Assay Detail
Binding
CHEMBL2160361
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Inhibition of JAK2 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
23
Total Activities
23
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 | 23 | 7.72 | 10.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 10.00 |
| CHEMBL2159143 | — | — | 1 | 8.68 |
| CHEMBL2159142 | — | — | 1 | 8.54 |
| CHEMBL2159198 | — | — | 1 | 8.30 |
| CHEMBL2159202 | — | — | 1 | 8.19 |
| CHEMBL2159205 | — | — | 1 | 8.03 |
| CHEMBL2159204 | — | — | 1 | 7.96 |
| CHEMBL2159206 | — | — | 1 | 7.96 |
| CHEMBL2159208 | — | — | 1 | 7.92 |
| CHEMBL2159200 | — | — | 1 | 7.92 |
| CHEMBL2159210 | — | — | 1 | 7.92 |
| CHEMBL2159207 | — | — | 1 | 7.77 |
| CHEMBL2159212 | — | — | 1 | 7.75 |
| CHEMBL2159211 | — | — | 1 | 7.68 |
| CHEMBL2159209 | — | — | 1 | 7.62 |
| CHEMBL2159214 | — | — | 1 | 7.58 |
| CHEMBL2159215 | — | — | 1 | 7.55 |
| CHEMBL2159199 | — | — | 1 | 7.18 |
| CHEMBL2159203 | — | — | 1 | 7.13 |
| CHEMBL2159141 | — | — | 1 | 6.70 |
| CHEMBL2152306 | — | — | 1 | 6.60 |
| CHEMBL2159213 | — | — | 1 | 6.28 |
| CHEMBL2159201 | — | — | 1 | 6.24 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1789941 | RUXOLITINIB | Ki | = | 0.1 | nM | 10.00 |
| CHEMBL2159143 | — | Ki | = | 2.1 | nM | 8.68 |
| CHEMBL2159142 | — | Ki | = | 2.9 | nM | 8.54 |
| CHEMBL2159198 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL2159202 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL2159205 | — | Ki | = | 9.3 | nM | 8.03 |
| CHEMBL2159204 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2159206 | — | Ki | = | 11.0 | nM | 7.96 |
| CHEMBL2159208 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2159200 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2159210 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL2159207 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL2159212 | — | Ki | = | 18.0 | nM | 7.75 |
| CHEMBL2159211 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL2159209 | — | Ki | = | 24.0 | nM | 7.62 |
| CHEMBL2159214 | — | Ki | = | 26.0 | nM | 7.58 |
| CHEMBL2159215 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL2159199 | — | Ki | = | 66.0 | nM | 7.18 |
| CHEMBL2159203 | — | Ki | = | 74.0 | nM | 7.13 |
| CHEMBL2159141 | — | Ki | = | 200.0 | nM | 6.70 |
| CHEMBL2152306 | — | Ki | = | 250.0 | nM | 6.60 |
| CHEMBL2159213 | — | Ki | = | 520.0 | nM | 6.28 |
| CHEMBL2159201 | — | Ki | = | 580.0 | nM | 6.24 |