Assay Detail
Binding
CHEMBL5147398
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Inhibition of human JAK2 kinase domain
18
Total Activities
18
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
Optimisation of momelotinib with improved potency and efficacy as pan-JAK inhibitor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 8.09 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5175300 | — | — | 1 | 8.52 |
| CHEMBL5189266 | — | — | 1 | 8.52 |
| CHEMBL5180789 | — | — | 1 | 8.30 |
| CHEMBL5171759 | — | — | 1 | 8.30 |
| CHEMBL5192167 | — | — | 1 | 8.30 |
| CHEMBL5169511 | — | — | 1 | 8.30 |
| CHEMBL5186530 | — | — | 1 | 8.22 |
| CHEMBL5179590 | — | — | 1 | 8.15 |
| CHEMBL5208298 | — | — | 1 | 8.10 |
| CHEMBL5192393 | — | — | 1 | 8.10 |
| CHEMBL5201856 | — | — | 1 | 8.00 |
| CHEMBL1078178 | MOMELOTINIB | 4.0 | 1 | 7.82 |
| CHEMBL5195322 | — | — | 1 | 7.77 |
| CHEMBL5174885 | — | — | 1 | 7.66 |
| CHEMBL5185244 | — | — | 1 | 7.28 |
| CHEMBL5198976 | — | — | 1 | - |
| CHEMBL5175767 | — | — | 1 | - |
| CHEMBL5171066 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5175300 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5189266 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5180789 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5171759 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5192167 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5169511 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5186530 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5179590 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL5208298 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5192393 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL5201856 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL1078178 | MOMELOTINIB | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL5195322 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5174885 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL5185244 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL5198976 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL5175767 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5171066 | — | IC50 | > | 500.0 | nM | - |