Assay Detail
Binding
CHEMBL2160364
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Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 30 to 45 mins
23
Total Activities
23
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
Discovery and optimization of C-2 methyl imidazopyrrolopyridines as potent and orally bioavailable JAK1 inhibitors with selectivity over JAK2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 23 | 6.72 | 7.62 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 7.62 |
| CHEMBL2159143 | — | — | 1 | 7.58 |
| CHEMBL2159142 | — | — | 1 | 7.46 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 7.28 |
| CHEMBL2159202 | — | — | 1 | 7.24 |
| CHEMBL2159210 | — | — | 1 | 7.06 |
| CHEMBL2159198 | — | — | 1 | 7.00 |
| CHEMBL2159205 | — | — | 1 | 6.96 |
| CHEMBL2159214 | — | — | 1 | 6.75 |
| CHEMBL2159215 | — | — | 1 | 6.72 |
| CHEMBL2159141 | — | — | 1 | 6.60 |
| CHEMBL2159212 | — | — | 1 | 6.60 |
| CHEMBL2159209 | — | — | 1 | 6.57 |
| CHEMBL2159208 | — | — | 1 | 6.55 |
| CHEMBL2159211 | — | — | 1 | 6.51 |
| CHEMBL2159204 | — | — | 1 | 6.46 |
| CHEMBL2159200 | — | — | 1 | 6.46 |
| CHEMBL2159203 | — | — | 1 | 6.31 |
| CHEMBL2159206 | — | — | 1 | 6.05 |
| CHEMBL2159199 | — | — | 1 | 6.00 |
| CHEMBL2159207 | — | — | 1 | 5.44 |
| CHEMBL2159201 | — | — | 1 | - |
| CHEMBL2159213 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | EC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2159143 | — | EC50 | = | 26.0 | nM | 7.58 |
| CHEMBL2159142 | — | EC50 | = | 35.0 | nM | 7.46 |
| CHEMBL221959 | TOFACITINIB | EC50 | = | 53.0 | nM | 7.28 |
| CHEMBL2159202 | — | EC50 | = | 57.0 | nM | 7.24 |
| CHEMBL2159210 | — | EC50 | = | 87.0 | nM | 7.06 |
| CHEMBL2159198 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2159205 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL2159214 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL2159215 | — | EC50 | = | 190.0 | nM | 6.72 |
| CHEMBL2159141 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2159212 | — | EC50 | = | 250.0 | nM | 6.60 |
| CHEMBL2159209 | — | EC50 | = | 270.0 | nM | 6.57 |
| CHEMBL2159208 | — | EC50 | = | 280.0 | nM | 6.55 |
| CHEMBL2159211 | — | EC50 | = | 310.0 | nM | 6.51 |
| CHEMBL2159204 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2159200 | — | EC50 | = | 350.0 | nM | 6.46 |
| CHEMBL2159203 | — | EC50 | = | 490.0 | nM | 6.31 |
| CHEMBL2159206 | — | EC50 | = | 890.0 | nM | 6.05 |
| CHEMBL2159199 | — | EC50 | = | 990.0 | nM | 6.00 |
| CHEMBL2159207 | — | EC50 | = | 3600.0 | nM | 5.44 |
| CHEMBL2159201 | — | EC50 | - | — | - | |
| CHEMBL2159213 | — | EC50 | - | — | - |