Assay Detail
Binding
CHEMBL5043746
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human SGK1 expressed in baculovirus expression system using 5-carboxyfluorescein -RPRAATF-NH2 as substrate preincubated for 30 mins followed by substrate addition in presence of 500 uM ATP and measured after 60 mins by microfluidics assay
56
Total Activities
56
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 |
Target
Serine/threonine-protein kinase Sgk1 (CHEMBL2343) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Rational Design of Highly Potent, Selective, and Bioavailable SGK1 Protein Kinase Inhibitors for the Treatment of Osteoarthritis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 56 | 7.45 | 9.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5074684 | — | — | 1 | 9.00 |
| CHEMBL5081869 | — | — | 1 | 9.00 |
| CHEMBL5083625 | — | — | 1 | 9.00 |
| CHEMBL5070612 | — | — | 1 | 9.00 |
| CHEMBL5085476 | — | — | 1 | 9.00 |
| CHEMBL5087162 | — | — | 1 | 9.00 |
| CHEMBL5071544 | — | — | 1 | 8.70 |
| CHEMBL5088069 | — | — | 1 | 8.70 |
| CHEMBL3355029 | — | — | 1 | 8.52 |
| CHEMBL5094921 | — | — | 1 | 8.52 |
| CHEMBL5081330 | — | — | 1 | 8.52 |
| CHEMBL5083859 | — | — | 1 | 8.40 |
| CHEMBL5077971 | — | — | 1 | 8.40 |
| CHEMBL5077848 | — | — | 1 | 8.40 |
| CHEMBL5093302 | — | — | 1 | 8.40 |
| CHEMBL5083614 | — | — | 1 | 8.30 |
| CHEMBL5086320 | — | — | 1 | 8.30 |
| CHEMBL5082336 | — | — | 1 | 8.05 |
| CHEMBL5093411 | — | — | 1 | 8.00 |
| CHEMBL5081823 | — | — | 1 | 7.96 |
| CHEMBL5093306 | — | — | 1 | 7.92 |
| CHEMBL5085315 | — | — | 1 | 7.85 |
| CHEMBL5083477 | — | — | 1 | 7.75 |
| CHEMBL5084696 | — | — | 1 | 7.68 |
| CHEMBL5080922 | — | — | 1 | 7.62 |
| CHEMBL3356044 | — | — | 1 | 7.47 |
| CHEMBL5087657 | — | — | 1 | 7.46 |
| CHEMBL5074701 | — | — | 1 | 7.42 |
| CHEMBL5082604 | — | — | 1 | 7.40 |
| CHEMBL5071556 | — | — | 1 | 7.35 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5074684 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5087162 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5085476 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5070612 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5081869 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5083625 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5071544 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL5088069 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3355029 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5094921 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5081330 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL5083859 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5077971 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5077848 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5093302 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL5083614 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5086320 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL5082336 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL5093411 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5081823 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5093306 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5085315 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL5083477 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5084696 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL5080922 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3356044 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL5087657 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5074701 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5082604 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5071556 | — | IC50 | = | 45.0 | nM | 7.35 |
| CHEMBL5075362 | — | IC50 | = | 107.0 | nM | 6.97 |
| CHEMBL5090286 | — | IC50 | = | 109.0 | nM | 6.96 |
| CHEMBL5079183 | — | IC50 | = | 128.0 | nM | 6.89 |
| CHEMBL5090299 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL5075992 | — | IC50 | = | 236.0 | nM | 6.63 |
| CHEMBL5083393 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL5079143 | — | IC50 | = | 265.0 | nM | 6.58 |
| CHEMBL5081215 | — | IC50 | = | 327.0 | nM | 6.49 |
| CHEMBL3092460 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL5075203 | — | IC50 | = | 438.0 | nM | 6.36 |
| CHEMBL5086767 | — | IC50 | = | 609.0 | nM | 6.21 |
| CHEMBL5079781 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL5083285 | — | IC50 | = | 633.0 | nM | 6.20 |
| CHEMBL5094428 | — | IC50 | = | 813.0 | nM | 6.09 |
| CHEMBL5078693 | — | IC50 | = | 929.0 | nM | 6.03 |
| CHEMBL5093575 | — | IC50 | = | 963.0 | nM | 6.02 |
| CHEMBL5087068 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL5071460 | — | IC50 | = | 1280.0 | nM | 5.89 |
| CHEMBL5093744 | — | IC50 | = | 2470.0 | nM | 5.61 |
| CHEMBL5084905 | — | IC50 | = | 17600.0 | nM | 4.75 |