Assay Detail
Binding
CHEMBL684724
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Glycinamide Ribonucleotide Transformylase (GART) using N10-formyl-5,8-dideazafolate (FDDF) as the cofactor.
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3972) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Protein structure-based design, synthesis, and biological evaluation of 5-thia-2,6-diamino-4(3H)-oxopyrimidines: potent inhibitors of glycinamide ribonucleotide transformylase with potent cell growth inhibition.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 15 | 7.38 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL82261 | — | — | 1 | 8.70 |
| CHEMBL85436 | — | — | 1 | 8.52 |
| CHEMBL82181 | — | — | 1 | 8.47 |
| CHEMBL84935 | — | — | 1 | 8.07 |
| CHEMBL84605 | — | — | 1 | 7.85 |
| CHEMBL82390 | — | — | 1 | 7.82 |
| CHEMBL84163 | — | — | 1 | 7.55 |
| CHEMBL309415 | — | — | 1 | 7.52 |
| CHEMBL315627 | — | — | 1 | 7.50 |
| CHEMBL85871 | — | — | 1 | 7.46 |
| CHEMBL315076 | — | — | 1 | 7.46 |
| CHEMBL84904 | — | — | 1 | 7.42 |
| CHEMBL84045 | — | — | 1 | 6.08 |
| CHEMBL85848 | — | — | 1 | 5.70 |
| CHEMBL84728 | — | — | 1 | 4.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL82261 | — | Ki | = | 2.0 | nM | 8.70 |
| CHEMBL85436 | — | Ki | = | 3.0 | nM | 8.52 |
| CHEMBL82181 | — | Ki | = | 3.4 | nM | 8.47 |
| CHEMBL84935 | — | Ki | = | 8.5 | nM | 8.07 |
| CHEMBL84605 | — | Ki | = | 14.0 | nM | 7.85 |
| CHEMBL82390 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL84163 | — | Ki | = | 28.0 | nM | 7.55 |
| CHEMBL309415 | — | Ki | = | 30.0 | nM | 7.52 |
| CHEMBL315627 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL85871 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL315076 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL84904 | — | Ki | = | 38.0 | nM | 7.42 |
| CHEMBL84045 | — | Ki | = | 825.0 | nM | 6.08 |
| CHEMBL85848 | — | Ki | = | 2000.0 | nM | 5.70 |
| CHEMBL84728 | — | Ki | = | 30000.0 | nM | 4.52 |