Assay Detail
Binding
CHEMBL5116484
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Inhibition of PSMA in human LNCaP cell extracts using NAAG as substrate by amplex red reagent based assay
17
Total Activities
17
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
Synthesis and initial in vitro evaluation of PSMA-targeting ligands with a modified aromatic moiety at the lysine ε-nitrogen atom.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 17 | 7.56 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5205430 | — | — | 1 | 8.82 |
| CHEMBL5202039 | — | — | 1 | 8.68 |
| CHEMBL5204026 | — | — | 1 | 8.15 |
| CHEMBL596351 | — | — | 1 | 7.96 |
| CHEMBL5182529 | — | — | 1 | 7.80 |
| CHEMBL5204600 | — | — | 1 | 7.72 |
| CHEMBL5187511 | — | — | 1 | 7.64 |
| CHEMBL5171332 | — | — | 1 | 7.64 |
| CHEMBL5184954 | — | — | 1 | 7.62 |
| CHEMBL5183648 | — | — | 1 | 7.46 |
| CHEMBL5202319 | — | — | 1 | 7.42 |
| CHEMBL5182330 | — | — | 1 | 7.29 |
| CHEMBL189217 | — | — | 1 | 7.10 |
| CHEMBL5206416 | — | — | 1 | 7.06 |
| CHEMBL5194802 | — | — | 1 | 7.00 |
| CHEMBL5203501 | — | — | 1 | 6.95 |
| CHEMBL458202 | — | — | 1 | 6.26 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5205430 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL5202039 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL5204026 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL596351 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5182529 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL5204600 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL5187511 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5171332 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL5184954 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL5183648 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5202319 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL5182330 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL189217 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5206416 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL5194802 | — | IC50 | = | 101.0 | nM | 7.00 |
| CHEMBL5203501 | — | IC50 | = | 112.0 | nM | 6.95 |
| CHEMBL458202 | — | IC50 | = | 547.0 | nM | 6.26 |