Assay Detail
Binding
CHEMBL4418848
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of His-tagged human recombinant SHMT2 expressed in Escherichia coli BLR(DE3) assessed as reduction in NADPH level using L-serine, THF and NADP+ incubated for 5 mins by SHMT2-MTHFD coupled reaction based fluorescence assay
195
Total Activities
195
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
Serine hydroxymethyltransferase, mitochondrial (CHEMBL4295747) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Compositions and methods relating to inhibiting serine hyrdoxymethyltransferase 2 activity
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 195 | 5.41 | 6.36 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL506 | PRIMAQUINE | 4.0 | 1 | 6.36 |
| CHEMBL4530254 | — | — | 1 | 6.27 |
| CHEMBL582132 | — | — | 1 | 6.16 |
| CHEMBL1528232 | — | — | 1 | 6.15 |
| CHEMBL4555669 | — | — | 1 | 6.07 |
| CHEMBL255044 | FLUPIRTINE | 4.0 | 1 | 6.03 |
| CHEMBL4519144 | — | — | 1 | 5.99 |
| CHEMBL4559774 | — | — | 1 | 5.93 |
| CHEMBL1300552 | — | — | 1 | 5.87 |
| CHEMBL4593782 | — | — | 1 | 5.87 |
| CHEMBL4447053 | — | — | 1 | 5.85 |
| CHEMBL4449009 | — | — | 1 | 5.82 |
| CHEMBL4573270 | — | — | 1 | 5.81 |
| CHEMBL4557965 | — | — | 1 | 5.81 |
| CHEMBL4553385 | — | — | 1 | 5.80 |
| CHEMBL4514553 | — | — | 1 | 5.79 |
| CHEMBL4447612 | — | — | 1 | 5.79 |
| CHEMBL4531045 | — | — | 1 | 5.78 |
| CHEMBL4584803 | — | — | 1 | 5.76 |
| CHEMBL4475301 | — | — | 1 | 5.76 |
| CHEMBL4575980 | — | — | 1 | 5.76 |
| CHEMBL4557996 | — | — | 1 | 5.74 |
| CHEMBL4436987 | — | — | 1 | 5.73 |
| CHEMBL4451110 | — | — | 1 | 5.73 |
| CHEMBL4464727 | — | — | 1 | 5.72 |
| CHEMBL1071 | OXAPROZIN | 4.0 | 1 | 5.71 |
| CHEMBL4471334 | — | — | 1 | 5.70 |
| CHEMBL4547456 | — | — | 1 | 5.69 |
| CHEMBL4473357 | — | — | 1 | 5.69 |
| CHEMBL4448873 | — | — | 1 | 5.67 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL506 | PRIMAQUINE | IC50 | = | 436.52 | nM | 6.36 |
| CHEMBL4530254 | — | IC50 | = | 540.0 | nM | 6.27 |
| CHEMBL582132 | — | IC50 | = | 690.0 | nM | 6.16 |
| CHEMBL1528232 | — | IC50 | = | 710.0 | nM | 6.15 |
| CHEMBL4555669 | — | IC50 | = | 850.0 | nM | 6.07 |
| CHEMBL255044 | FLUPIRTINE | IC50 | = | 933.25 | nM | 6.03 |
| CHEMBL4519144 | — | IC50 | = | 1020.0 | nM | 5.99 |
| CHEMBL4559774 | — | IC50 | = | 1170.0 | nM | 5.93 |
| CHEMBL1300552 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4593782 | — | IC50 | = | 1350.0 | nM | 5.87 |
| CHEMBL4447053 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4449009 | — | IC50 | = | 1510.0 | nM | 5.82 |
| CHEMBL4573270 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4557965 | — | IC50 | = | 1550.0 | nM | 5.81 |
| CHEMBL4553385 | — | IC50 | = | 1580.0 | nM | 5.80 |
| CHEMBL4447612 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL4514553 | — | IC50 | = | 1620.0 | nM | 5.79 |
| CHEMBL4531045 | — | IC50 | = | 1660.0 | nM | 5.78 |
| CHEMBL4475301 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL4584803 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL4575980 | — | IC50 | = | 1740.0 | nM | 5.76 |
| CHEMBL4557996 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL4451110 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL4436987 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL4464727 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL1071 | OXAPROZIN | IC50 | = | 1949.84 | nM | 5.71 |
| CHEMBL4471334 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4473357 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL4547456 | — | IC50 | = | 2040.0 | nM | 5.69 |
| CHEMBL4440546 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL4448873 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL4577602 | — | IC50 | = | 2140.0 | nM | 5.67 |
| CHEMBL4444905 | — | IC50 | = | 2190.0 | nM | 5.66 |
| CHEMBL4451169 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL4438740 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL4464489 | — | IC50 | = | 2240.0 | nM | 5.65 |
| CHEMBL4561726 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4561599 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4537620 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4462291 | — | IC50 | = | 2340.0 | nM | 5.63 |
| CHEMBL4550873 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4585136 | — | IC50 | = | 2400.0 | nM | 5.62 |
| CHEMBL4441189 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL30432 | GW282974X | IC50 | = | 2454.71 | nM | 5.61 |
| CHEMBL4567493 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL4526437 | — | IC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL4440469 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL4565701 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL4581290 | — | IC50 | = | 2510.0 | nM | 5.60 |
| CHEMBL4521853 | — | IC50 | = | 2510.0 | nM | 5.60 |