Assay Detail
Binding
CHEMBL944098
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Inhibition of human recombinant DHFR
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Synthesis and biological evaluation of novel 2,4-diaminoquinazoline derivatives as SMN2 promoter activators for the potential treatment of spinal muscular atrophy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.58 | 9.41 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL251427 | — | — | 1 | 9.41 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 9.00 |
| CHEMBL253976 | — | — | 1 | 7.60 |
| CHEMBL398416 | — | — | 1 | 7.47 |
| CHEMBL251906 | — | — | 1 | 7.41 |
| CHEMBL255019 | — | — | 1 | 5.08 |
| CHEMBL251428 | — | — | 1 | 4.97 |
| CHEMBL251430 | — | — | 1 | 4.26 |
| CHEMBL250231 | — | — | 1 | 4.01 |
| CHEMBL251675 | — | — | 1 | - |
| CHEMBL251429 | — | — | 1 | - |
| CHEMBL251434 | — | — | 1 | - |
| CHEMBL250075 | — | — | 1 | - |
| CHEMBL413990 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL251427 | — | IC50 | = | 0.39 | nM | 9.41 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL253976 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL398416 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL251906 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL255019 | — | IC50 | = | 8400.0 | nM | 5.08 |
| CHEMBL251428 | — | IC50 | = | 10700.0 | nM | 4.97 |
| CHEMBL251430 | — | IC50 | = | 55200.0 | nM | 4.26 |
| CHEMBL250231 | — | IC50 | = | 98000.0 | nM | 4.01 |
| CHEMBL251675 | — | IC50 | - | — | - | |
| CHEMBL251429 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL251434 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL250075 | — | IC50 | > | 125000.0 | nM | - |
| CHEMBL413990 | — | IC50 | > | 125000.0 | nM | - |