Assay Detail
Binding
CHEMBL5377863
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Inhibition of recombinant JAK2 (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 | 7.35 | 8.18 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5423944 | — | — | 1 | 8.18 |
| CHEMBL5398372 | — | — | 2 | 8.13 |
| CHEMBL5427932 | — | — | 1 | 8.07 |
| CHEMBL5435417 | — | — | 1 | 8.06 |
| CHEMBL5396523 | — | — | 1 | 8.05 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 8.02 |
| CHEMBL5410919 | — | — | 1 | 7.88 |
| CHEMBL5430795 | — | — | 1 | 7.80 |
| CHEMBL5397297 | — | — | 1 | 7.78 |
| CHEMBL5402123 | — | — | 1 | 7.73 |
| CHEMBL5408324 | — | — | 1 | 7.65 |
| CHEMBL5440017 | — | — | 1 | 7.61 |
| CHEMBL5405043 | — | — | 1 | 7.57 |
| CHEMBL5423894 | — | — | 1 | 7.48 |
| CHEMBL5405140 | — | — | 1 | 7.37 |
| CHEMBL5441087 | — | — | 1 | 7.19 |
| CHEMBL5423387 | — | — | 1 | 7.06 |
| CHEMBL5439582 | — | — | 1 | 7.06 |
| CHEMBL5434116 | — | — | 1 | 7.05 |
| CHEMBL5420407 | — | — | 1 | 7.00 |
| CHEMBL5400756 | — | — | 1 | 6.74 |
| CHEMBL5404261 | — | — | 1 | 6.73 |
| CHEMBL3301607 | FILGOTINIB | 4.0 | 1 | 6.73 |
| CHEMBL4742766 | — | — | 1 | 6.69 |
| CHEMBL5410927 | — | — | 1 | 6.59 |
| CHEMBL5430831 | — | — | 1 | 6.12 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5423944 | — | IC50 | = | 6.68 | nM | 8.18 |
| CHEMBL5398372 | — | IC50 | = | 7.39 | nM | 8.13 |
| CHEMBL5427932 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL5435417 | — | IC50 | = | 8.78 | nM | 8.06 |
| CHEMBL5396523 | — | IC50 | = | 8.97 | nM | 8.05 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 9.63 | nM | 8.02 |
| CHEMBL5410919 | — | IC50 | = | 13.1 | nM | 7.88 |
| CHEMBL5430795 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL5397297 | — | IC50 | = | 16.8 | nM | 7.78 |
| CHEMBL5402123 | — | IC50 | = | 18.7 | nM | 7.73 |
| CHEMBL5408324 | — | IC50 | = | 22.6 | nM | 7.65 |
| CHEMBL5440017 | — | IC50 | = | 24.5 | nM | 7.61 |
| CHEMBL5405043 | — | IC50 | = | 27.1 | nM | 7.57 |
| CHEMBL5423894 | — | IC50 | = | 32.9 | nM | 7.48 |
| CHEMBL5405140 | — | IC50 | = | 43.2 | nM | 7.37 |
| CHEMBL5441087 | — | IC50 | = | 64.9 | nM | 7.19 |
| CHEMBL5423387 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5439582 | — | IC50 | = | 87.8 | nM | 7.06 |
| CHEMBL5434116 | — | IC50 | = | 88.1 | nM | 7.05 |
| CHEMBL5420407 | — | IC50 | = | 99.6 | nM | 7.00 |
| CHEMBL5400756 | — | IC50 | = | 180.7 | nM | 6.74 |
| CHEMBL5404261 | — | IC50 | = | 187.8 | nM | 6.73 |
| CHEMBL3301607 | FILGOTINIB | IC50 | = | 184.9 | nM | 6.73 |
| CHEMBL4742766 | — | IC50 | = | 203.34 | nM | 6.69 |
| CHEMBL5410927 | — | IC50 | = | 255.9 | nM | 6.59 |
| CHEMBL5430831 | — | IC50 | = | 761.8 | nM | 6.12 |
| CHEMBL5398372 | — | IC50 | = | 865.5 | nM | 6.06 |