Assay Detail
Binding
CHEMBL5316781
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of Cy5 modified rapamycin from GST tagged FKBP12 (1 to 108 residues) (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 6 hrs by fluorescence plate reader analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| 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 |
|---|---|---|---|
| Kd | 3 | 7.80 | 9.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL413 | SIROLIMUS | 4.0 | 1 | 9.36 |
| CHEMBL5418335 | — | — | 1 | 7.88 |
| CHEMBL5431157 | — | — | 1 | 6.15 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL413 | SIROLIMUS | Kd | = | 0.44 | nM | 9.36 |
| CHEMBL5418335 | — | Kd | = | 13.3 | nM | 7.88 |
| CHEMBL5431157 | — | Kd | = | 701.0 | nM | 6.15 |