Assay Detail
Binding
CHEMBL2384162
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Inhibition of rat liver DHFR
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, synthesis, and molecular modeling of novel pyrido[2,3-d]pyrimidine analogues as antifolates; application of Buchwald-Hartwig aminations of heterocycles.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 6.65 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.60 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 8.52 |
| CHEMBL7492 | PIRITREXIM | 2.0 | 1 | 8.48 |
| CHEMBL2382329 | — | — | 1 | 8.43 |
| CHEMBL2382327 | — | — | 1 | 8.23 |
| CHEMBL2382330 | — | — | 1 | 8.17 |
| CHEMBL2382334 | — | — | 1 | 7.68 |
| CHEMBL2382328 | — | — | 1 | 7.62 |
| CHEMBL2382331 | — | — | 1 | 7.55 |
| CHEMBL2382335 | — | — | 1 | 7.16 |
| CHEMBL2382332 | — | — | 1 | 7.14 |
| CHEMBL2382326 | — | — | 1 | 6.92 |
| CHEMBL2382314 | — | — | 1 | 6.38 |
| CHEMBL2382336 | — | — | 1 | 6.37 |
| CHEMBL2382333 | — | — | 1 | 6.21 |
| CHEMBL2382316 | — | — | 1 | 6.12 |
| CHEMBL2382324 | — | — | 1 | 5.96 |
| CHEMBL36 | PYRIMETHAMINE | 4.0 | 1 | 5.82 |
| CHEMBL2382317 | — | — | 1 | 5.77 |
| CHEMBL2382323 | — | — | 1 | 5.54 |
| CHEMBL2382321 | — | — | 1 | 5.48 |
| CHEMBL2382315 | — | — | 1 | 5.41 |
| CHEMBL2382319 | — | — | 1 | 5.40 |
| CHEMBL2382318 | — | — | 1 | 5.40 |
| CHEMBL2382325 | — | — | 1 | 5.28 |
| CHEMBL2382322 | — | — | 1 | 4.92 |
| CHEMBL2382320 | — | — | 1 | 4.92 |
| CHEMBL22 | TRIMETHOPRIM | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34259 | METHOTREXATE | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL7492 | PIRITREXIM | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL2382329 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL2382327 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL2382330 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL2382334 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL2382328 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL2382331 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL2382335 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL2382332 | — | IC50 | = | 72.0 | nM | 7.14 |
| CHEMBL2382326 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2382314 | — | IC50 | = | 420.0 | nM | 6.38 |
| CHEMBL2382336 | — | IC50 | = | 430.0 | nM | 6.37 |
| CHEMBL2382333 | — | IC50 | = | 610.0 | nM | 6.21 |
| CHEMBL2382316 | — | IC50 | = | 760.0 | nM | 6.12 |
| CHEMBL2382324 | — | IC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL36 | PYRIMETHAMINE | IC50 | = | 1500.0 | nM | 5.82 |
| CHEMBL2382317 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL2382323 | — | IC50 | = | 2900.0 | nM | 5.54 |
| CHEMBL2382321 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL2382315 | — | IC50 | = | 3900.0 | nM | 5.41 |
| CHEMBL2382319 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2382318 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL2382325 | — | IC50 | = | 5200.0 | nM | 5.28 |
| CHEMBL2382322 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL2382320 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL22 | TRIMETHOPRIM | IC50 | = | 180000.0 | nM | - |