Assay Detail
Binding
CHEMBL4477151
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Inhibition of PHGDH in human MDA-MB-468 cells assessed as reduction in [13C3]-serine production incubated for 180 mins by LC/MS/MS analysis
73
Total Activities
73
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | MDA-MB-468 |
| 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 | 73 | 6.93 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4541133 | — | — | 1 | 9.52 |
| CHEMBL4536737 | — | — | 1 | 9.10 |
| CHEMBL4584313 | — | — | 1 | 8.80 |
| CHEMBL4518579 | — | — | 1 | 8.54 |
| CHEMBL4579388 | — | — | 1 | 8.48 |
| CHEMBL4540875 | — | — | 1 | 8.43 |
| CHEMBL4521661 | — | — | 1 | 8.41 |
| CHEMBL4541457 | — | — | 1 | 8.30 |
| CHEMBL4526788 | — | — | 1 | 8.15 |
| CHEMBL4522256 | — | — | 1 | 8.14 |
| CHEMBL4545772 | — | — | 1 | 8.08 |
| CHEMBL4522032 | — | — | 1 | 8.00 |
| CHEMBL4548756 | — | — | 1 | 7.92 |
| CHEMBL4542730 | — | — | 1 | 7.90 |
| CHEMBL4557404 | — | — | 1 | 7.83 |
| CHEMBL4536870 | — | — | 1 | 7.70 |
| CHEMBL4550162 | — | — | 1 | 7.65 |
| CHEMBL4514445 | — | — | 1 | 7.62 |
| CHEMBL4531113 | — | — | 1 | 7.62 |
| CHEMBL4522081 | — | — | 1 | 7.53 |
| CHEMBL4534115 | — | — | 1 | 7.52 |
| CHEMBL4545321 | — | — | 1 | 7.48 |
| CHEMBL4535665 | — | — | 1 | 7.47 |
| CHEMBL4590502 | — | — | 1 | 7.45 |
| CHEMBL4513944 | — | — | 1 | 7.43 |
| CHEMBL4565578 | — | — | 1 | 7.36 |
| CHEMBL4563552 | — | — | 1 | 7.29 |
| CHEMBL4580038 | — | — | 1 | 7.28 |
| CHEMBL4579433 | — | — | 1 | 7.27 |
| CHEMBL4535659 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4541133 | — | IC50 | = | 0.3 | nM | 9.52 |
| CHEMBL4536737 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL4584313 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL4518579 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL4579388 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL4540875 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL4521661 | — | IC50 | = | 3.9 | nM | 8.41 |
| CHEMBL4541457 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL4526788 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL4522256 | — | IC50 | = | 7.3 | nM | 8.14 |
| CHEMBL4545772 | — | IC50 | = | 8.3 | nM | 8.08 |
| CHEMBL4522032 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL4548756 | — | IC50 | = | 11.9 | nM | 7.92 |
| CHEMBL4542730 | — | IC50 | = | 12.6 | nM | 7.90 |
| CHEMBL4557404 | — | IC50 | = | 14.7 | nM | 7.83 |
| CHEMBL4536870 | — | IC50 | = | 20.1 | nM | 7.70 |
| CHEMBL4550162 | — | IC50 | = | 22.2 | nM | 7.65 |
| CHEMBL4514445 | — | IC50 | = | 23.9 | nM | 7.62 |
| CHEMBL4531113 | — | IC50 | = | 23.7 | nM | 7.62 |
| CHEMBL4522081 | — | IC50 | = | 29.3 | nM | 7.53 |
| CHEMBL4534115 | — | IC50 | = | 30.2 | nM | 7.52 |
| CHEMBL4545321 | — | IC50 | = | 32.8 | nM | 7.48 |
| CHEMBL4535665 | — | IC50 | = | 34.2 | nM | 7.47 |
| CHEMBL4590502 | — | IC50 | = | 35.9 | nM | 7.45 |
| CHEMBL4513944 | — | IC50 | = | 37.4 | nM | 7.43 |
| CHEMBL4565578 | — | IC50 | = | 44.1 | nM | 7.36 |
| CHEMBL4563552 | — | IC50 | = | 51.4 | nM | 7.29 |
| CHEMBL4580038 | — | IC50 | = | 52.5 | nM | 7.28 |
| CHEMBL4579433 | — | IC50 | = | 53.8 | nM | 7.27 |
| CHEMBL4535659 | — | IC50 | = | 62.1 | nM | 7.21 |
| CHEMBL4530135 | — | IC50 | = | 64.8 | nM | 7.19 |
| CHEMBL4573469 | — | IC50 | = | 66.3 | nM | 7.18 |
| CHEMBL4518189 | — | IC50 | = | 68.4 | nM | 7.17 |
| CHEMBL4571043 | — | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL4549376 | — | IC50 | = | 70.1 | nM | 7.15 |
| CHEMBL4593777 | — | IC50 | = | 72.1 | nM | 7.14 |
| CHEMBL4590594 | — | IC50 | = | 73.3 | nM | 7.13 |
| CHEMBL4548661 | — | IC50 | = | 78.6 | nM | 7.11 |
| CHEMBL4550915 | — | IC50 | = | 82.8 | nM | 7.08 |
| CHEMBL4587490 | — | IC50 | = | 88.8 | nM | 7.05 |
| CHEMBL4527489 | — | IC50 | = | 102.9 | nM | 6.99 |
| CHEMBL4565378 | — | IC50 | = | 109.2 | nM | 6.96 |
| CHEMBL4527049 | — | IC50 | = | 134.9 | nM | 6.87 |
| CHEMBL4520085 | — | IC50 | = | 135.7 | nM | 6.87 |
| CHEMBL4554160 | — | IC50 | = | 138.7 | nM | 6.86 |
| CHEMBL4544428 | — | IC50 | = | 141.8 | nM | 6.85 |
| CHEMBL4557237 | — | IC50 | = | 166.6 | nM | 6.78 |
| CHEMBL4558955 | — | IC50 | = | 165.9 | nM | 6.78 |
| CHEMBL4520837 | — | IC50 | = | 203.3 | nM | 6.69 |
| CHEMBL4568312 | — | IC50 | = | 249.0 | nM | 6.60 |