Assay Detail
Binding
CHEMBL4154039
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Binding affinity to N-terminal His6-tagged p53 DNA binding domain Y220C mutant (94 to 312 residues) (unknown origin) expressed in Escherichia coli C41 by ITC
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Aminobenzothiazole derivatives stabilize the thermolabile p53 cancer mutant Y220C and show anticancer activity in p53-Y220C cell lines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 20 | 4.54 | 5.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4162051 | — | — | 1 | 5.40 |
| CHEMBL4168439 | — | — | 1 | 4.85 |
| CHEMBL4165245 | — | — | 1 | 4.68 |
| CHEMBL4168045 | — | — | 1 | 4.66 |
| CHEMBL4176302 | — | — | 1 | 4.52 |
| CHEMBL4164612 | — | — | 1 | 4.52 |
| CHEMBL4168664 | — | — | 1 | 4.52 |
| CHEMBL4160123 | — | — | 1 | 4.48 |
| CHEMBL4164831 | — | — | 1 | 4.30 |
| CHEMBL4175464 | — | — | 1 | 4.22 |
| CHEMBL4163490 | — | — | 1 | 4.20 |
| CHEMBL4176523 | — | — | 1 | 4.16 |
| CHEMBL4171387 | — | — | 1 | - |
| CHEMBL4168268 | — | — | 1 | - |
| CHEMBL4160358 | — | — | 1 | - |
| CHEMBL4161418 | — | — | 1 | - |
| CHEMBL4171145 | — | — | 1 | - |
| CHEMBL4175243 | — | — | 1 | - |
| CHEMBL4161192 | — | — | 1 | - |
| CHEMBL4171798 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4162051 | — | Kd | = | 4000.0 | nM | 5.40 |
| CHEMBL4168439 | — | Kd | = | 14000.0 | nM | 4.85 |
| CHEMBL4165245 | — | Kd | = | 21000.0 | nM | 4.68 |
| CHEMBL4168045 | — | Kd | = | 22000.0 | nM | 4.66 |
| CHEMBL4176302 | — | Kd | = | 30000.0 | nM | 4.52 |
| CHEMBL4164612 | — | Kd | = | 30000.0 | nM | 4.52 |
| CHEMBL4168664 | — | Kd | = | 30000.0 | nM | 4.52 |
| CHEMBL4160123 | — | Kd | = | 33000.0 | nM | 4.48 |
| CHEMBL4164831 | — | Kd | = | 50000.0 | nM | 4.30 |
| CHEMBL4175464 | — | Kd | = | 60000.0 | nM | 4.22 |
| CHEMBL4163490 | — | Kd | = | 63000.0 | nM | 4.20 |
| CHEMBL4176523 | — | Kd | = | 70000.0 | nM | 4.16 |
| CHEMBL4171387 | — | Kd | = | 122000.0 | nM | - |
| CHEMBL4168268 | — | Kd | = | 113000.0 | nM | - |
| CHEMBL4160358 | — | Kd | = | 306000.0 | nM | - |
| CHEMBL4161418 | — | Kd | = | 139000.0 | nM | - |
| CHEMBL4171145 | — | Kd | - | — | - | |
| CHEMBL4175243 | — | Kd | = | 108000.0 | nM | - |
| CHEMBL4161192 | — | Kd | = | 726000.0 | nM | - |
| CHEMBL4171798 | — | Kd | = | 116000.0 | nM | - |