Assay Detail
Binding
CHEMBL3766652
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Inhibition of JAK1 (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 | 7.13 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 9.00 |
| CHEMBL3763991 | — | — | 1 | 8.16 |
| CHEMBL3763252 | — | — | 1 | 7.82 |
| CHEMBL3765822 | — | — | 1 | 7.80 |
| CHEMBL3763213 | — | — | 1 | 7.80 |
| CHEMBL3764277 | — | — | 1 | 7.62 |
| CHEMBL3764030 | — | — | 1 | 7.52 |
| CHEMBL3764463 | — | — | 1 | 7.19 |
| CHEMBL3765517 | — | — | 1 | 7.17 |
| CHEMBL3764637 | — | — | 1 | 7.10 |
| CHEMBL3764167 | — | — | 1 | 7.05 |
| CHEMBL3765131 | — | — | 1 | 7.04 |
| CHEMBL3764383 | — | — | 1 | 7.00 |
| CHEMBL3763864 | — | — | 1 | 6.89 |
| CHEMBL3763697 | — | — | 1 | 6.64 |
| CHEMBL3763184 | — | — | 1 | 6.58 |
| CHEMBL3763289 | — | — | 1 | 6.43 |
| CHEMBL498859 | — | — | 1 | 6.31 |
| CHEMBL3763310 | — | — | 1 | 6.00 |
| CHEMBL3763833 | — | — | 1 | 5.51 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105759 | BARICITINIB | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL3763991 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL3763252 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL3765822 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3763213 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3764277 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3764030 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3764463 | — | IC50 | = | 65.0 | nM | 7.19 |
| CHEMBL3765517 | — | IC50 | = | 67.0 | nM | 7.17 |
| CHEMBL3764637 | — | IC50 | = | 79.0 | nM | 7.10 |
| CHEMBL3764167 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL3765131 | — | IC50 | = | 91.0 | nM | 7.04 |
| CHEMBL3764383 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL3763864 | — | IC50 | = | 130.0 | nM | 6.89 |
| CHEMBL3763697 | — | IC50 | = | 230.0 | nM | 6.64 |
| CHEMBL3763184 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL3763289 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL498859 | — | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL3763310 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3763833 | — | IC50 | = | 3100.0 | nM | 5.51 |