Assay Detail
Binding
CHEMBL4630007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged recombinant full-length human Lck using TK-substrate-biotin as substrate incubated for 60 mins in presence of ATP by fluorescence method
62
Total Activities
62
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 Janus Kinase Inhibitor Bearing a Highly Three-Dimensional Spiro Scaffold: JTE-052 (Delgocitinib) as a New Dermatological Agent to Treat Inflammatory Skin Disorders.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 62 | 5.67 | 6.66 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4646256 | — | — | 1 | 6.66 |
| CHEMBL221959 | TOFACITINIB | 4.0 | 1 | 6.47 |
| CHEMBL4639774 | — | — | 1 | 6.47 |
| CHEMBL4641927 | — | — | 1 | 6.40 |
| CHEMBL4639538 | — | — | 1 | 6.34 |
| CHEMBL4644221 | — | — | 1 | 6.26 |
| CHEMBL3693624 | — | — | 1 | 6.20 |
| CHEMBL3689514 | — | — | 1 | 5.82 |
| CHEMBL4636510 | — | — | 1 | 5.70 |
| CHEMBL3689517 | — | — | 1 | 5.58 |
| CHEMBL4634530 | — | — | 1 | 5.48 |
| CHEMBL3689515 | — | — | 1 | 5.43 |
| CHEMBL3693620 | — | — | 1 | 5.39 |
| CHEMBL4649366 | — | — | 1 | 5.38 |
| CHEMBL3693599 | — | — | 1 | 5.35 |
| CHEMBL3689516 | — | — | 1 | 5.33 |
| CHEMBL3693618 | — | — | 1 | 5.30 |
| CHEMBL3689522 | — | — | 1 | 5.28 |
| CHEMBL4638326 | — | — | 1 | 5.26 |
| CHEMBL4297507 | DELGOCITINIB | 3.0 | 1 | 5.24 |
| CHEMBL3693592 | — | — | 1 | 5.24 |
| CHEMBL4635108 | — | — | 1 | 5.23 |
| CHEMBL3689519 | — | — | 1 | 5.20 |
| CHEMBL3689524 | — | — | 1 | 5.07 |
| CHEMBL4649779 | — | — | 1 | - |
| CHEMBL3693625 | — | — | 1 | - |
| CHEMBL3969009 | — | — | 1 | - |
| CHEMBL4646093 | — | — | 1 | - |
| CHEMBL4638316 | — | — | 1 | - |
| CHEMBL4642854 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4646256 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL221959 | TOFACITINIB | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4639774 | — | IC50 | = | 340.0 | nM | 6.47 |
| CHEMBL4641927 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4639538 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4644221 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL3693624 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL3689514 | — | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL4636510 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL3689517 | — | IC50 | = | 2600.0 | nM | 5.58 |
| CHEMBL4634530 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3689515 | — | IC50 | = | 3700.0 | nM | 5.43 |
| CHEMBL3693620 | — | IC50 | = | 4100.0 | nM | 5.39 |
| CHEMBL4649366 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3693599 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL3689516 | — | IC50 | = | 4700.0 | nM | 5.33 |
| CHEMBL3693618 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3689522 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4638326 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL3693592 | — | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4297507 | DELGOCITINIB | IC50 | = | 5800.0 | nM | 5.24 |
| CHEMBL4635108 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL3689519 | — | IC50 | = | 6300.0 | nM | 5.20 |
| CHEMBL3689524 | — | IC50 | = | 8600.0 | nM | 5.07 |
| CHEMBL4634866 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1630770 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4635905 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4632930 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4644838 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4641433 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4636726 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4632573 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639875 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4637223 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643597 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4646425 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4640920 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3693596 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4639731 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3689526 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3693628 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4645444 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4643358 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3689518 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4642854 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4638316 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4646093 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3969009 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL3693625 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL4649779 | — | IC50 | > | 10000.0 | nM | - |