Assay Detail
Toxicity
CHEMBL5120629
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Inhibition of JAK2 signaling pathway in human CHEP cells assessed as inhibition of EPO-induced cell survival preincubated for 1 hr followed by EPO addition and measured after 48 hrs by CellTiter-Glo luminescent assay
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Toxicity |
| Organism | Homo sapiens |
| Cell Type | CHEP |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Optimization of Pyrimidine Compounds as Potent JAK1 Inhibitors and the Discovery of R507 as a Clinical Candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 12 | 6.54 | 7.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5187209 | — | — | 1 | 7.38 |
| CHEMBL5192889 | — | — | 1 | 7.09 |
| CHEMBL5205935 | — | — | 1 | 7.08 |
| CHEMBL5198389 | — | — | 1 | 6.88 |
| CHEMBL5170161 | — | — | 1 | 6.77 |
| CHEMBL5209379 | — | — | 1 | 6.76 |
| CHEMBL5184050 | — | — | 1 | 6.45 |
| CHEMBL4594441 | IFIDANCITINIB | 2.0 | 1 | 6.31 |
| CHEMBL5203646 | — | — | 1 | 6.30 |
| CHEMBL5188333 | — | — | 1 | 5.96 |
| CHEMBL5173045 | — | — | 1 | 5.77 |
| CHEMBL5192063 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5187209 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL5192889 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL5205935 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL5198389 | — | IC50 | = | 132.0 | nM | 6.88 |
| CHEMBL5170161 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL5209379 | — | IC50 | = | 173.0 | nM | 6.76 |
| CHEMBL5184050 | — | IC50 | = | 354.0 | nM | 6.45 |
| CHEMBL4594441 | IFIDANCITINIB | IC50 | = | 490.0 | nM | 6.31 |
| CHEMBL5203646 | — | IC50 | = | 503.0 | nM | 6.30 |
| CHEMBL5188333 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL5173045 | — | IC50 | = | 1689.0 | nM | 5.77 |
| CHEMBL5192063 | — | IC50 | = | 1976.0 | nM | 5.70 |