Assay Detail
Binding
CHEMBL5253198
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Binding affinity to PSMA in human LNCaP cells after 45 mins in presence of 68Ga-labeled PSMA-10 by gamma counting assay
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | LNCaP |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Linker Modification Strategies To Control the Prostate-Specific Membrane Antigen (PSMA)-Targeting and Pharmacokinetic Properties of DOTA-Conjugated PSMA Inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 19 | 8.18 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5283285 | — | — | 1 | 9.30 |
| CHEMBL5270513 | — | — | 1 | 9.28 |
| CHEMBL5275438 | — | — | 1 | 8.74 |
| CHEMBL5279851 | — | — | 1 | 8.71 |
| CHEMBL4594280 | VIPIVOTIDE TETRAXETAN | 2.0 | 1 | 8.63 |
| CHEMBL5279511 | — | — | 1 | 8.21 |
| CHEMBL5287113 | — | — | 1 | 8.20 |
| CHEMBL5268818 | — | — | 1 | 8.12 |
| CHEMBL5268703 | — | — | 1 | 8.05 |
| CHEMBL5284385 | — | — | 1 | 8.03 |
| CHEMBL3578202 | GOZETOTIDE | 4.0 | 1 | 7.92 |
| CHEMBL5282249 | — | — | 1 | 7.89 |
| CHEMBL5289867 | — | — | 1 | 7.82 |
| CHEMBL5267599 | — | — | 1 | 7.75 |
| CHEMBL5281545 | — | — | 1 | 7.71 |
| CHEMBL5272927 | — | — | 1 | 7.68 |
| CHEMBL5269260 | — | — | 1 | 7.61 |
| CHEMBL5274946 | — | — | 1 | 7.54 |
| CHEMBL5279223 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5283285 | — | Ki | = | 0.5 | nM | 9.30 |
| CHEMBL5270513 | — | Ki | = | 0.53 | nM | 9.28 |
| CHEMBL5275438 | — | Ki | = | 1.81 | nM | 8.74 |
| CHEMBL5279851 | — | Ki | = | 1.97 | nM | 8.71 |
| CHEMBL4594280 | VIPIVOTIDE TETRAXETAN | Ki | = | 2.34 | nM | 8.63 |
| CHEMBL5279511 | — | Ki | = | 6.19 | nM | 8.21 |
| CHEMBL5287113 | — | Ki | = | 6.31 | nM | 8.20 |
| CHEMBL5268818 | — | Ki | = | 7.51 | nM | 8.12 |
| CHEMBL5268703 | — | Ki | = | 8.86 | nM | 8.05 |
| CHEMBL5284385 | — | Ki | = | 9.33 | nM | 8.03 |
| CHEMBL3578202 | GOZETOTIDE | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL5282249 | — | Ki | = | 12.78 | nM | 7.89 |
| CHEMBL5289867 | — | Ki | = | 15.31 | nM | 7.82 |
| CHEMBL5267599 | — | Ki | = | 17.7 | nM | 7.75 |
| CHEMBL5281545 | — | Ki | = | 19.4 | nM | 7.71 |
| CHEMBL5272927 | — | Ki | = | 20.96 | nM | 7.68 |
| CHEMBL5269260 | — | Ki | = | 24.71 | nM | 7.61 |
| CHEMBL5274946 | — | Ki | = | 28.6 | nM | 7.54 |
| CHEMBL5279223 | — | Ki | - | — | - |