Assay Detail
Binding
CHEMBL861259
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human Pin1 PPIase Activity by protease free PPIase assay
21
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (CHEMBL2288) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Nanomolar inhibitors of the peptidyl prolyl cis/trans isomerase Pin1 from combinatorial peptide libraries.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 4.96 | 6.68 |
| Ki | 6 | 7.43 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL219531 | — | — | 1 | 8.92 |
| CHEMBL438271 | — | — | 2 | 8.32 |
| CHEMBL436759 | — | — | 1 | 7.74 |
| CHEMBL441398 | — | — | 2 | 6.74 |
| CHEMBL380685 | — | — | 1 | 6.59 |
| CHEMBL383244 | — | — | 1 | 6.26 |
| CHEMBL219523 | — | — | 1 | 5.16 |
| CHEMBL414584 | — | — | 1 | 5.10 |
| CHEMBL411584 | — | — | 1 | 5.00 |
| CHEMBL405287 | — | — | 1 | 4.82 |
| CHEMBL425273 | — | — | 1 | 4.82 |
| CHEMBL219287 | — | — | 1 | 4.70 |
| CHEMBL413855 | — | — | 1 | 4.70 |
| CHEMBL268078 | — | — | 1 | 4.66 |
| CHEMBL437349 | — | — | 1 | 4.60 |
| CHEMBL558539 | — | — | 1 | 4.52 |
| CHEMBL218960 | — | — | 1 | - |
| CHEMBL267945 | — | — | 1 | - |
| CHEMBL440637 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL219531 | — | Ki | = | 1.2 | nM | 8.92 |
| CHEMBL438271 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL436759 | — | Ki | = | 18.3 | nM | 7.74 |
| CHEMBL441398 | — | Ki | = | 183.0 | nM | 6.74 |
| CHEMBL441398 | — | IC50 | = | 210.0 | nM | 6.68 |
| CHEMBL380685 | — | Ki | = | 258.0 | nM | 6.59 |
| CHEMBL383244 | — | Ki | = | 547.0 | nM | 6.26 |
| CHEMBL219523 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL414584 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL411584 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL405287 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL425273 | — | IC50 | = | 15000.0 | nM | 4.82 |
| CHEMBL438271 | — | IC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL413855 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL219287 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL268078 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL437349 | — | IC50 | = | 25000.0 | nM | 4.60 |
| CHEMBL558539 | — | IC50 | = | 30000.0 | nM | 4.52 |
| CHEMBL218960 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL267945 | — | IC50 | > | 50000.0 | nM | - |
| CHEMBL440637 | — | IC50 | > | 50000.0 | nM | - |