Assay Detail
Binding
CHEMBL4713240
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant JAK2 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr followed by anti-pSTAT1 antibody addition and measured after 30 mins by Lanthascreen TR-FRET assay
44
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery and Biological Evaluation of N-Methyl-pyrrolo[2,3-b]pyridine-5-carboxamide Derivatives as JAK1-Selective Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 44 | 6.93 | 8.53 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4783938 | — | — | 1 | 8.53 |
| CHEMBL4761365 | — | — | 2 | 8.43 |
| CHEMBL4787133 | — | — | 1 | 8.36 |
| CHEMBL4744772 | — | — | 1 | 8.35 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.30 |
| CHEMBL4779060 | — | — | 1 | 8.05 |
| CHEMBL4747742 | — | — | 1 | 7.96 |
| CHEMBL4777200 | — | — | 1 | 7.55 |
| CHEMBL4755612 | — | — | 1 | 7.55 |
| CHEMBL4789693 | — | — | 1 | 7.54 |
| CHEMBL4781706 | — | — | 1 | 7.35 |
| CHEMBL4759666 | — | — | 1 | 7.24 |
| CHEMBL4787731 | — | — | 1 | 7.24 |
| CHEMBL4779340 | — | — | 1 | 7.20 |
| CHEMBL3593765 | — | — | 1 | 7.08 |
| CHEMBL4785910 | — | — | 1 | 7.06 |
| CHEMBL4750779 | — | — | 1 | 7.05 |
| CHEMBL4795901 | — | — | 1 | 7.05 |
| CHEMBL4761631 | — | — | 1 | 7.05 |
| CHEMBL4785998 | — | — | 1 | 7.03 |
| CHEMBL4759320 | — | — | 1 | 6.82 |
| CHEMBL4747285 | — | — | 1 | 6.82 |
| CHEMBL4786466 | — | — | 1 | 6.79 |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | 6.77 |
| CHEMBL4741376 | — | — | 1 | 6.76 |
| CHEMBL4744048 | — | — | 1 | 6.75 |
| CHEMBL4750665 | — | — | 1 | 6.63 |
| CHEMBL4777577 | — | — | 1 | 6.61 |
| CHEMBL4742766 | — | — | 1 | 6.50 |
| CHEMBL4763801 | — | — | 1 | 6.33 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4783938 | — | IC50 | = | 2.94 | nM | 8.53 |
| CHEMBL4761365 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4787133 | — | IC50 | = | 4.34 | nM | 8.36 |
| CHEMBL4744772 | — | IC50 | = | 4.46 | nM | 8.35 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 4.98 | nM | 8.30 |
| CHEMBL4779060 | — | IC50 | = | 8.83 | nM | 8.05 |
| CHEMBL4747742 | — | IC50 | = | 10.9 | nM | 7.96 |
| CHEMBL4755612 | — | IC50 | = | 28.4 | nM | 7.55 |
| CHEMBL4777200 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4789693 | — | IC50 | = | 28.5 | nM | 7.54 |
| CHEMBL4781706 | — | IC50 | = | 44.3 | nM | 7.35 |
| CHEMBL4759666 | — | IC50 | = | 57.7 | nM | 7.24 |
| CHEMBL4787731 | — | IC50 | = | 57.6 | nM | 7.24 |
| CHEMBL4779340 | — | IC50 | = | 63.2 | nM | 7.20 |
| CHEMBL3593765 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4785910 | — | IC50 | = | 86.6 | nM | 7.06 |
| CHEMBL4795901 | — | IC50 | = | 89.9 | nM | 7.05 |
| CHEMBL4750779 | — | IC50 | = | 88.5 | nM | 7.05 |
| CHEMBL4761631 | — | IC50 | = | 89.3 | nM | 7.05 |
| CHEMBL4785998 | — | IC50 | = | 93.8 | nM | 7.03 |
| CHEMBL4747285 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL4759320 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL4786466 | — | IC50 | = | 162.0 | nM | 6.79 |
| CHEMBL3301607 | FILGOTINIB | IC50 | = | 171.0 | nM | 6.77 |
| CHEMBL4741376 | — | IC50 | = | 175.0 | nM | 6.76 |
| CHEMBL4744048 | — | IC50 | = | 179.0 | nM | 6.75 |
| CHEMBL4750665 | — | IC50 | = | 232.0 | nM | 6.63 |
| CHEMBL4777577 | — | IC50 | = | 245.0 | nM | 6.61 |
| CHEMBL4742766 | — | IC50 | = | 319.0 | nM | 6.50 |
| CHEMBL4763801 | — | IC50 | = | 469.0 | nM | 6.33 |
| CHEMBL4742822 | — | IC50 | = | 503.8 | nM | 6.30 |
| CHEMBL4750605 | — | IC50 | = | 514.0 | nM | 6.29 |
| CHEMBL4761365 | — | IC50 | = | 625.0 | nM | 6.20 |
| CHEMBL4747270 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL4746952 | — | IC50 | = | 712.0 | nM | 6.15 |
| CHEMBL4781679 | — | IC50 | = | 759.0 | nM | 6.12 |
| CHEMBL4746186 | — | IC50 | = | 817.0 | nM | 6.09 |
| CHEMBL4749677 | — | IC50 | = | 1080.0 | nM | 5.97 |
| CHEMBL4787974 | — | IC50 | = | 2590.0 | nM | 5.59 |
| CHEMBL4763821 | — | IC50 | = | 3540.0 | nM | 5.45 |
| CHEMBL4756788 | — | IC50 | = | 7060.0 | nM | 5.15 |
| CHEMBL4784576 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4792719 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4787224 | — | IC50 | > | 10000.0 | nM | - |