Assay Detail
Binding
CHEMBL5316778
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 4EBP1 phosphorylation at Thr37/46 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 | 7 — Homologous single protein target |
| 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 | 8.55 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5420034 | — | — | 1 | 10.22 |
| CHEMBL5429186 | — | — | 1 | 10.10 |
| CHEMBL5419721 | — | — | 1 | 9.38 |
| CHEMBL5441038 | — | — | 1 | 9.36 |
| CHEMBL5430111 | — | — | 1 | 9.36 |
| CHEMBL5422529 | — | — | 1 | 9.32 |
| CHEMBL5404497 | — | — | 1 | 9.17 |
| CHEMBL5413401 | — | — | 1 | 9.15 |
| CHEMBL5399980 | — | — | 1 | 9.01 |
| CHEMBL5430354 | — | — | 1 | 9.00 |
| CHEMBL5422165 | — | — | 1 | 8.96 |
| CHEMBL5404617 | — | — | 1 | 8.96 |
| CHEMBL5422229 | — | — | 1 | 8.89 |
| CHEMBL5434290 | — | — | 1 | 8.85 |
| CHEMBL5440792 | — | — | 1 | 8.85 |
| CHEMBL5314926 | RMC-5552 | 1.0 | 1 | 8.80 |
| CHEMBL5418134 | — | — | 1 | 8.77 |
| CHEMBL5424277 | — | — | 1 | 8.77 |
| CHEMBL5425648 | — | — | 1 | 8.60 |
| CHEMBL5427995 | — | — | 1 | 8.36 |
| CHEMBL3545097 | SAPANISERTIB | 2.0 | 1 | 7.72 |
| CHEMBL5419762 | — | — | 1 | 7.60 |
| CHEMBL5408375 | — | — | 1 | 7.51 |
| CHEMBL5428156 | — | — | 1 | 6.75 |
| CHEMBL5417140 | — | — | 1 | 6.50 |
| CHEMBL1241674 | — | — | 1 | 6.50 |
| CHEMBL5416606 | — | — | 1 | 6.43 |
| CHEMBL1908360 | EVEROLIMUS | 4.0 | 1 | - |
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | - |
| CHEMBL5418335 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5420034 | — | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL5429186 | — | IC50 | = | 0.08 | nM | 10.10 |
| CHEMBL5419721 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL5441038 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL5430111 | — | IC50 | = | 0.44 | nM | 9.36 |
| CHEMBL5422529 | — | IC50 | = | 0.48 | nM | 9.32 |
| CHEMBL5404497 | — | IC50 | = | 0.67 | nM | 9.17 |
| CHEMBL5413401 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL5399980 | — | IC50 | = | 0.97 | nM | 9.01 |
| CHEMBL5430354 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL5422165 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5404617 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL5422229 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL5434290 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5440792 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL5314926 | RMC-5552 | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL5418134 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5424277 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL5425648 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL5427995 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL3545097 | SAPANISERTIB | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5419762 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL5408375 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL5428156 | — | IC50 | = | 180.0 | nM | 6.75 |
| CHEMBL5417140 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL1241674 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5416606 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL1908360 | EVEROLIMUS | IC50 | > | 1000.0 | nM | - |
| CHEMBL413 | SIROLIMUS | IC50 | > | 1000.0 | nM | - |
| CHEMBL5418335 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5431157 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL5394998 | — | IC50 | > | 1000.0 | nM | - |
| CHEMBL1081312 | — | IC50 | > | 1000.0 | nM | - |