Assay Detail
Binding
CHEMBL3375441
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human SGK1 using fluo-5(6)-carboxyfluorescein)-RPRAATF-NH2 fluorescently labeled peptide by substrate phosphorylation assay in presence of 500 uM ATP
54
Total Activities
54
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
Discovery of N-[4-(1H-Pyrazolo[3,4-b]pyrazin-6-yl)-phenyl]-sulfonamides as Highly Active and Selective SGK1 Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 54 | 6.65 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3356034 | — | — | 1 | 8.40 |
| CHEMBL3356050 | — | — | 1 | 8.40 |
| CHEMBL3356035 | — | — | 1 | 8.22 |
| CHEMBL3356037 | — | — | 1 | 8.15 |
| CHEMBL3356059 | — | — | 1 | 7.96 |
| CHEMBL3092463 | — | — | 1 | 7.89 |
| CHEMBL3356025 | — | — | 1 | 7.85 |
| CHEMBL3356028 | — | — | 1 | 7.77 |
| CHEMBL3092461 | — | — | 1 | 7.60 |
| CHEMBL3092466 | — | — | 1 | 7.54 |
| CHEMBL3092467 | — | — | 1 | 7.47 |
| CHEMBL3356044 | — | — | 1 | 7.47 |
| CHEMBL3356049 | — | — | 1 | 7.41 |
| CHEMBL3356053 | — | — | 1 | 7.40 |
| CHEMBL3356048 | — | — | 1 | 7.39 |
| CHEMBL3092468 | — | — | 1 | 7.39 |
| CHEMBL3092462 | — | — | 1 | 7.30 |
| CHEMBL3356033 | — | — | 1 | 7.29 |
| CHEMBL3356052 | — | — | 1 | 7.21 |
| CHEMBL3356021 | — | — | 1 | 7.20 |
| CHEMBL3092464 | — | — | 1 | 7.06 |
| CHEMBL3356029 | — | — | 1 | 6.89 |
| CHEMBL3356060 | — | — | 1 | 6.82 |
| CHEMBL3356036 | — | — | 1 | 6.77 |
| CHEMBL3356039 | — | — | 1 | 6.74 |
| CHEMBL3356054 | — | — | 1 | 6.74 |
| CHEMBL3356032 | — | — | 1 | 6.73 |
| CHEMBL3356026 | — | — | 1 | 6.70 |
| CHEMBL3356024 | — | — | 1 | 6.58 |
| CHEMBL3356051 | — | — | 1 | 6.53 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3356034 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3356050 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL3356035 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3356037 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3356059 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3092463 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3356025 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3356028 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3092461 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL3092466 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3092467 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3356044 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL3356049 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3356053 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3092468 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3356048 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL3092462 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3356033 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3356052 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL3356021 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL3092464 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL3356029 | — | IC50 | = | 129.0 | nM | 6.89 |
| CHEMBL3356060 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL3356036 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL3356054 | — | IC50 | = | 182.0 | nM | 6.74 |
| CHEMBL3356039 | — | IC50 | = | 183.0 | nM | 6.74 |
| CHEMBL3356032 | — | IC50 | = | 186.0 | nM | 6.73 |
| CHEMBL3356026 | — | IC50 | = | 199.0 | nM | 6.70 |
| CHEMBL3356024 | — | IC50 | = | 261.0 | nM | 6.58 |
| CHEMBL3356051 | — | IC50 | = | 293.0 | nM | 6.53 |
| CHEMBL3356023 | — | IC50 | = | 396.0 | nM | 6.40 |
| CHEMBL3092460 | — | IC50 | = | 442.0 | nM | 6.36 |
| CHEMBL3356019 | — | IC50 | = | 518.0 | nM | 6.29 |
| CHEMBL3092465 | — | IC50 | = | 580.0 | nM | 6.24 |
| CHEMBL3356058 | — | IC50 | = | 605.0 | nM | 6.22 |
| CHEMBL3356040 | — | IC50 | = | 639.0 | nM | 6.19 |
| CHEMBL3356047 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL3356018 | — | IC50 | = | 718.0 | nM | 6.14 |
| CHEMBL3356038 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL3356041 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3356030 | — | IC50 | = | 1110.0 | nM | 5.96 |
| CHEMBL3356042 | — | IC50 | = | 1260.0 | nM | 5.90 |
| CHEMBL3356061 | — | IC50 | = | 1340.0 | nM | 5.87 |
| CHEMBL3356046 | — | IC50 | = | 1490.0 | nM | 5.83 |
| CHEMBL3356027 | — | IC50 | = | 1970.0 | nM | 5.71 |
| CHEMBL3356031 | — | IC50 | = | 2580.0 | nM | 5.59 |
| CHEMBL3356056 | — | IC50 | = | 3330.0 | nM | 5.48 |
| CHEMBL3356055 | — | IC50 | = | 4550.0 | nM | 5.34 |
| CHEMBL3356043 | — | IC50 | = | 4760.0 | nM | 5.32 |
| CHEMBL3356057 | — | IC50 | = | 5730.0 | nM | 5.24 |