Assay Detail
Binding
CHEMBL3766653
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Inhibition of JAK2 (unknown origin) using Ulight-JAK1 substrate peptide assessed as reduction in ATP-dependent substrate phosphorylation after 45 mins by TR-FRET assay
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure-Based Design and Synthesis of 3-Amino-1,5-dihydro-4H-pyrazolopyridin-4-one Derivatives as Tyrosine Kinase 2 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 20 | 6.93 | 9.10 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 9.10 |
| CHEMBL3763991 | — | — | 1 | 8.15 |
| CHEMBL3764277 | — | — | 1 | 7.92 |
| CHEMBL3765517 | — | — | 1 | 7.89 |
| CHEMBL3763252 | — | — | 1 | 7.89 |
| CHEMBL3763213 | — | — | 1 | 7.85 |
| CHEMBL3765822 | — | — | 1 | 7.77 |
| CHEMBL3764030 | — | — | 1 | 7.16 |
| CHEMBL3764383 | — | — | 1 | 6.85 |
| CHEMBL3764167 | — | — | 1 | 6.75 |
| CHEMBL3764637 | — | — | 1 | 6.51 |
| CHEMBL3763697 | — | — | 1 | 6.41 |
| CHEMBL3764463 | — | — | 1 | 6.26 |
| CHEMBL498859 | — | — | 1 | 6.18 |
| CHEMBL3763184 | — | — | 1 | 6.08 |
| CHEMBL3765131 | — | — | 1 | 6.04 |
| CHEMBL3763289 | — | — | 1 | 5.85 |
| CHEMBL3763864 | — | — | 1 | 5.77 |
| CHEMBL3763310 | — | — | 1 | 5.15 |
| CHEMBL3763833 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105759 | BARICITINIB | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL3763991 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3764277 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL3765517 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3763252 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3763213 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3765822 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3764030 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL3764383 | — | IC50 | = | 140.0 | nM | 6.85 |
| CHEMBL3764167 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL3764637 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL3763697 | — | IC50 | = | 390.0 | nM | 6.41 |
| CHEMBL3764463 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL498859 | — | IC50 | = | 660.0 | nM | 6.18 |
| CHEMBL3763184 | — | IC50 | = | 830.0 | nM | 6.08 |
| CHEMBL3765131 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3763289 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL3763864 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL3763310 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3763833 | — | IC50 | > | 10000.0 | nM | - |