Assay Detail
Binding
CHEMBL1067650
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of GARFtase in human KB cells assessed as [14C]glycine incorporation in to [14C]FGAR in folate free RPMI medium with 2 nM LCV by in-situassay
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | KB |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3972) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 6 | 5.66 | 6.20 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL590740 | — | — | 1 | 6.20 |
| CHEMBL605580 | — | — | 1 | 5.12 |
| CHEMBL365307 | — | — | 1 | - |
| CHEMBL491104 | — | — | 1 | - |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | - |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL590740 | — | IC50 | = | 630.0 | nM | 6.20 |
| CHEMBL605580 | — | IC50 | = | 7650.0 | nM | 5.12 |
| CHEMBL365307 | — | IC50 | = | 6800.0 | nM | - |
| CHEMBL491104 | — | IC50 | = | 13300.0 | nM | - |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 14000.0 | nM | - |
| CHEMBL225072 | PEMETREXED | IC50 | = | 30000.0 | nM | - |