Assay Detail
Binding
CHEMBL4338135
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant MTHFD1 (unknown origin) using THF as substrate incubated for 30 mins in presence of NAD
23
Total Activities
23
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
C-1-tetrahydrofolate synthase, cytoplasmic (CHEMBL2541) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of a Potent, Selective, and Orally Available MTHFD2 Inhibitor (DS18561882) with in Vivo Antitumor Activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 5.23 | 6.24 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4463968 | — | — | 1 | 6.24 |
| CHEMBL4470947 | — | — | 1 | 5.96 |
| CHEMBL4483030 | — | — | 1 | 5.54 |
| CHEMBL4542665 | — | — | 1 | 5.38 |
| CHEMBL4584730 | — | — | 1 | 5.31 |
| CHEMBL4441993 | — | — | 1 | 5.30 |
| CHEMBL4534641 | — | — | 1 | 5.28 |
| CHEMBL4441792 | — | — | 1 | 5.27 |
| CHEMBL4546647 | — | — | 1 | 5.19 |
| CHEMBL4538356 | — | — | 1 | 5.10 |
| CHEMBL4460077 | — | — | 1 | 5.08 |
| CHEMBL4474051 | — | — | 1 | 4.92 |
| CHEMBL4458187 | — | — | 1 | 4.73 |
| CHEMBL4460238 | — | — | 1 | 4.64 |
| CHEMBL4472668 | — | — | 1 | 4.57 |
| CHEMBL4438430 | — | — | 1 | - |
| CHEMBL4592118 | — | — | 1 | - |
| CHEMBL4451401 | — | — | 1 | - |
| CHEMBL4473116 | — | — | 1 | - |
| CHEMBL4436668 | — | — | 1 | - |
| CHEMBL4551634 | — | — | 1 | - |
| CHEMBL4467997 | — | — | 1 | - |
| CHEMBL4526400 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4463968 | — | IC50 | = | 570.0 | nM | 6.24 |
| CHEMBL4470947 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL4483030 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL4542665 | — | IC50 | = | 4200.0 | nM | 5.38 |
| CHEMBL4584730 | — | IC50 | = | 4900.0 | nM | 5.31 |
| CHEMBL4441993 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL4534641 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4441792 | — | IC50 | = | 5400.0 | nM | 5.27 |
| CHEMBL4546647 | — | IC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL4538356 | — | IC50 | = | 8000.0 | nM | 5.10 |
| CHEMBL4460077 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL4474051 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL4458187 | — | IC50 | = | 18700.0 | nM | 4.73 |
| CHEMBL4460238 | — | IC50 | = | 23000.0 | nM | 4.64 |
| CHEMBL4472668 | — | IC50 | = | 27000.0 | nM | 4.57 |
| CHEMBL4438430 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4592118 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4451401 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4473116 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4436668 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4551634 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4467997 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4526400 | — | IC50 | > | 30000.0 | nM | - |