Assay Detail
Binding
CHEMBL3766654
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Inhibition of JAK3 (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 | 7.34 | 8.55 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3763213 | — | — | 1 | 8.55 |
| CHEMBL3765822 | — | — | 1 | 8.48 |
| CHEMBL3765517 | — | — | 1 | 8.40 |
| CHEMBL3764277 | — | — | 1 | 8.34 |
| CHEMBL3763252 | — | — | 1 | 8.28 |
| CHEMBL3764030 | — | — | 1 | 8.19 |
| CHEMBL3763991 | — | — | 1 | 7.64 |
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 7.60 |
| CHEMBL3764463 | — | — | 1 | 7.57 |
| CHEMBL3764637 | — | — | 1 | 7.50 |
| CHEMBL3765131 | — | — | 1 | 7.41 |
| CHEMBL3764167 | — | — | 1 | 7.28 |
| CHEMBL3763864 | — | — | 1 | 7.09 |
| CHEMBL3764383 | — | — | 1 | 7.07 |
| CHEMBL3763184 | — | — | 1 | 7.04 |
| CHEMBL3763697 | — | — | 1 | 7.00 |
| CHEMBL498859 | — | — | 1 | 6.43 |
| CHEMBL3763289 | — | — | 1 | 5.72 |
| CHEMBL3763833 | — | — | 1 | 5.66 |
| CHEMBL3763310 | — | — | 1 | 5.47 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3763213 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3765822 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL3765517 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3764277 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL3763252 | — | IC50 | = | 5.3 | nM | 8.28 |
| CHEMBL3764030 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL3763991 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL2105759 | BARICITINIB | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3764463 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3764637 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3765131 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3764167 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3763864 | — | IC50 | = | 82.0 | nM | 7.09 |
| CHEMBL3764383 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL3763184 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL3763697 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL498859 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL3763289 | — | IC50 | = | 1900.0 | nM | 5.72 |
| CHEMBL3763833 | — | IC50 | = | 2200.0 | nM | 5.66 |
| CHEMBL3763310 | — | IC50 | = | 3400.0 | nM | 5.47 |