Assay Detail
Binding
CHEMBL2214837
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Inhibition of JAK1 kinase domain assessed as phosphorylation of N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr after 30 mins
38
Total Activities
35
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Structure-based discovery of C-2 substituted imidazo-pyrrolopyridine JAK1 inhibitors with improved selectivity over JAK2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 38 | 8.29 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2206059 | — | — | 1 | 9.70 |
| CHEMBL2206638 | — | — | 2 | 9.52 |
| CHEMBL2152401 | — | — | 1 | 9.22 |
| CHEMBL2206639 | — | — | 1 | 9.22 |
| CHEMBL2206624 | — | — | 1 | 8.77 |
| CHEMBL2206634 | — | — | 1 | 8.68 |
| CHEMBL2206629 | — | — | 2 | 8.68 |
| CHEMBL2206633 | — | — | 1 | 8.59 |
| CHEMBL2206632 | — | — | 1 | 8.59 |
| CHEMBL2206061 | — | — | 1 | 8.54 |
| CHEMBL2206637 | — | — | 1 | 8.52 |
| CHEMBL2206636 | — | — | 1 | 8.48 |
| CHEMBL2206623 | — | — | 1 | 8.43 |
| CHEMBL2206058 | — | — | 1 | 8.42 |
| CHEMBL2206628 | — | — | 1 | 8.38 |
| CHEMBL2206611 | — | — | 1 | 8.37 |
| CHEMBL2206060 | — | — | 1 | 8.34 |
| CHEMBL2206626 | — | — | 1 | 8.30 |
| CHEMBL2206635 | — | — | 1 | 8.28 |
| CHEMBL2206622 | — | — | 1 | 8.27 |
| CHEMBL2206627 | — | — | 2 | 8.24 |
| CHEMBL2206621 | — | — | 1 | 8.14 |
| CHEMBL2206620 | — | — | 1 | 8.08 |
| CHEMBL2206614 | — | — | 1 | 8.06 |
| CHEMBL2206062 | — | — | 1 | 8.04 |
| CHEMBL2206616 | — | — | 1 | 8.03 |
| CHEMBL2206631 | — | — | 1 | 8.00 |
| CHEMBL2206625 | — | — | 1 | 7.92 |
| CHEMBL2206618 | — | — | 1 | 7.89 |
| CHEMBL2206617 | — | — | 1 | 7.85 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2206059 | — | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2206638 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL2206639 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2152401 | — | Ki | = | 0.6 | nM | 9.22 |
| CHEMBL2206624 | — | Ki | = | 1.7 | nM | 8.77 |
| CHEMBL2206634 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2206629 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2206633 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2206632 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2206061 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2206637 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL2206638 | — | Ki | = | 3.2 | nM | 8.49 |
| CHEMBL2206636 | — | Ki | = | 3.3 | nM | 8.48 |
| CHEMBL2206623 | — | Ki | = | 3.7 | nM | 8.43 |
| CHEMBL2206058 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL2206628 | — | Ki | = | 4.2 | nM | 8.38 |
| CHEMBL2206611 | — | Ki | = | 4.3 | nM | 8.37 |
| CHEMBL2206060 | — | Ki | = | 4.6 | nM | 8.34 |
| CHEMBL2206626 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2206635 | — | Ki | = | 5.3 | nM | 8.28 |
| CHEMBL2206622 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2206627 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL2206621 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL2206620 | — | Ki | = | 8.4 | nM | 8.08 |
| CHEMBL2206614 | — | Ki | = | 8.7 | nM | 8.06 |
| CHEMBL2206062 | — | Ki | = | 9.1 | nM | 8.04 |
| CHEMBL2206616 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL2206631 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2206625 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2206618 | — | Ki | = | 13.0 | nM | 7.89 |
| CHEMBL2206617 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL2206619 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2206612 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL2206629 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2206613 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2206630 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2206615 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL2206627 | — | Ki | = | 97.0 | nM | 7.01 |