Assay Detail
Binding
CHEMBL4477153
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of N-terminal HIS-tagged and TEV cleavage site containing full length PHGDH (unknown origin) expressed in Escherichia coli assessed as reduction in conversion of 3-Phosphoglycerate and NAD to 3-Phosphohydroxypyruvate and NADH using 250 uM NAD and 500 uM 3-PG incubated for 240 mins by fluorescence based assay
192
Total Activities
192
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
Tosylacetate based compounds and derivatives thereof as phgdh inhibitors
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 192 | 6.37 | 8.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4527607 | — | — | 1 | 8.52 |
| CHEMBL4520837 | — | — | 1 | 8.52 |
| CHEMBL4515492 | — | — | 1 | 8.52 |
| CHEMBL4542437 | — | — | 1 | 8.40 |
| CHEMBL4436264 | — | — | 1 | 8.40 |
| CHEMBL4548014 | — | — | 1 | 8.30 |
| CHEMBL4483622 | — | — | 1 | 8.30 |
| CHEMBL4587306 | — | — | 1 | 8.30 |
| CHEMBL4547034 | — | — | 1 | 8.22 |
| CHEMBL4533417 | — | — | 1 | 8.22 |
| CHEMBL4483483 | — | — | 1 | 8.22 |
| CHEMBL4560976 | — | — | 1 | 8.15 |
| CHEMBL4548203 | — | — | 1 | 8.15 |
| CHEMBL4580665 | — | — | 1 | 8.10 |
| CHEMBL4467246 | — | — | 1 | 8.10 |
| CHEMBL4517873 | — | — | 1 | 8.10 |
| CHEMBL4585012 | — | — | 1 | 8.10 |
| CHEMBL4518612 | — | — | 1 | 8.05 |
| CHEMBL4513843 | — | — | 1 | 8.00 |
| CHEMBL4592933 | — | — | 1 | 8.00 |
| CHEMBL4547905 | — | — | 1 | 7.96 |
| CHEMBL4517506 | — | — | 1 | 7.96 |
| CHEMBL4572814 | — | — | 1 | 7.92 |
| CHEMBL4572184 | — | — | 1 | 7.89 |
| CHEMBL4587964 | — | — | 1 | 7.77 |
| CHEMBL4551822 | — | — | 1 | 7.70 |
| CHEMBL4524231 | — | — | 1 | 7.68 |
| CHEMBL4556963 | — | — | 1 | 7.62 |
| CHEMBL4541970 | — | — | 1 | 7.57 |
| CHEMBL4576106 | — | — | 1 | 7.54 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4515492 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4527607 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4520837 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4542437 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4436264 | — | IC50 | = | 4.0 | nM | 8.40 |
| CHEMBL4587306 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4483622 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4548014 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4547034 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4533417 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4483483 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL4560976 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4548203 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4467246 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4580665 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4585012 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4517873 | — | IC50 | = | 8.0 | nM | 8.10 |
| CHEMBL4518612 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL4513843 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4592933 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL4547905 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4517506 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL4572814 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL4572184 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL4587964 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL4551822 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL4524231 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL4556963 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL4541970 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4576106 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL4580853 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL4549808 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4557402 | — | IC50 | = | 41.0 | nM | 7.39 |
| CHEMBL4552712 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL4521930 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL4513944 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4574871 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL4516261 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4578446 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4569609 | — | IC50 | = | 62.0 | nM | 7.21 |
| CHEMBL4550369 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4568292 | — | IC50 | = | 74.0 | nM | 7.13 |
| CHEMBL4530767 | — | IC50 | = | 76.0 | nM | 7.12 |
| CHEMBL4521064 | — | IC50 | = | 84.0 | nM | 7.08 |
| CHEMBL4572318 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL4545772 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL4483039 | — | IC50 | = | 89.0 | nM | 7.05 |
| CHEMBL4536159 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4578573 | — | IC50 | = | 98.0 | nM | 7.01 |
| CHEMBL4514983 | — | IC50 | = | 120.0 | nM | 6.92 |