Assay Detail
Binding
CHEMBL668780
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Inhibition of dihydrofolate reductase (DHFR) from rat liver (rl)
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Pneumocystis carinii and Toxoplasma gondii dihydrofolate reductase inhibitors and antitumor agents: synthesis and biological activities of 2,4-diamino-5-methyl-6-[(monosubstituted anilino)methyl] pyrido[2,3-d]pyrimidines.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.49 | 8.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.82 |
| CHEMBL23532 | — | — | 1 | 8.68 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL50514 | — | — | 1 | 8.12 |
| CHEMBL264386 | — | — | 1 | 7.89 |
| CHEMBL79922 | — | — | 1 | 7.75 |
| CHEMBL310880 | — | — | 1 | 7.58 |
| CHEMBL420224 | — | — | 1 | 7.48 |
| CHEMBL80065 | — | — | 1 | 7.46 |
| CHEMBL82924 | — | — | 1 | 7.44 |
| CHEMBL79347 | — | — | 1 | 7.44 |
| CHEMBL80066 | — | — | 1 | 7.43 |
| CHEMBL82975 | — | — | 1 | 7.38 |
| CHEMBL283518 | — | — | 1 | 7.36 |
| CHEMBL23416 | — | — | 1 | 7.29 |
| CHEMBL81820 | — | — | 1 | 7.28 |
| CHEMBL312348 | — | — | 1 | 7.25 |
| CHEMBL80070 | — | — | 1 | 7.10 |
| CHEMBL81119 | — | — | 1 | 7.06 |
| CHEMBL309966 | — | — | 1 | 7.00 |
| CHEMBL79123 | — | — | 1 | 6.77 |
| CHEMBL84457 | — | — | 1 | 6.77 |
| CHEMBL281803 | — | — | 1 | 6.39 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL7492 | PIRITREXIM | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL23532 | — | IC50 | = | 2.1 | nM | 8.68 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL50514 | — | IC50 | = | 7.6 | nM | 8.12 |
| CHEMBL264386 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL79922 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL310880 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL420224 | — | IC50 | = | 33.0 | nM | 7.48 |
| CHEMBL80065 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL82924 | — | IC50 | = | 36.3 | nM | 7.44 |
| CHEMBL79347 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL80066 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL82975 | — | IC50 | = | 42.0 | nM | 7.38 |
| CHEMBL283518 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL23416 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL81820 | — | IC50 | = | 53.0 | nM | 7.28 |
| CHEMBL312348 | — | IC50 | = | 55.6 | nM | 7.25 |
| CHEMBL80070 | — | IC50 | = | 80.1 | nM | 7.10 |
| CHEMBL81119 | — | IC50 | = | 88.0 | nM | 7.06 |
| CHEMBL309966 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL79123 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL84457 | — | IC50 | = | 169.0 | nM | 6.77 |
| CHEMBL281803 | — | IC50 | = | 407.0 | nM | 6.39 |