Assay Detail
Binding
CHEMBL2390549
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Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins
28
Total Activities
28
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 | 28 | 6.91 | 8.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386635 | — | — | 1 | 8.24 |
| CHEMBL2386629 | — | — | 1 | 7.55 |
| CHEMBL2386636 | — | — | 1 | 7.37 |
| CHEMBL2386640 | — | — | 1 | 7.33 |
| CHEMBL2386634 | — | — | 1 | 7.31 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.28 |
| CHEMBL2386630 | — | — | 1 | 7.24 |
| CHEMBL2386637 | — | — | 1 | 7.19 |
| CHEMBL2385096 | — | — | 1 | 7.16 |
| CHEMBL2386645 | — | — | 1 | 7.16 |
| CHEMBL2386632 | — | — | 1 | 7.13 |
| CHEMBL2386643 | — | — | 1 | 7.08 |
| CHEMBL2386648 | — | — | 1 | 7.06 |
| CHEMBL2159198 | — | — | 1 | 7.00 |
| CHEMBL2386653 | — | — | 1 | 6.96 |
| CHEMBL2386646 | — | — | 1 | 6.96 |
| CHEMBL2386633 | — | — | 1 | 6.92 |
| CHEMBL2386627 | — | — | 1 | 6.92 |
| CHEMBL2386638 | — | — | 1 | 6.89 |
| CHEMBL2386628 | — | — | 1 | 6.62 |
| CHEMBL2386644 | — | — | 1 | 6.50 |
| CHEMBL2386641 | — | — | 1 | 6.48 |
| CHEMBL2386639 | — | — | 1 | 6.44 |
| CHEMBL2386626 | — | — | 1 | 6.42 |
| CHEMBL2386642 | — | — | 1 | 6.39 |
| CHEMBL2386625 | — | — | 1 | 6.39 |
| CHEMBL2386647 | — | — | 1 | 6.29 |
| CHEMBL2386649 | — | — | 1 | 5.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386635 | — | EC50 | = | 5.7 | nM | 8.24 |
| CHEMBL2386629 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2386636 | — | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2386640 | — | EC50 | = | 47.0 | nM | 7.33 |
| CHEMBL2386634 | — | EC50 | = | 49.0 | nM | 7.31 |
| CHEMBL221959 | TOFACITINIB | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2386630 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2386637 | — | EC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2385096 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2386645 | — | EC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2386632 | — | EC50 | = | 74.0 | nM | 7.13 |
| CHEMBL2386643 | — | EC50 | = | 84.0 | nM | 7.08 |
| CHEMBL2386648 | — | EC50 | = | 88.0 | nM | 7.06 |
| CHEMBL2159198 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2386653 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2386646 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2386633 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2386627 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2386638 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2386628 | — | EC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2386644 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2386641 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2386639 | — | EC50 | = | 360.0 | nM | 6.44 |
| CHEMBL2386626 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2386642 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2386625 | — | EC50 | = | 410.0 | nM | 6.39 |
| CHEMBL2386647 | — | EC50 | = | 510.0 | nM | 6.29 |
| CHEMBL2386649 | — | EC50 | = | 8200.0 | nM | 5.09 |