Assay Detail
Binding
CHEMBL4719151
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human N-terminal His-tagged Pin1 expressed in Escherichia coli BL21 using Suc-Ala-Glu-Pro-Phe-4-nitroanilide as substrate incubated for 10 mins followed by substrate addition and measured for 90 sec by spectrophotometry
24
Total Activities
24
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
Synthesis and Pin1 inhibitory activity of thiazole derivatives.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.24 | 7.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL585917 | — | — | 1 | 7.30 |
| CHEMBL3322225 | — | — | 1 | 5.53 |
| CHEMBL4792060 | — | — | 1 | 5.53 |
| CHEMBL4757254 | — | — | 1 | 5.50 |
| CHEMBL4744323 | — | — | 1 | 5.49 |
| CHEMBL4779755 | — | — | 1 | 5.34 |
| CHEMBL4781756 | — | — | 1 | 5.33 |
| CHEMBL4791317 | — | — | 1 | 5.33 |
| CHEMBL4777545 | — | — | 1 | 5.30 |
| CHEMBL4745481 | — | — | 1 | 5.29 |
| CHEMBL4745229 | — | — | 1 | 5.27 |
| CHEMBL4764554 | — | — | 1 | 5.27 |
| CHEMBL4740631 | — | — | 1 | 5.26 |
| CHEMBL4759628 | — | — | 1 | 5.22 |
| CHEMBL4762421 | — | — | 1 | 5.09 |
| CHEMBL4782310 | — | — | 1 | 5.03 |
| CHEMBL4761085 | — | — | 1 | 5.03 |
| CHEMBL4795100 | — | — | 1 | 4.96 |
| CHEMBL4747974 | — | — | 1 | 4.87 |
| CHEMBL4796536 | — | — | 1 | 4.85 |
| CHEMBL4740637 | — | — | 1 | 4.83 |
| CHEMBL4791517 | — | — | 1 | 4.74 |
| CHEMBL4745826 | — | — | 1 | 4.68 |
| CHEMBL4797808 | — | — | 1 | 4.63 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL585917 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3322225 | — | IC50 | = | 2960.0 | nM | 5.53 |
| CHEMBL4792060 | — | IC50 | = | 2930.0 | nM | 5.53 |
| CHEMBL4757254 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL4744323 | — | IC50 | = | 3220.0 | nM | 5.49 |
| CHEMBL4779755 | — | IC50 | = | 4570.0 | nM | 5.34 |
| CHEMBL4781756 | — | IC50 | = | 4680.0 | nM | 5.33 |
| CHEMBL4791317 | — | IC50 | = | 4670.0 | nM | 5.33 |
| CHEMBL4777545 | — | IC50 | = | 5020.0 | nM | 5.30 |
| CHEMBL4745481 | — | IC50 | = | 5180.0 | nM | 5.29 |
| CHEMBL4745229 | — | IC50 | = | 5420.0 | nM | 5.27 |
| CHEMBL4764554 | — | IC50 | = | 5380.0 | nM | 5.27 |
| CHEMBL4740631 | — | IC50 | = | 5500.0 | nM | 5.26 |
| CHEMBL4759628 | — | IC50 | = | 6040.0 | nM | 5.22 |
| CHEMBL4762421 | — | IC50 | = | 8110.0 | nM | 5.09 |
| CHEMBL4782310 | — | IC50 | = | 9350.0 | nM | 5.03 |
| CHEMBL4761085 | — | IC50 | = | 9440.0 | nM | 5.03 |
| CHEMBL4795100 | — | IC50 | = | 11100.0 | nM | 4.96 |
| CHEMBL4747974 | — | IC50 | = | 13400.0 | nM | 4.87 |
| CHEMBL4796536 | — | IC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL4740637 | — | IC50 | = | 14800.0 | nM | 4.83 |
| CHEMBL4791517 | — | IC50 | = | 18100.0 | nM | 4.74 |
| CHEMBL4745826 | — | IC50 | = | 21100.0 | nM | 4.68 |
| CHEMBL4797808 | — | IC50 | = | 23400.0 | nM | 4.63 |