Assay Detail
Binding
CHEMBL820617
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Inhibition of isolated thymidylate synthase partially purified from L1210 mouse leukemia cells
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | L1210 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Design and synthesis of potent non-polyglutamatable quinazoline antifolate thymidylate synthase inhibitors.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 38 | 8.34 | 9.28 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL337914 | — | — | 1 | 9.28 |
| CHEMBL420155 | — | — | 1 | 9.22 |
| CHEMBL338429 | — | — | 1 | 9.21 |
| CHEMBL105346 | — | — | 1 | 9.07 |
| CHEMBL126325 | — | — | 1 | 8.85 |
| CHEMBL126648 | PLEVITREXED | 2.0 | 1 | 8.85 |
| CHEMBL439975 | — | — | 1 | 8.85 |
| CHEMBL341334 | — | — | 1 | 8.80 |
| CHEMBL127583 | — | — | 1 | 8.79 |
| CHEMBL126555 | — | — | 1 | 8.74 |
| CHEMBL340888 | — | — | 1 | 8.72 |
| CHEMBL338598 | — | — | 1 | 8.70 |
| CHEMBL340814 | — | — | 1 | 8.70 |
| CHEMBL127598 | — | — | 1 | 8.66 |
| CHEMBL127954 | — | — | 1 | 8.62 |
| CHEMBL125856 | — | — | 1 | 8.62 |
| CHEMBL340842 | — | — | 1 | 8.49 |
| CHEMBL127142 | — | — | 1 | 8.49 |
| CHEMBL338644 | — | — | 1 | 8.47 |
| CHEMBL127541 | — | — | 1 | 8.36 |
| CHEMBL123614 | — | — | 1 | 8.28 |
| CHEMBL126914 | — | — | 1 | 8.27 |
| CHEMBL127745 | — | — | 1 | 8.27 |
| CHEMBL127333 | — | — | 1 | 8.25 |
| CHEMBL341323 | — | — | 1 | 8.24 |
| CHEMBL126541 | — | — | 1 | 8.17 |
| CHEMBL341262 | — | — | 1 | 8.14 |
| CHEMBL126242 | — | — | 1 | 8.05 |
| CHEMBL128033 | — | — | 1 | 8.05 |
| CHEMBL441086 | — | — | 1 | 7.89 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL337914 | — | IC50 | = | 0.52 | nM | 9.28 |
| CHEMBL420155 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL338429 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL105346 | — | IC50 | = | 0.86 | nM | 9.07 |
| CHEMBL126325 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL126648 | PLEVITREXED | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL439975 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL341334 | — | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL127583 | — | IC50 | = | 1.62 | nM | 8.79 |
| CHEMBL126555 | — | IC50 | = | 1.8 | nM | 8.74 |
| CHEMBL340888 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL338598 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL340814 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL127598 | — | IC50 | = | 2.2 | nM | 8.66 |
| CHEMBL125856 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL127954 | — | IC50 | = | 2.4 | nM | 8.62 |
| CHEMBL340842 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL127142 | — | IC50 | = | 3.2 | nM | 8.49 |
| CHEMBL338644 | — | IC50 | = | 3.4 | nM | 8.47 |
| CHEMBL127541 | — | IC50 | = | 4.4 | nM | 8.36 |
| CHEMBL123614 | — | IC50 | = | 5.2 | nM | 8.28 |
| CHEMBL126914 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL127745 | — | IC50 | = | 5.4 | nM | 8.27 |
| CHEMBL127333 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL341323 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL126541 | — | IC50 | = | 6.8 | nM | 8.17 |
| CHEMBL341262 | — | IC50 | = | 7.2 | nM | 8.14 |
| CHEMBL126242 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL128033 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL441086 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL340635 | — | IC50 | = | 13.4 | nM | 7.87 |
| CHEMBL126697 | — | IC50 | = | 14.2 | nM | 7.85 |
| CHEMBL125971 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL339022 | — | IC50 | = | 15.4 | nM | 7.81 |
| CHEMBL389051 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL434209 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL127175 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 670.0 | nM | 6.17 |