Assay Detail
Binding
CHEMBL2155759
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Inhibition of JAK2
11
Total Activities
11
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Identification of imidazo-pyrrolopyridines as novel and potent JAK1 inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 7.91 | 9.52 |
| IC50 | 1 | 7.55 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2152297 | — | — | 1 | 9.52 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.15 |
| CHEMBL2152300 | — | — | 1 | 8.92 |
| CHEMBL2152305 | — | — | 1 | 8.36 |
| CHEMBL2152299 | — | — | 1 | 7.60 |
| CHEMBL2152303 | — | — | 1 | 7.60 |
| CHEMBL1795071 | RUXOLITINIB PHOSPHATE | 4.0 | 1 | 7.55 |
| CHEMBL2152302 | — | — | 1 | 7.33 |
| CHEMBL2152301 | — | — | 1 | 7.25 |
| CHEMBL2152304 | — | — | 1 | 7.23 |
| CHEMBL2152298 | — | — | 1 | 6.11 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2152297 | — | Ki | = | 0.3 | nM | 9.52 |
| CHEMBL221959 | TOFACITINIB | Ki | = | 0.7 | nM | 9.15 |
| CHEMBL2152300 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2152305 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL2152299 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL2152303 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL1795071 | RUXOLITINIB PHOSPHATE | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2152302 | — | Ki | = | 47.0 | nM | 7.33 |
| CHEMBL2152301 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL2152304 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL2152298 | — | Ki | = | 770.0 | nM | 6.11 |