Assay Detail
Functional
CHEMBL1006395
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Antiproliferative activity against human FRbeta expressing Chinese hamster D4 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cricetulus griseus |
| Cell Type | D4 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Synthesis and discovery of high affinity folate receptor-specific glycinamide ribonucleotide formyltransferase inhibitors with antitumor activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 11 | 7.57 | 8.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 8.59 |
| CHEMBL192632 | — | — | 1 | 8.25 |
| CHEMBL365307 | — | — | 1 | 8.00 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.96 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 7.66 |
| CHEMBL501999 | — | — | 1 | 7.28 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.22 |
| CHEMBL502528 | — | — | 1 | 7.10 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 6.97 |
| CHEMBL526928 | — | — | 1 | 6.70 |
| CHEMBL498800 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34412 | LOMETREXOL | IC50 | = | 2.6 | nM | 8.59 |
| CHEMBL192632 | — | IC50 | = | 5.6 | nM | 8.25 |
| CHEMBL365307 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL501999 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL502528 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL526928 | — | IC50 | = | 198.0 | nM | 6.70 |
| CHEMBL498800 | — | IC50 | > | 1000.0 | nM | - |