Assay Detail
Binding
CHEMBL2390546
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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 in presence of whole blood
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Tissue | Blood |
| 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 | 21 | 6.77 | 7.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2386635 | — | — | 1 | 7.55 |
| CHEMBL2386629 | — | — | 1 | 7.54 |
| CHEMBL2386636 | — | — | 1 | 7.48 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.37 |
| CHEMBL2385096 | — | — | 1 | 7.29 |
| CHEMBL2386630 | — | — | 1 | 7.21 |
| CHEMBL2386634 | — | — | 1 | 7.11 |
| CHEMBL2386632 | — | — | 1 | 7.09 |
| CHEMBL2386633 | — | — | 1 | 6.89 |
| CHEMBL2386627 | — | — | 1 | 6.85 |
| CHEMBL2386653 | — | — | 1 | 6.75 |
| CHEMBL2386645 | — | — | 1 | 6.66 |
| CHEMBL2386628 | — | — | 1 | 6.55 |
| CHEMBL2386647 | — | — | 1 | 6.50 |
| CHEMBL2386637 | — | — | 1 | 6.50 |
| CHEMBL2386648 | — | — | 1 | 6.48 |
| CHEMBL2386640 | — | — | 1 | 6.48 |
| CHEMBL2386625 | — | — | 1 | 6.14 |
| CHEMBL2386646 | — | — | 1 | 6.09 |
| CHEMBL2386638 | — | — | 1 | 5.82 |
| CHEMBL2386643 | — | — | 1 | 5.80 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2386635 | — | EC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2386629 | — | EC50 | = | 29.0 | nM | 7.54 |
| CHEMBL2386636 | — | EC50 | = | 33.0 | nM | 7.48 |
| CHEMBL221959 | TOFACITINIB | EC50 | = | 43.0 | nM | 7.37 |
| CHEMBL2385096 | — | EC50 | = | 51.0 | nM | 7.29 |
| CHEMBL2386630 | — | EC50 | = | 62.0 | nM | 7.21 |
| CHEMBL2386634 | — | EC50 | = | 78.0 | nM | 7.11 |
| CHEMBL2386632 | — | EC50 | = | 82.0 | nM | 7.09 |
| CHEMBL2386633 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL2386627 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL2386653 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2386645 | — | EC50 | = | 220.0 | nM | 6.66 |
| CHEMBL2386628 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2386647 | — | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL2386637 | — | EC50 | = | 313.0 | nM | 6.50 |
| CHEMBL2386648 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2386640 | — | EC50 | = | 330.0 | nM | 6.48 |
| CHEMBL2386625 | — | EC50 | = | 730.0 | nM | 6.14 |
| CHEMBL2386646 | — | EC50 | = | 820.0 | nM | 6.09 |
| CHEMBL2386638 | — | EC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2386643 | — | EC50 | = | 1600.0 | nM | 5.80 |