Assay Detail
Binding
CHEMBL5377860
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Inhibition of recombinant JAK3 (unknown origin) using GFP-STAT1 as substrate incubated for 1 hr by TR-FRET Lanthascreen assay
27
Total Activities
26
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
Identification and Biological Evaluation of a Potent and Selective JAK1 Inhibitor for the Treatment of Pulmonary Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 27 | 7.37 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.00 |
| CHEMBL5398372 | — | — | 2 | 8.44 |
| CHEMBL5427932 | — | — | 1 | 8.32 |
| CHEMBL5430795 | — | — | 1 | 8.16 |
| CHEMBL5423944 | — | — | 1 | 8.09 |
| CHEMBL5435417 | — | — | 1 | 8.08 |
| CHEMBL5410919 | — | — | 1 | 8.04 |
| CHEMBL5397297 | — | — | 1 | 8.03 |
| CHEMBL5396523 | — | — | 1 | 7.97 |
| CHEMBL5440017 | — | — | 1 | 7.94 |
| CHEMBL5402123 | — | — | 1 | 7.92 |
| CHEMBL5405140 | — | — | 1 | 7.84 |
| CHEMBL5423894 | — | — | 1 | 7.75 |
| CHEMBL5408324 | — | — | 1 | 7.64 |
| CHEMBL5405043 | — | — | 1 | 7.39 |
| CHEMBL5439582 | — | — | 1 | 6.94 |
| CHEMBL5400756 | — | — | 1 | 6.84 |
| CHEMBL5420407 | — | — | 1 | 6.78 |
| CHEMBL5423387 | — | — | 1 | 6.66 |
| CHEMBL5441087 | — | — | 1 | 6.60 |
| CHEMBL5434116 | — | — | 1 | 6.60 |
| CHEMBL4742766 | — | — | 1 | 6.51 |
| CHEMBL5410927 | — | — | 1 | 6.50 |
| CHEMBL5404261 | — | — | 1 | 6.44 |
| CHEMBL5430831 | — | — | 1 | 6.18 |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | 6.18 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | IC50 | = | 0.99 | nM | 9.00 |
| CHEMBL5398372 | — | IC50 | = | 3.63 | nM | 8.44 |
| CHEMBL5427932 | — | IC50 | = | 4.81 | nM | 8.32 |
| CHEMBL5430795 | — | IC50 | = | 6.93 | nM | 8.16 |
| CHEMBL5423944 | — | IC50 | = | 8.05 | nM | 8.09 |
| CHEMBL5435417 | — | IC50 | = | 8.39 | nM | 8.08 |
| CHEMBL5410919 | — | IC50 | = | 9.11 | nM | 8.04 |
| CHEMBL5397297 | — | IC50 | = | 9.24 | nM | 8.03 |
| CHEMBL5396523 | — | IC50 | = | 10.8 | nM | 7.97 |
| CHEMBL5440017 | — | IC50 | = | 11.6 | nM | 7.94 |
| CHEMBL5402123 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5405140 | — | IC50 | = | 14.5 | nM | 7.84 |
| CHEMBL5423894 | — | IC50 | = | 17.6 | nM | 7.75 |
| CHEMBL5408324 | — | IC50 | = | 22.7 | nM | 7.64 |
| CHEMBL5405043 | — | IC50 | = | 40.5 | nM | 7.39 |
| CHEMBL5439582 | — | IC50 | = | 115.5 | nM | 6.94 |
| CHEMBL5400756 | — | IC50 | = | 143.4 | nM | 6.84 |
| CHEMBL5420407 | — | IC50 | = | 166.8 | nM | 6.78 |
| CHEMBL5423387 | — | IC50 | = | 221.1 | nM | 6.66 |
| CHEMBL5441087 | — | IC50 | = | 250.9 | nM | 6.60 |
| CHEMBL5434116 | — | IC50 | = | 249.6 | nM | 6.60 |
| CHEMBL4742766 | — | IC50 | = | 305.2 | nM | 6.51 |
| CHEMBL5410927 | — | IC50 | = | 316.1 | nM | 6.50 |
| CHEMBL5404261 | — | IC50 | = | 363.6 | nM | 6.44 |
| CHEMBL5430831 | — | IC50 | = | 664.4 | nM | 6.18 |
| CHEMBL3301607 | FILGOTINIB | IC50 | = | 653.6 | nM | 6.18 |
| CHEMBL5398372 | — | IC50 | = | 957.4 | nM | 6.02 |