Assay Detail
Binding
CHEMBL2160360
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Inhibition of JAK1 kinase domain using N-terminal 5-carboxyfluorescein-tagged Val-Ala-Leu-Val-Asp-Gly-Tyr-Phe-Arg-Leu-Thr-Thr as substrate after 30 mins
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous 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 |
|---|---|---|---|
| Ki | 22 | 8.37 | 9.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 9.70 |
| CHEMBL2159143 | — | — | 1 | 9.05 |
| CHEMBL2159202 | — | — | 1 | 8.92 |
| CHEMBL2159142 | — | — | 1 | 8.89 |
| CHEMBL2159198 | — | — | 1 | 8.89 |
| CHEMBL2159205 | — | — | 1 | 8.82 |
| CHEMBL2159210 | — | — | 1 | 8.74 |
| CHEMBL2159204 | — | — | 1 | 8.70 |
| CHEMBL2159208 | — | — | 1 | 8.59 |
| CHEMBL2159200 | — | — | 1 | 8.55 |
| CHEMBL2159206 | — | — | 1 | 8.35 |
| CHEMBL2159214 | — | — | 1 | 8.32 |
| CHEMBL2159215 | — | — | 1 | 8.27 |
| CHEMBL2159209 | — | — | 1 | 8.24 |
| CHEMBL2159207 | — | — | 1 | 8.21 |
| CHEMBL2159212 | — | — | 1 | 8.17 |
| CHEMBL2159211 | — | — | 1 | 8.14 |
| CHEMBL2159203 | — | — | 1 | 8.03 |
| CHEMBL2159141 | — | — | 1 | 8.00 |
| CHEMBL2159199 | — | — | 1 | 7.75 |
| CHEMBL2159213 | — | — | 1 | 7.05 |
| CHEMBL2159201 | — | — | 1 | 6.82 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | Ki | = | 0.2 | nM | 9.70 |
| CHEMBL2159143 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL2159202 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL2159142 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2159198 | — | Ki | = | 1.3 | nM | 8.89 |
| CHEMBL2159205 | — | Ki | = | 1.5 | nM | 8.82 |
| CHEMBL2159210 | — | Ki | = | 1.8 | nM | 8.74 |
| CHEMBL2159204 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL2159208 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL2159200 | — | Ki | = | 2.8 | nM | 8.55 |
| CHEMBL2159206 | — | Ki | = | 4.5 | nM | 8.35 |
| CHEMBL2159214 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL2159215 | — | Ki | = | 5.4 | nM | 8.27 |
| CHEMBL2159209 | — | Ki | = | 5.8 | nM | 8.24 |
| CHEMBL2159207 | — | Ki | = | 6.1 | nM | 8.21 |
| CHEMBL2159212 | — | Ki | = | 6.7 | nM | 8.17 |
| CHEMBL2159211 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL2159203 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL2159141 | — | Ki | = | 10.0 | nM | 8.00 |
| CHEMBL2159199 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2159213 | — | Ki | = | 90.0 | nM | 7.05 |
| CHEMBL2159201 | — | Ki | = | 150.0 | nM | 6.82 |