Assay Detail
Binding
CHEMBL4052447
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Binding affinity to human N-terminal MDM2 (1 to 118 residues) expressed in Escherichia coli BL21 (DE3) after 15 mins in presence of 5-FAM-LTFEHYWAQLTS by FP assay
29
Total Activities
29
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
1,4,5-Trisubstituted Imidazole-Based p53-MDM2/MDMX Antagonists with Aliphatic Linkers for Conjugation with Biological Carriers.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 29 | 6.95 | 8.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4078749 | — | — | 1 | 8.22 |
| CHEMBL4084081 | — | — | 1 | 8.10 |
| CHEMBL4085272 | — | — | 1 | 7.82 |
| CHEMBL4077617 | — | — | 1 | 7.77 |
| CHEMBL4098976 | — | — | 1 | 7.68 |
| CHEMBL4072678 | — | — | 1 | 7.64 |
| CHEMBL4099580 | — | — | 1 | 7.42 |
| CHEMBL4091842 | — | — | 1 | 7.42 |
| CHEMBL4104110 | — | — | 1 | 7.27 |
| CHEMBL4093959 | — | — | 1 | 7.24 |
| CHEMBL4063649 | — | — | 1 | 7.23 |
| CHEMBL4089364 | — | — | 1 | 7.22 |
| CHEMBL4086204 | — | — | 1 | 7.01 |
| CHEMBL4081423 | — | — | 1 | 6.92 |
| CHEMBL4067165 | — | — | 1 | 6.80 |
| CHEMBL4096776 | — | — | 1 | 6.65 |
| CHEMBL4104786 | — | — | 1 | 6.49 |
| CHEMBL4096099 | — | — | 1 | 6.36 |
| CHEMBL4094325 | — | — | 1 | 6.18 |
| CHEMBL4064085 | — | — | 1 | 5.64 |
| CHEMBL4066410 | — | — | 1 | 5.22 |
| CHEMBL4102063 | — | — | 1 | 4.55 |
| CHEMBL4088498 | — | — | 1 | - |
| CHEMBL4060276 | — | — | 1 | - |
| CHEMBL4073720 | — | — | 1 | - |
| CHEMBL4075565 | — | — | 1 | - |
| CHEMBL4068179 | — | — | 1 | - |
| CHEMBL4071052 | — | — | 1 | - |
| CHEMBL4086907 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4078749 | — | Ki | = | 6.0 | nM | 8.22 |
| CHEMBL4084081 | — | Ki | = | 8.0 | nM | 8.10 |
| CHEMBL4085272 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL4077617 | — | Ki | = | 17.0 | nM | 7.77 |
| CHEMBL4098976 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL4072678 | — | Ki | = | 23.0 | nM | 7.64 |
| CHEMBL4099580 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4091842 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL4104110 | — | Ki | = | 54.0 | nM | 7.27 |
| CHEMBL4093959 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL4063649 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL4089364 | — | Ki | = | 60.0 | nM | 7.22 |
| CHEMBL4086204 | — | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL4081423 | — | Ki | = | 121.0 | nM | 6.92 |
| CHEMBL4067165 | — | Ki | = | 157.0 | nM | 6.80 |
| CHEMBL4096776 | — | Ki | = | 225.0 | nM | 6.65 |
| CHEMBL4104786 | — | Ki | = | 322.0 | nM | 6.49 |
| CHEMBL4096099 | — | Ki | = | 433.0 | nM | 6.36 |
| CHEMBL4094325 | — | Ki | = | 656.0 | nM | 6.18 |
| CHEMBL4064085 | — | Ki | = | 2310.0 | nM | 5.64 |
| CHEMBL4066410 | — | Ki | = | 6020.0 | nM | 5.22 |
| CHEMBL4102063 | — | Ki | = | 28000.0 | nM | 4.55 |
| CHEMBL4088498 | — | Ki | - | — | - | |
| CHEMBL4060276 | — | Ki | - | — | - | |
| CHEMBL4073720 | — | Ki | - | — | - | |
| CHEMBL4075565 | — | Ki | - | — | - | |
| CHEMBL4068179 | — | Ki | - | — | - | |
| CHEMBL4071052 | — | Ki | - | — | - | |
| CHEMBL4086907 | — | Ki | - | — | - |