Assay Detail
Binding
CHEMBL5375111
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Inhibition of GST-fused JAK1 (866 to 1154 residues)(unknown origin) using FITC-Ahr-KKSRGDYMTMQIG-NH2 peptide as substrate incubated for 30 mins in presence of ATP by caliper microfluidic mobility shift assay
17
Total Activities
17
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
Design of a Supersoft Topical JAK Inhibitor, Which Is Effective in Human Skin but Rapidly Deactivated in Blood.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.71 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5412967 | — | — | 1 | 9.00 |
| CHEMBL5407260 | — | — | 1 | 8.52 |
| CHEMBL5396554 | — | — | 1 | 8.30 |
| CHEMBL5404574 | — | — | 1 | 8.30 |
| CHEMBL5407329 | — | — | 1 | 8.30 |
| CHEMBL5422886 | — | — | 1 | 8.22 |
| CHEMBL5431257 | — | — | 1 | 8.05 |
| CHEMBL5409953 | — | — | 1 | 8.05 |
| CHEMBL5420083 | — | — | 1 | 7.72 |
| CHEMBL5403897 | — | — | 1 | 7.70 |
| CHEMBL5417474 | — | — | 1 | 7.57 |
| CHEMBL5424439 | — | — | 1 | 7.54 |
| CHEMBL5270549 | — | — | 1 | 7.30 |
| CHEMBL5395839 | — | — | 1 | 7.16 |
| CHEMBL5420971 | — | — | 1 | 6.92 |
| CHEMBL5279787 | — | — | 1 | 6.88 |
| CHEMBL5271559 | — | — | 1 | 5.49 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5412967 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5407260 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5396554 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5404574 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5407329 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5422886 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL5431257 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5409953 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5420083 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5403897 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5417474 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL5424439 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL5270549 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5395839 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL5420971 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5279787 | — | IC50 | = | 131.0 | nM | 6.88 |
| CHEMBL5271559 | — | IC50 | = | 3272.0 | nM | 5.49 |