Assay Detail
Binding
CHEMBL4714607
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human full length N-terminal His-tagged GARFTase expressed in Chinese Hamster MTXRII-OuaR2-4 R2 cells assessed as reduction in THF formation using 10-CHOTHF as substrate by spectrophotometric method
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | R2 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Discovery of 6-substituted thieno[2,3-d]pyrimidine analogs as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis in folate receptor expressing human tumors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 5.62 | 6.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4783397 | — | — | 1 | 6.82 |
| CHEMBL4761741 | — | — | 1 | 6.04 |
| CHEMBL4741259 | — | — | 1 | 5.87 |
| CHEMBL491104 | — | — | 1 | 5.53 |
| CHEMBL4759798 | — | — | 1 | 5.37 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 5.29 |
| CHEMBL4790375 | — | — | 1 | 5.09 |
| CHEMBL4789686 | — | — | 1 | 4.97 |
| CHEMBL4755197 | — | — | 1 | - |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4783397 | — | Ki | = | 150.0 | nM | 6.82 |
| CHEMBL4761741 | — | Ki | = | 910.0 | nM | 6.04 |
| CHEMBL4741259 | — | Ki | = | 1360.0 | nM | 5.87 |
| CHEMBL491104 | — | Ki | = | 2970.0 | nM | 5.53 |
| CHEMBL4759798 | — | Ki | = | 4280.0 | nM | 5.37 |
| CHEMBL34259 | METHOTREXATE | Ki | = | 5190.0 | nM | 5.29 |
| CHEMBL4790375 | — | Ki | = | 8190.0 | nM | 5.09 |
| CHEMBL4789686 | — | Ki | = | 10720.0 | nM | 4.97 |
| CHEMBL4755197 | — | Ki | > | 150000.0 | nM | - |
| CHEMBL225072 | PEMETREXED | Ki | > | 150000.0 | nM | - |