Assay Detail
Binding
CHEMBL4432159
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant N-terminal 6His-tagged human GARFTase assessed as formation of 5,8-dideazafolate from 10-formyl-5,8-dideazafolic acid measured at every 15 seconds over 20 min by spectrophotometric analysis
9
Total Activities
9
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
Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3972) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Tumor Targeting with Novel 6-Substituted Pyrrolo [2,3-d] Pyrimidine Antifolates with Heteroatom Bridge Substitutions via Cellular Uptake by Folate Receptor α and the Proton-Coupled Folate Transporter and Inhibition of de Novo Purine Nucleotide Biosynthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.91 | 7.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4437824 | — | — | 1 | 7.23 |
| CHEMBL4444011 | — | — | 1 | 7.21 |
| CHEMBL4447805 | — | — | 1 | 7.21 |
| CHEMBL1834488 | — | — | 1 | 7.17 |
| CHEMBL4471269 | — | — | 1 | 7.00 |
| CHEMBL4553188 | — | — | 1 | 6.91 |
| CHEMBL192632 | — | — | 1 | 6.80 |
| CHEMBL4467936 | — | — | 1 | 6.70 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 6.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4437824 | — | Ki | = | 59.0 | nM | 7.23 |
| CHEMBL4444011 | — | Ki | = | 62.0 | nM | 7.21 |
| CHEMBL4447805 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL1834488 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL4471269 | — | Ki | = | 99.0 | nM | 7.00 |
| CHEMBL4553188 | — | Ki | = | 122.0 | nM | 6.91 |
| CHEMBL192632 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL4467936 | — | Ki | = | 201.0 | nM | 6.70 |
| CHEMBL225072 | PEMETREXED | Ki | = | 1000.0 | nM | 6.00 |