Assay Detail
Binding
CHEMBL3706340
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Time Resolved Fluorescence Energy Transfer (TR-FRET) Assay: The inhibition of p53-MDM2 and p53-MDM4 interactions is measured by time resolved fluorescence energy transfer (TR-FRET). Fluorescence energy transfer (or Foerster resonance energy transfer) describes an energy transfer between donor and acceptor fluorescent molecules. For this assay, human MDM2 protein (amino acids 2-188) and human MDM4 protein (amino acids 2-185), tagged with a C-terminal biotin moiety, are used in combination with a Europium labeled streptavidin (Perkin Elmer, Inc., Waltham, MA, USA) serving as the donor fluorophore. The p53 derived, Cy5 labeled peptide Cy5-TFSDLWKLL (p53 aa18-26) is the energy acceptor. Upon excitation of the donor molecule at 340nm, binding interaction between MDM2 or MDM4 and the p53 peptide induces energy transfer and enhanced response at the acceptor emission wavelength at 665 nm.
134
Total Activities
133
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
Pyrazolopyrrolidine compounds
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 134 | 8.28 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3691739 | — | — | 1 | 9.30 |
| CHEMBL3691737 | — | — | 1 | 9.22 |
| CHEMBL3691776 | — | — | 1 | 9.22 |
| CHEMBL3691772 | — | — | 1 | 9.15 |
| CHEMBL3687268 | — | — | 1 | 9.15 |
| CHEMBL3687307 | — | — | 1 | 8.96 |
| CHEMBL3691710 | — | — | 1 | 8.96 |
| CHEMBL3691709 | — | — | 1 | 8.96 |
| CHEMBL3687312 | — | — | 1 | 8.96 |
| CHEMBL3691708 | — | — | 1 | 8.96 |
| CHEMBL3687275 | — | — | 1 | 8.96 |
| CHEMBL3691706 | — | — | 1 | 8.92 |
| CHEMBL3691722 | — | — | 1 | 8.92 |
| CHEMBL3691704 | — | — | 1 | 8.89 |
| CHEMBL3691696 | — | — | 1 | 8.89 |
| CHEMBL3687250 | — | — | 1 | 8.85 |
| CHEMBL3691695 | — | — | 1 | 8.82 |
| CHEMBL3687277 | — | — | 1 | 8.82 |
| CHEMBL3687316 | — | — | 1 | 8.80 |
| CHEMBL3687276 | — | — | 1 | 8.80 |
| CHEMBL3691721 | — | — | 1 | 8.77 |
| CHEMBL3687271 | — | — | 1 | 8.77 |
| CHEMBL3687315 | — | — | 1 | 8.77 |
| CHEMBL3691703 | — | — | 1 | 8.77 |
| CHEMBL3691720 | — | — | 1 | 8.74 |
| CHEMBL3691698 | — | — | 1 | 8.74 |
| CHEMBL3687292 | — | — | 1 | 8.74 |
| CHEMBL3687310 | — | — | 1 | 8.72 |
| CHEMBL3691694 | — | — | 1 | 8.72 |
| CHEMBL3691697 | — | — | 1 | 8.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3691739 | — | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL3691737 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3691776 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL3691772 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3687268 | — | IC50 | = | 0.7 | nM | 9.15 |
| CHEMBL3687275 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3687312 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3687307 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3691709 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3691708 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3691710 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL3691706 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3691722 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL3691704 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3691696 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL3687250 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL3691695 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3687277 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL3687316 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3687276 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL3687271 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3691703 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3687315 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3691721 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL3691698 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3687292 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3691720 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL3691694 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3687310 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL3687293 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3687266 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3691697 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3691702 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3691715 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3687249 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3691700 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL3687253 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3687251 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3691705 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL3687311 | — | IC50 | = | 2.3 | nM | 8.64 |
| CHEMBL3687248 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL3691718 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3687267 | — | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL3691735 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3687306 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3687262 | — | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL3687273 | — | IC50 | = | 2.7 | nM | 8.57 |
| CHEMBL3687244 | — | IC50 | = | 2.8 | nM | 8.55 |
| CHEMBL3691701 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL3687245 | — | IC50 | = | 2.9 | nM | 8.54 |