Assay Detail
ADMET
CHEMBL4022973
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Inhibition of JAK2 in CD34+ human whole blood assessed as reduction in EOP induced STAT5 phosphorylation preincubated for 45 mins followed by EOP addition measured after 15 mins by flow cytometric analysis
43
Total Activities
43
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | ADMET |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification of N-{cis-3-[Methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino]cyclobutyl}propane-1-sulfonamide (PF-04965842): A Selective JAK1 Clinical Candidate for the Treatment of Autoimmune Diseases.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 43 | 5.44 | 7.06 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2105759 | BARICITINIB | 4.0 | 1 | 7.06 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.52 |
| CHEMBL1789941 | RUXOLITINIB | 4.0 | 1 | 6.17 |
| CHEMBL4104105 | — | — | 1 | 5.71 |
| CHEMBL4059667 | — | — | 1 | 5.70 |
| CHEMBL4093955 | — | — | 1 | 5.65 |
| CHEMBL3658860 | — | — | 1 | 5.39 |
| CHEMBL3655080 | — | — | 1 | 5.38 |
| CHEMBL3655104 | — | — | 1 | 5.35 |
| CHEMBL4063642 | — | — | 1 | 5.33 |
| CHEMBL4085264 | — | — | 1 | 5.27 |
| CHEMBL4100048 | — | — | 1 | 5.26 |
| CHEMBL4103435 | — | — | 1 | 5.21 |
| CHEMBL4103698 | — | — | 1 | 5.17 |
| CHEMBL3655086 | — | — | 1 | 5.17 |
| CHEMBL3655081 | ABROCITINIB | 4.0 | 1 | 5.14 |
| CHEMBL3655095 | — | — | 1 | 5.12 |
| CHEMBL3655082 | — | — | 1 | 5.03 |
| CHEMBL4077614 | — | — | 1 | 4.99 |
| CHEMBL4100431 | — | — | 1 | 4.92 |
| CHEMBL4087961 | — | — | 1 | 4.79 |
| CHEMBL4099048 | — | — | 1 | - |
| CHEMBL4087044 | — | — | 1 | - |
| CHEMBL4065613 | — | — | 1 | - |
| CHEMBL4079179 | — | — | 1 | - |
| CHEMBL4066404 | — | — | 1 | - |
| CHEMBL4068319 | — | — | 1 | - |
| CHEMBL4101374 | — | — | 1 | - |
| CHEMBL4066876 | — | — | 1 | - |
| CHEMBL4101725 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2105759 | BARICITINIB | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 302.0 | nM | 6.52 |
| CHEMBL1789941 | RUXOLITINIB | IC50 | = | 677.0 | nM | 6.17 |
| CHEMBL4104105 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL4059667 | — | IC50 | = | 1990.0 | nM | 5.70 |
| CHEMBL4093955 | — | IC50 | = | 2260.0 | nM | 5.65 |
| CHEMBL3658860 | — | IC50 | = | 4090.0 | nM | 5.39 |
| CHEMBL3655080 | — | IC50 | = | 4120.0 | nM | 5.38 |
| CHEMBL3655104 | — | IC50 | = | 4460.0 | nM | 5.35 |
| CHEMBL4063642 | — | IC50 | = | 4670.0 | nM | 5.33 |
| CHEMBL4085264 | — | IC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL4100048 | — | IC50 | = | 5437.0 | nM | 5.26 |
| CHEMBL4103435 | — | IC50 | = | 6110.0 | nM | 5.21 |
| CHEMBL4103698 | — | IC50 | = | 6800.0 | nM | 5.17 |
| CHEMBL3655086 | — | IC50 | = | 6810.0 | nM | 5.17 |
| CHEMBL3655081 | ABROCITINIB | IC50 | = | 7178.0 | nM | 5.14 |
| CHEMBL3655095 | — | IC50 | = | 7540.0 | nM | 5.12 |
| CHEMBL3655082 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL4077614 | — | IC50 | = | 10200.0 | nM | 4.99 |
| CHEMBL4100431 | — | IC50 | = | 11900.0 | nM | 4.92 |
| CHEMBL4087961 | — | IC50 | = | 16100.0 | nM | 4.79 |
| CHEMBL4092805 | — | IC50 | > | 15900.0 | nM | - |
| CHEMBL4085011 | — | IC50 | - | — | - | |
| CHEMBL4071850 | — | IC50 | - | — | - | |
| CHEMBL4098094 | — | IC50 | - | — | - | |
| CHEMBL4078655 | — | IC50 | - | — | - | |
| CHEMBL3655097 | — | IC50 | - | — | - | |
| CHEMBL4082035 | — | IC50 | - | — | - | |
| CHEMBL4075575 | — | IC50 | - | — | - | |
| CHEMBL4090590 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4103586 | — | IC50 | - | — | - | |
| CHEMBL4089286 | — | IC50 | - | — | - | |
| CHEMBL4059894 | — | IC50 | - | — | - | |
| CHEMBL4093643 | — | IC50 | - | — | - | |
| CHEMBL4101725 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4066876 | — | IC50 | - | — | - | |
| CHEMBL4101374 | — | IC50 | - | — | - | |
| CHEMBL4068319 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4066404 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4079179 | — | IC50 | > | 20000.0 | nM | - |
| CHEMBL4065613 | — | IC50 | > | 15606.0 | nM | - |
| CHEMBL4087044 | — | IC50 | > | 15348.0 | nM | - |
| CHEMBL4099048 | — | IC50 | > | 6930.0 | nM | - |