Assay Detail
Binding
CHEMBL4375168
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal His6-tagged human PHGDH (4 to 315 residues) assessed as effect on NADH fluorescence incubated for 2 hrs using 3-PG substrate in presence of 250 uM NAD+ and PSAT1 by diaphorase based luminescence assay
16
Total Activities
16
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
D-3-phosphoglycerate dehydrogenase (CHEMBL2311243) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Intracellular Trapping of the Selective Phosphoglycerate Dehydrogenase (PHGDH) Inhibitor <b>BI-4924</b> Disrupts Serine Biosynthesis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 6.67 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4520837 | — | — | 1 | 8.52 |
| CHEMBL4436264 | — | — | 1 | 8.40 |
| CHEMBL4467246 | — | — | 1 | 8.10 |
| CHEMBL4438014 | — | — | 1 | 7.02 |
| CHEMBL4469992 | — | — | 1 | 6.64 |
| CHEMBL4594097 | — | — | 1 | 6.61 |
| CHEMBL4522467 | — | — | 1 | 6.60 |
| CHEMBL4473052 | — | — | 1 | 6.52 |
| CHEMBL4560125 | — | — | 1 | 6.47 |
| CHEMBL4457646 | — | — | 1 | 6.46 |
| CHEMBL4474620 | — | — | 1 | 6.38 |
| CHEMBL4444192 | — | — | 1 | 6.15 |
| CHEMBL4437057 | — | — | 1 | 6.13 |
| CHEMBL4460522 | — | — | 1 | 5.89 |
| CHEMBL4446511 | — | — | 1 | 5.63 |
| CHEMBL4520181 | — | — | 1 | 5.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4520837 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4436264 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4467246 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4438014 | — | IC50 | = | 95.0 | nM | 7.02 |
| CHEMBL4469992 | — | IC50 | = | 228.0 | nM | 6.64 |
| CHEMBL4594097 | — | IC50 | = | 246.0 | nM | 6.61 |
| CHEMBL4522467 | — | IC50 | = | 249.0 | nM | 6.60 |
| CHEMBL4473052 | — | IC50 | = | 301.0 | nM | 6.52 |
| CHEMBL4560125 | — | IC50 | = | 341.0 | nM | 6.47 |
| CHEMBL4457646 | — | IC50 | = | 345.0 | nM | 6.46 |
| CHEMBL4474620 | — | IC50 | = | 412.0 | nM | 6.38 |
| CHEMBL4444192 | — | IC50 | = | 714.0 | nM | 6.15 |
| CHEMBL4437057 | — | IC50 | = | 746.0 | nM | 6.13 |
| CHEMBL4460522 | — | IC50 | = | 1294.0 | nM | 5.89 |
| CHEMBL4446511 | — | IC50 | = | 2368.0 | nM | 5.63 |
| CHEMBL4520181 | — | IC50 | = | 6694.0 | nM | 5.17 |