Assay Detail
Binding
CHEMBL3742598
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Rce1-mediated CaaX protease activity using ABZ-KSKTKC(farnesyl)QIIM and ABZ-KSKTKC(farnesyl)VIQI as substrate assessed as residual activity measured every 30 to 60 seconds for 60 mins
58
Total Activities
58
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
8-Hydroxyquinoline-based inhibitors of the Rce1 protease disrupt Ras membrane localization in human cells.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 58 | 5.11 | 5.42 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3741765 | — | — | 1 | 5.42 |
| CHEMBL3741937 | — | — | 1 | 5.41 |
| CHEMBL3740962 | — | — | 1 | 5.38 |
| CHEMBL3740249 | — | — | 1 | 5.31 |
| CHEMBL3742211 | — | — | 1 | 5.30 |
| CHEMBL3741101 | — | — | 1 | 5.28 |
| CHEMBL3741673 | — | — | 1 | 5.27 |
| CHEMBL3740203 | — | — | 1 | 5.17 |
| CHEMBL1979298 | — | — | 1 | 5.16 |
| CHEMBL3740563 | — | — | 1 | 5.15 |
| CHEMBL3740034 | — | — | 1 | 5.09 |
| CHEMBL2003928 | — | — | 1 | 5.06 |
| CHEMBL3741464 | — | — | 1 | 5.05 |
| CHEMBL3740606 | — | — | 1 | 5.03 |
| CHEMBL3740547 | — | — | 1 | 5.01 |
| CHEMBL2006267 | — | — | 1 | 4.96 |
| CHEMBL3739720 | — | — | 1 | 4.85 |
| CHEMBL3740917 | — | — | 1 | 4.80 |
| CHEMBL3739592 | — | — | 1 | 4.42 |
| CHEMBL3741914 | — | — | 1 | - |
| CHEMBL3740323 | — | — | 1 | - |
| CHEMBL3740282 | — | — | 1 | - |
| CHEMBL3741366 | — | — | 1 | - |
| CHEMBL3740198 | — | — | 1 | - |
| CHEMBL3739709 | — | — | 1 | - |
| CHEMBL3742035 | — | — | 1 | - |
| CHEMBL3742099 | — | — | 1 | - |
| CHEMBL3740306 | — | — | 1 | - |
| CHEMBL3741794 | — | — | 1 | - |
| CHEMBL3742344 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3741765 | — | IC50 | = | 3800.0 | nM | 5.42 |
| CHEMBL3741937 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL3740962 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL3740249 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL3742211 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL3741101 | — | IC50 | = | 5300.0 | nM | 5.28 |
| CHEMBL3741673 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL3740203 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL1979298 | — | IC50 | = | 6900.0 | nM | 5.16 |
| CHEMBL3740563 | — | IC50 | = | 7100.0 | nM | 5.15 |
| CHEMBL3740034 | — | IC50 | = | 8200.0 | nM | 5.09 |
| CHEMBL2003928 | — | IC50 | = | 8800.0 | nM | 5.06 |
| CHEMBL3741464 | — | IC50 | = | 8900.0 | nM | 5.05 |
| CHEMBL3740606 | — | IC50 | = | 9400.0 | nM | 5.03 |
| CHEMBL3740547 | — | IC50 | = | 9800.0 | nM | 5.01 |
| CHEMBL2006267 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3739720 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL3740917 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3739592 | — | IC50 | = | 38000.0 | nM | 4.42 |
| CHEMBL3742350 | — | IC50 | - | — | - | |
| CHEMBL3740657 | — | IC50 | - | — | - | |
| CHEMBL3739854 | — | IC50 | - | — | - | |
| CHEMBL3741515 | — | IC50 | - | — | - | |
| CHEMBL533917 | — | IC50 | - | — | - | |
| CHEMBL546448 | — | IC50 | - | — | - | |
| CHEMBL3741756 | — | IC50 | - | — | - | |
| CHEMBL3742049 | — | IC50 | - | — | - | |
| CHEMBL3740943 | — | IC50 | - | — | - | |
| CHEMBL3740666 | — | IC50 | - | — | - | |
| CHEMBL3740207 | — | IC50 | - | — | - | |
| CHEMBL3740240 | — | IC50 | - | — | - | |
| CHEMBL3740461 | — | IC50 | - | — | - | |
| CHEMBL3740613 | — | IC50 | - | — | - | |
| CHEMBL3739530 | — | IC50 | - | — | - | |
| CHEMBL3739589 | — | IC50 | - | — | - | |
| CHEMBL3740263 | — | IC50 | - | — | - | |
| CHEMBL3742401 | — | IC50 | - | — | - | |
| CHEMBL3740852 | — | IC50 | - | — | - | |
| CHEMBL3741402 | — | IC50 | - | — | - | |
| CHEMBL3742344 | — | IC50 | - | — | - | |
| CHEMBL3741794 | — | IC50 | - | — | - | |
| CHEMBL3740306 | — | IC50 | - | — | - | |
| CHEMBL3742099 | — | IC50 | - | — | - | |
| CHEMBL3742035 | — | IC50 | - | — | - | |
| CHEMBL3739709 | — | IC50 | - | — | - | |
| CHEMBL3740198 | — | IC50 | - | — | - | |
| CHEMBL3741366 | — | IC50 | - | — | - | |
| CHEMBL3740282 | — | IC50 | - | — | - | |
| CHEMBL3740323 | — | IC50 | - | — | - | |
| CHEMBL3741914 | — | IC50 | - | — | - |