 42 | single protein format | BindingDB Database | ||
| 2. | ALA3707926 | B | Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4. | Homo sapiens | 42 | single protein format | BindingDB Database | ||
| 3. | ALA3707947 | B | Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4. | Homo sapiens | 42 | single protein format | BindingDB Database | ||
| 4. | ALA3707974 | B | Enzyme Assay: Test article and assay controls were added to a 384-well plate. Reaction mixtures contained 20 mM HEPES, pH 7.4, 10 mM magnesium chloride, 0.01% bovine serum albumin (BSA), 0.0005% Tween 20, 1 mM ATP and 1 μM peptide substrate. The JAK1 and TYK2 assays contained 1 μM of the IRStide peptide (5FAMKKSRGDYMTMQID) and the JAK2 and JAK3 assays contained 1 μM of the JAKtide peptide (FITC-KGGEEEEYFELVKK). The assays were initiated by the addition of 20 nM JAK1, 1 nM JAK2, 1 nM JAK3 or 1 nM TYK2 enzyme and were incubated at room temperature for three hours for JAK1, 60 minutes for JAK2, 75 minutes for JAK3 or 135 minutes for TYK2. Enzyme concentrations and incubation times were optimized for each new enzyme preps and were modified slightly over time to ensure 20%-30% phosphorylation. The assays were stopped with a final concentration of 10 mM EDTA, 0.1% Coating Reagent and 100 mM HEPES, pH=7.4. | Homo sapiens | 42 | single protein format | BindingDB Database | ||
| 5. | ALA4022969 | B | Inhibition of recombinant human JAK1 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assay | Homo sapiens | 43 | single protein format | Scientific Literature | ||
| 6. | ALA4022970 | A | Inhibition of recombinant human JAK2 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay | Homo sapiens | 43 | single protein format | Scientific Literature | ||
| 7. | ALA4022971 | U | Selectivity ratio of IC50 for recombinant human JAK2 to IC50 for recombinant human JAK1 in presence of 1 mM ATP | Homo sapiens | 43 | assay format | Scientific Literature | ||
| 8. | ALA4022972 | B | Inhibition of JAK1/TYK2 in human whole blood assessed as reduction in IFNalpha induced STAT3 phosphorylation preincubated for 45 mins followed by IFNalpha addition measured after 15 mins by flow cytometric analysis | Homo sapiens | 43 | protein complex format | Scientific Literature | ||
| 9. | ALA4022973 | A | Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis | Homo sapiens | 43 | single protein format | Scientific Literature | ||
| 10. | ALA4022974 | A | Apparent intrinsic clearance in human liver microsomes at 1 uM | Homo sapiens | 43 | assay format | Scientific Literature | ||
| 11. | ALA4022975 | P | Octanol/water phosphate buffer partition coefficient, log D of compound at pH 7.4 | 43 | small-molecule physicochemical format | Scientific Literature | |||
| 12. | ALA4022976 | B | Inhibition of recombinant human JAK3 using FITC-KGGEEEEYFELVKK as substrate in presence of 1 mM ATP by mobility shift assay | Homo sapiens | 43 | single protein format | Scientific Literature | ||
| 13. | ALA4022977 | B | Inhibition of recombinant human TYK2 using 5'FAM-KKSRGDYMTMQID as substrate in presence of 1 mM ATP by mobility shift assay | Homo sapiens | 43 | single protein format | Scientific Literature | ||
| 14. | ALA4022978 | A | Clearance in rat at 1 mg/kg, iv or 3 mg/kg, po | Rattus norvegicus | 4 | organism-based format | Scientific Literature | ||
| 15. | ALA4022979 | A | Volume of distribution at steady state in rat at 1 mg/kg, iv or 3 mg/kg, po | Rattus norvegicus | 4 | organism-based format | Scientific Literature | ||
| 16. | ALA4022980 | A | Half life in rat at 1 mg/kg, iv or 3 mg/kg, po | Rattus norvegicus | 4 | organism-based format | Scientific Literature | ||
| 17. | ALA4022981 | A | Oral bioavailability in rat at 3 mg/kg | Rattus norvegicus | 4 | organism-based format | Scientific Literature | ||
| 18. | ALA4022982 | P | Aqueous solubility of the compound at pH 7.4 | 4 | small-molecule physicochemical format | Scientific Literature | |||
| 19. | ALA4022983 | A | Apparent permeability in RRCK cells from apical to basolateral side | Canis lupus familiaris | 4 | cell-based format | Scientific Literature | ||
| 20. | ALA4022984 | B | Inhibition of recombinant human JAK3 using FITC-KGGEEEEYFELVKK as substrate in presence of 4 uM ATP by mobility shift assay | Homo sapiens | 1 | single protein format | Scientific Literature |
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