Assay Detail
Binding
CHEMBL2390550
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant JAK1 (unknown origin) using Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins in presence of ATP
34
Total Activities
34
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
Identification of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 34 | 8.45 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386635 | — | — | 1 | 10.00 |
| CHEMBL2386636 | — | — | 1 | 9.52 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.15 |
| CHEMBL2386640 | — | — | 1 | 9.10 |
| CHEMBL2386629 | — | — | 1 | 9.10 |
| CHEMBL2386634 | — | — | 1 | 9.05 |
| CHEMBL2386637 | — | — | 1 | 8.96 |
| CHEMBL2386630 | — | — | 1 | 8.96 |
| CHEMBL2386632 | — | — | 1 | 8.92 |
| CHEMBL2159198 | — | — | 1 | 8.89 |
| CHEMBL2386645 | — | — | 1 | 8.80 |
| CHEMBL2386643 | — | — | 1 | 8.74 |
| CHEMBL2386633 | — | — | 1 | 8.72 |
| CHEMBL2386648 | — | — | 1 | 8.70 |
| CHEMBL2385096 | — | — | 1 | 8.70 |
| CHEMBL2386646 | — | — | 1 | 8.59 |
| CHEMBL2386627 | — | — | 1 | 8.57 |
| CHEMBL2386653 | — | — | 1 | 8.55 |
| CHEMBL2386647 | — | — | 1 | 8.47 |
| CHEMBL2386638 | — | — | 1 | 8.46 |
| CHEMBL2386628 | — | — | 1 | 8.31 |
| CHEMBL2386649 | — | — | 1 | 8.28 |
| CHEMBL2386625 | — | — | 1 | 8.27 |
| CHEMBL2386644 | — | — | 1 | 8.14 |
| CHEMBL2159141 | — | — | 1 | 8.00 |
| CHEMBL2386639 | — | — | 1 | 8.00 |
| CHEMBL2386626 | — | — | 1 | 7.92 |
| CHEMBL2386641 | — | — | 1 | 7.89 |
| CHEMBL2386642 | — | — | 1 | 7.80 |
| CHEMBL2386651 | — | — | 1 | 7.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386635 | — | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2386636 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL221959 | TOFACITINIB | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2386640 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2386629 | — | Ki | = | 0.8 | nM | 9.10 |
| CHEMBL2386634 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL2386637 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2386630 | — | Ki | = | 1.1 | nM | 8.96 |
| CHEMBL2386632 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2159198 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2386645 | — | Ki | = | 1.6 | nM | 8.80 |
| CHEMBL2386643 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2386633 | — | Ki | = | 1.9 | nM | 8.72 |
| CHEMBL2386648 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2385096 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2386646 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2386627 | — | Ki | = | 2.7 | nM | 8.57 |
| CHEMBL2386653 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL2386647 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL2386638 | — | Ki | = | 3.5 | nM | 8.46 |
| CHEMBL2386628 | — | Ki | = | 4.9 | nM | 8.31 |
| CHEMBL2386649 | — | Ki | = | 5.2 | nM | 8.28 |
| CHEMBL2386625 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2386644 | — | Ki | = | 7.2 | nM | 8.14 |
| CHEMBL2159141 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2386639 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2386626 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2386641 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2386642 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2386651 | — | Ki | = | 31.0 | nM | 7.51 |
| CHEMBL2386650 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL2152306 | — | Ki | = | 46.0 | nM | 7.34 |
| CHEMBL2386631 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL2386652 | — | Ki | = | 68.0 | nM | 7.17 |