Assay Detail
Binding
CHEMBL4375167
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 19 uM NAD+ and PSAT1 by diaphorase based luminescence assay
60
Total Activities
60
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 | 60 | 5.98 | 8.70 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4436264 | — | — | 1 | 8.70 |
| CHEMBL4467246 | — | — | 1 | 8.52 |
| CHEMBL4438014 | — | — | 1 | 7.85 |
| CHEMBL4458393 | — | — | 1 | 7.60 |
| CHEMBL4522467 | — | — | 1 | 7.55 |
| CHEMBL4594097 | — | — | 1 | 7.55 |
| CHEMBL4469992 | — | — | 1 | 7.52 |
| CHEMBL4473052 | — | — | 1 | 7.52 |
| CHEMBL4474620 | — | — | 1 | 7.29 |
| CHEMBL4457646 | — | — | 1 | 7.24 |
| CHEMBL4560125 | — | — | 1 | 7.21 |
| CHEMBL4565713 | — | — | 1 | 7.16 |
| CHEMBL4437057 | — | — | 1 | 7.14 |
| CHEMBL4444192 | — | — | 1 | 7.09 |
| CHEMBL4588817 | — | — | 1 | 7.00 |
| CHEMBL4446190 | — | — | 1 | 7.00 |
| CHEMBL4460522 | — | — | 1 | 6.91 |
| CHEMBL4446511 | — | — | 1 | 6.59 |
| CHEMBL4528650 | — | — | 1 | 6.52 |
| CHEMBL4435368 | — | — | 1 | 6.40 |
| CHEMBL4561620 | — | — | 1 | 6.10 |
| CHEMBL4520181 | — | — | 1 | 6.08 |
| CHEMBL4476414 | — | — | 1 | 6.05 |
| CHEMBL4524921 | — | — | 1 | 5.89 |
| CHEMBL4521090 | — | — | 1 | 5.85 |
| CHEMBL4562446 | — | — | 1 | 5.71 |
| CHEMBL4460438 | — | — | 1 | 5.64 |
| CHEMBL4435257 | — | — | 1 | 5.60 |
| CHEMBL4528065 | — | — | 1 | 5.51 |
| CHEMBL4441109 | — | — | 1 | 5.48 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4436264 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL4467246 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL4438014 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL4458393 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL4522467 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4594097 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4469992 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4473052 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL4474620 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL4457646 | — | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL4560125 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4565713 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL4437057 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL4444192 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL4446190 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4588817 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4460522 | — | IC50 | = | 123.0 | nM | 6.91 |
| CHEMBL4446511 | — | IC50 | = | 254.0 | nM | 6.59 |
| CHEMBL4528650 | — | IC50 | = | 300.0 | nM | 6.52 |
| CHEMBL4435368 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL4561620 | — | IC50 | = | 800.0 | nM | 6.10 |
| CHEMBL4520181 | — | IC50 | = | 824.0 | nM | 6.08 |
| CHEMBL4476414 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL4524921 | — | IC50 | = | 1300.0 | nM | 5.89 |
| CHEMBL4521090 | — | IC50 | = | 1400.0 | nM | 5.85 |
| CHEMBL4562446 | — | IC50 | = | 1950.0 | nM | 5.71 |
| CHEMBL4460438 | — | IC50 | = | 2300.0 | nM | 5.64 |
| CHEMBL4435257 | — | IC50 | = | 2500.0 | nM | 5.60 |
| CHEMBL4528065 | — | IC50 | = | 3100.0 | nM | 5.51 |
| CHEMBL4441109 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL4519850 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL4443133 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4473931 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL4475246 | — | IC50 | = | 5700.0 | nM | 5.24 |
| CHEMBL4563937 | — | IC50 | = | 5830.0 | nM | 5.23 |
| CHEMBL4582751 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL4446581 | — | IC50 | = | 6700.0 | nM | 5.17 |
| CHEMBL4569664 | — | IC50 | = | 11700.0 | nM | 4.93 |
| CHEMBL4471731 | — | IC50 | = | 12100.0 | nM | 4.92 |
| CHEMBL4553827 | — | IC50 | = | 12200.0 | nM | 4.91 |
| CHEMBL4531432 | — | IC50 | = | 16200.0 | nM | 4.79 |
| CHEMBL4572650 | — | IC50 | = | 21500.0 | nM | 4.67 |
| CHEMBL4458092 | — | IC50 | = | 22000.0 | nM | 4.66 |
| CHEMBL4451612 | — | IC50 | = | 23200.0 | nM | 4.63 |
| CHEMBL4559464 | — | IC50 | = | 33700.0 | nM | 4.47 |
| CHEMBL4466603 | — | IC50 | = | 38100.0 | nM | 4.42 |
| CHEMBL4456888 | — | IC50 | = | 39600.0 | nM | 4.40 |
| CHEMBL4535551 | — | IC50 | = | 42100.0 | nM | 4.38 |
| CHEMBL4443791 | — | IC50 | = | 53800.0 | nM | 4.27 |
| CHEMBL4518793 | — | IC50 | = | 55400.0 | nM | 4.26 |