Assay Detail
Binding
CHEMBL2390548
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Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | TF-1 |
| 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 |
|---|---|---|---|
| EC50 | 11 | 5.84 | 7.03 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.03 |
| CHEMBL2159198 | — | — | 1 | 6.31 |
| CHEMBL2386637 | — | — | 1 | 6.14 |
| CHEMBL2386645 | — | — | 1 | 5.82 |
| CHEMBL2386638 | — | — | 1 | 5.82 |
| CHEMBL2386640 | — | — | 1 | 5.77 |
| CHEMBL2386643 | — | — | 1 | 5.54 |
| CHEMBL2386641 | — | — | 1 | 5.36 |
| CHEMBL2386644 | — | — | 1 | 5.33 |
| CHEMBL2386639 | — | — | 1 | 5.28 |
| CHEMBL2386642 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | EC50 | = | 93.0 | nM | 7.03 |
| CHEMBL2159198 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2386637 | — | EC50 | = | 730.0 | nM | 6.14 |
| CHEMBL2386645 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2386638 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2386640 | — | EC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2386643 | — | EC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2386641 | — | EC50 | = | 4400.0 | nM | 5.36 |
| CHEMBL2386644 | — | EC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL2386639 | — | EC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL2386642 | — | EC50 | > | 10.0 | nM | - |