Assay Detail
Binding
CHEMBL4835003
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Inhibition of SAE in human HCT116 cells assessed as redistribution of SUMO2/3 proteins from nucleus to cytosol preincubated for 2 hrs followed by compound washout and measured immediately by immunofluorescence assay
26
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 7 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Discovery of TAK-981, a First-in-Class Inhibitor of SUMO-Activating Enzyme for the Treatment of Cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 7.47 | 8.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4848140 | — | — | 1 | 8.40 |
| CHEMBL4848114 | — | — | 1 | 8.30 |
| CHEMBL4861509 | — | — | 1 | 8.15 |
| CHEMBL4848442 | — | — | 1 | 8.10 |
| CHEMBL4873956 | — | — | 1 | 8.05 |
| CHEMBL4849766 | — | — | 1 | 8.00 |
| CHEMBL4864361 | — | — | 1 | 7.80 |
| CHEMBL4852516 | — | — | 1 | 7.77 |
| CHEMBL4877684 | — | — | 1 | 7.77 |
| CHEMBL4858933 | — | — | 1 | 7.75 |
| CHEMBL4873487 | — | — | 1 | 7.72 |
| CHEMBL4850183 | — | — | 1 | 7.72 |
| CHEMBL4854038 | — | — | 1 | 7.72 |
| CHEMBL4870385 | — | — | 1 | 7.60 |
| CHEMBL4860917 | — | — | 1 | 7.54 |
| CHEMBL4862901 | — | — | 1 | 7.50 |
| CHEMBL4860263 | — | — | 2 | 7.37 |
| CHEMBL4855964 | — | — | 1 | 7.28 |
| CHEMBL4860960 | — | — | 1 | 7.18 |
| CHEMBL4862248 | — | — | 1 | 7.08 |
| CHEMBL4853360 | — | — | 1 | 6.85 |
| CHEMBL4856040 | — | — | 1 | 6.78 |
| CHEMBL4872222 | — | — | 1 | 6.74 |
| CHEMBL4878832 | — | — | 1 | 6.60 |
| CHEMBL4865157 | — | — | 1 | 6.44 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4848140 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4848114 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4861509 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4848442 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4873956 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4849766 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4864361 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4852516 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4877684 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4858933 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL4854038 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4873487 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4850183 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL4870385 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4860917 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4862901 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL4860263 | — | IC50 | = | 43.0 | nM | 7.37 |
| CHEMBL4855964 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4860960 | — | IC50 | = | 66.0 | nM | 7.18 |
| CHEMBL4862248 | — | IC50 | = | 83.0 | nM | 7.08 |
| CHEMBL4853360 | — | IC50 | = | 142.0 | nM | 6.85 |
| CHEMBL4856040 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL4872222 | — | IC50 | = | 184.0 | nM | 6.74 |
| CHEMBL4878832 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL4865157 | — | IC50 | = | 365.0 | nM | 6.44 |
| CHEMBL4860263 | — | IC50 | = | 1210.0 | nM | 5.92 |