Assay Detail
Binding
CHEMBL5316779
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of mTORC1 in human MDA-MB-468 cells assessed as reduction in AKT phosphorylation at Ser473 by AlphaLISA assay
33
Total Activities
33
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-468 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of RMC-5552, a Selective Bi-Steric Inhibitor of mTORC1, for the Treatment of mTORC1-Activated Tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 33 | 8.00 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5420034 | — | — | 1 | 9.28 |
| CHEMBL5429186 | — | — | 1 | 9.13 |
| CHEMBL5427995 | — | — | 1 | 8.85 |
| CHEMBL3545097 | SAPANISERTIB | 2.0 | 1 | 8.74 |
| CHEMBL5404497 | — | — | 1 | 8.74 |
| CHEMBL5413401 | — | — | 1 | 8.54 |
| CHEMBL5422165 | — | — | 1 | 8.51 |
| CHEMBL5418134 | — | — | 1 | 8.44 |
| CHEMBL5419721 | — | — | 1 | 8.33 |
| CHEMBL5404617 | — | — | 1 | 8.28 |
| CHEMBL5424277 | — | — | 1 | 8.17 |
| CHEMBL5434290 | — | — | 1 | 8.08 |
| CHEMBL5430111 | — | — | 1 | 8.06 |
| CHEMBL5441038 | — | — | 1 | 7.92 |
| CHEMBL5422229 | — | — | 1 | 7.89 |
| CHEMBL5430354 | — | — | 1 | 7.77 |
| CHEMBL5440792 | — | — | 1 | 7.75 |
| CHEMBL5422529 | — | — | 1 | 7.72 |
| CHEMBL5425648 | — | — | 1 | 7.62 |
| CHEMBL5419762 | — | — | 1 | 7.48 |
| CHEMBL5399980 | — | — | 1 | 7.46 |
| CHEMBL5314926 | RMC-5552 | 1.0 | 1 | 7.46 |
| CHEMBL1241674 | — | — | 1 | 7.42 |
| CHEMBL5408375 | — | — | 1 | 6.96 |
| CHEMBL5416606 | — | — | 1 | 6.92 |
| CHEMBL5428156 | — | — | 1 | 6.35 |
| CHEMBL1908360 | EVEROLIMUS | 4.0 | 1 | - |
| CHEMBL5431157 | — | — | 1 | - |
| CHEMBL5418335 | — | — | 1 | - |
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5420034 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL5429186 | — | IC50 | = | 0.74 | nM | 9.13 |
| CHEMBL5427995 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3545097 | SAPANISERTIB | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5404497 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL5413401 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL5422165 | — | IC50 | = | 3.1 | nM | 8.51 |
| CHEMBL5418134 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL5419721 | — | IC50 | = | 4.7 | nM | 8.33 |
| CHEMBL5404617 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL5424277 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL5434290 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL5430111 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL5441038 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL5422229 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL5430354 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL5440792 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL5422529 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5425648 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5419762 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL5399980 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5314926 | RMC-5552 | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL1241674 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5408375 | — | IC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5416606 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5428156 | — | IC50 | = | 450.0 | nM | 6.35 |
| CHEMBL1908360 | EVEROLIMUS | IC50 | > | 1000.0 | nM | - |
| CHEMBL5431157 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5418335 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | IC50 | > | 1000.0 | nM | - |
| CHEMBL5417140 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1081312 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5394998 | — | IC50 | > | 1000.0 | nM | - |