Assay Detail
Binding
CHEMBL4266977
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal His6-tagged human Pin1 using Suc-Ala-Glu-cis-Pro-Phe-4-nitroanilide as substrate preincubated for 30 mins followed by substrate addition measured for 90 secs
11
Total Activities
11
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 |
Target
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (CHEMBL2288) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Design, synthesis and biological evaluation of ring A modified 11-keto-boswellic acid derivatives as Pin1 inhibitors with remarkable anti-prostate cancer activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 5.73 | 6.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4283818 | — | — | 1 | 6.34 |
| CHEMBL4278419 | — | — | 1 | 6.26 |
| CHEMBL4294741 | — | — | 1 | 6.17 |
| CHEMBL4287574 | — | — | 1 | 6.01 |
| CHEMBL4287705 | — | — | 1 | 6.00 |
| CHEMBL4292071 | — | — | 1 | 5.90 |
| CHEMBL4276931 | — | — | 1 | 5.80 |
| CHEMBL4280911 | — | — | 1 | 5.66 |
| CHEMBL4289090 | — | — | 1 | 5.57 |
| CHEMBL43612 | JUGLONE | — | 1 | 5.00 |
| CHEMBL237111 | AKBA | -1.0 | 1 | 4.30 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4283818 | — | IC50 | = | 460.0 | nM | 6.34 |
| CHEMBL4278419 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL4294741 | — | IC50 | = | 680.0 | nM | 6.17 |
| CHEMBL4287574 | — | IC50 | = | 970.0 | nM | 6.01 |
| CHEMBL4287705 | — | IC50 | = | 1010.0 | nM | 6.00 |
| CHEMBL4292071 | — | IC50 | = | 1270.0 | nM | 5.90 |
| CHEMBL4276931 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL4280911 | — | IC50 | = | 2180.0 | nM | 5.66 |
| CHEMBL4289090 | — | IC50 | = | 2680.0 | nM | 5.57 |
| CHEMBL43612 | JUGLONE | IC50 | = | 10030.0 | nM | 5.00 |
| CHEMBL237111 | AKBA | IC50 | = | 50360.0 | nM | 4.30 |