Assay Detail
Binding
CHEMBL2390366
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Inhibition of JAK3 (unknown origin) using Leu-Pro-Leu-Asp-Lys-Asp-Tyr-Tyr-Val-Val-Arg as substrate after 30 mins in presence of ATP
7
Total Activities
7
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 of C-2 hydroxyethyl imidazopyrrolopyridines as potent JAK1 inhibitors with favorable physicochemical properties and high selectivity over JAK2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 7 | 7.66 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 9.40 |
| CHEMBL2386635 | — | — | 1 | 8.23 |
| CHEMBL2386636 | — | — | 1 | 8.11 |
| CHEMBL2385096 | — | — | 1 | 7.28 |
| CHEMBL2386629 | — | — | 1 | 7.12 |
| CHEMBL2386653 | — | — | 1 | 6.96 |
| CHEMBL2386633 | — | — | 1 | 6.55 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL221959 | TOFACITINIB | Ki | = | 0.4 | nM | 9.40 |
| CHEMBL2386635 | — | Ki | = | 5.9 | nM | 8.23 |
| CHEMBL2386636 | — | Ki | = | 7.8 | nM | 8.11 |
| CHEMBL2385096 | — | Ki | = | 53.0 | nM | 7.28 |
| CHEMBL2386629 | — | Ki | = | 76.0 | nM | 7.12 |
| CHEMBL2386653 | — | Ki | = | 110.0 | nM | 6.96 |
| CHEMBL2386633 | — | Ki | = | 280.0 | nM | 6.55 |