Assay Detail
Functional
CHEMBL1006397
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Antiproliferative activity against human RFC and FRalpha expressing human KB cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | KB |
| 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 | 8.10 | 8.92 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 8.92 |
| CHEMBL192632 | — | — | 1 | 8.77 |
| CHEMBL365307 | — | — | 1 | 8.72 |
| CHEMBL501999 | — | — | 1 | 8.24 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 8.23 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.22 |
| CHEMBL502528 | — | — | 1 | 7.89 |
| CHEMBL526928 | — | — | 1 | 7.64 |
| CHEMBL119 | TRIMETREXATE | 4.0 | 1 | 7.24 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.17 |
| CHEMBL498800 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL34412 | LOMETREXOL | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL192632 | — | IC50 | = | 1.7 | nM | 8.77 |
| CHEMBL365307 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL501999 | — | IC50 | = | 5.8 | nM | 8.24 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL502528 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL526928 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL119 | TRIMETREXATE | IC50 | = | 58.0 | nM | 7.24 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL498800 | — | IC50 | > | 1000.0 | nM | - |