Assay Detail
Binding
CHEMBL815675
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In vitro inhibition against L1210 thymidylate synthase (TS)
25
Total Activities
25
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Quinazoline antifolate thymidylate synthase inhibitors: bridge modifications and conformationally restricted analogues in the C2-methyl series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 25 | 5.44 | 7.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL434209 | — | — | 1 | 7.40 |
| CHEMBL74059 | — | — | 1 | 6.82 |
| CHEMBL40321 | — | — | 1 | 6.60 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 6.17 |
| CHEMBL307949 | — | — | 1 | 6.14 |
| CHEMBL69232 | — | — | 1 | 5.97 |
| CHEMBL74064 | — | — | 1 | 5.58 |
| CHEMBL71035 | — | — | 1 | 5.49 |
| CHEMBL71366 | — | — | 1 | 5.42 |
| CHEMBL74180 | — | — | 1 | 5.37 |
| CHEMBL70515 | — | — | 1 | 5.35 |
| CHEMBL72608 | — | — | 1 | 5.33 |
| CHEMBL70995 | — | — | 1 | 5.17 |
| CHEMBL71952 | — | — | 1 | 5.16 |
| CHEMBL306305 | — | — | 1 | 5.08 |
| CHEMBL70427 | — | — | 1 | 5.08 |
| CHEMBL68806 | — | — | 1 | 5.08 |
| CHEMBL308586 | — | — | 1 | 5.02 |
| CHEMBL74229 | — | — | 1 | 5.00 |
| CHEMBL72049 | — | — | 1 | 4.99 |
| CHEMBL70289 | — | — | 1 | 4.88 |
| CHEMBL71177 | — | — | 1 | 4.85 |
| CHEMBL309008 | — | — | 1 | 4.78 |
| CHEMBL302821 | — | — | 1 | 4.67 |
| CHEMBL68969 | — | — | 1 | 4.61 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL434209 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL74059 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL40321 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 670.0 | nM | 6.17 |
| CHEMBL307949 | — | IC50 | = | 720.0 | nM | 6.14 |
| CHEMBL69232 | — | IC50 | = | 1070.0 | nM | 5.97 |
| CHEMBL74064 | — | IC50 | = | 2620.0 | nM | 5.58 |
| CHEMBL71035 | — | IC50 | = | 3270.0 | nM | 5.49 |
| CHEMBL71366 | — | IC50 | = | 3820.0 | nM | 5.42 |
| CHEMBL74180 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL70515 | — | IC50 | = | 4500.0 | nM | 5.35 |
| CHEMBL72608 | — | IC50 | = | 4660.0 | nM | 5.33 |
| CHEMBL70995 | — | IC50 | = | 6730.0 | nM | 5.17 |
| CHEMBL71952 | — | IC50 | = | 6980.0 | nM | 5.16 |
| CHEMBL306305 | — | IC50 | = | 8270.0 | nM | 5.08 |
| CHEMBL70427 | — | IC50 | = | 8280.0 | nM | 5.08 |
| CHEMBL68806 | — | IC50 | = | 8420.0 | nM | 5.08 |
| CHEMBL308586 | — | IC50 | = | 9520.0 | nM | 5.02 |
| CHEMBL74229 | — | IC50 | = | 9900.0 | nM | 5.00 |
| CHEMBL72049 | — | IC50 | = | 10300.0 | nM | 4.99 |
| CHEMBL70289 | — | IC50 | = | 13280.0 | nM | 4.88 |
| CHEMBL71177 | — | IC50 | = | 14120.0 | nM | 4.85 |
| CHEMBL309008 | — | IC50 | = | 16660.0 | nM | 4.78 |
| CHEMBL302821 | — | IC50 | = | 21480.0 | nM | 4.67 |
| CHEMBL68969 | — | IC50 | = | 24800.0 | nM | 4.61 |