Assay Detail
Binding
CHEMBL2155760
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Inhibition of JAK3
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 | 7.61 | 9.40 |
| IC50 | 1 | 6.09 | 6.09 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.40 |
| CHEMBL2152297 | — | — | 1 | 9.05 |
| CHEMBL2152300 | — | — | 1 | 8.42 |
| CHEMBL2152299 | — | — | 1 | 7.66 |
| CHEMBL2152305 | — | — | 1 | 7.48 |
| CHEMBL2152298 | — | — | 1 | 6.92 |
| CHEMBL2152301 | — | — | 1 | 6.89 |
| CHEMBL2152303 | — | — | 1 | 6.89 |
| CHEMBL2152304 | — | — | 1 | 6.70 |
| CHEMBL2152302 | — | — | 1 | 6.66 |
| CHEMBL1795071 | RUXOLITINIB PHOSPHATE | 4.0 | 1 | 6.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2152297 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL2152300 | — | Ki | = | 3.8 | nM | 8.42 |
| CHEMBL2152299 | — | Ki | = | 22.0 | nM | 7.66 |
| CHEMBL2152305 | — | Ki | = | 33.0 | nM | 7.48 |
| CHEMBL2152298 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL2152301 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2152303 | — | Ki | = | 130.0 | nM | 6.89 |
| CHEMBL2152304 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2152302 | — | Ki | = | 220.0 | nM | 6.66 |
| CHEMBL1795071 | RUXOLITINIB PHOSPHATE | IC50 | = | 810.0 | nM | 6.09 |