Assay Detail
Binding
CHEMBL3625645
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Inhibition of recombinant JAK1 (unknown origin) using 5-FAM-KKKKEEIYFFFG-OH substrate and ATP incubated for 180 mins by scintillation counting method
10
Total Activities
10
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
Discovery of a Highly Selective JAK2 Inhibitor, BMS-911543, for the Treatment of Myeloproliferative Neoplasms.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 6.96 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3622150 | — | — | 1 | 7.80 |
| CHEMBL3622143 | — | — | 1 | 7.72 |
| CHEMBL3622144 | — | — | 1 | 7.66 |
| CHEMBL3622145 | — | — | 1 | 7.40 |
| CHEMBL3622146 | — | — | 1 | 7.32 |
| CHEMBL3545215 | BMS-911543 | 2.0 | 1 | 7.12 |
| CHEMBL3622142 | — | — | 1 | 6.60 |
| CHEMBL3622148 | — | — | 1 | 6.48 |
| CHEMBL3622149 | — | — | 1 | 6.27 |
| CHEMBL3622147 | — | — | 1 | 5.22 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3622150 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3622143 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3622144 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL3622145 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3622146 | — | IC50 | = | 48.0 | nM | 7.32 |
| CHEMBL3545215 | BMS-911543 | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL3622142 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL3622148 | — | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL3622149 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL3622147 | — | IC50 | = | 6000.0 | nM | 5.22 |