Assay Detail
Functional
CHEMBL1838954
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Antiproliferative activity against human KB cells expressing human RFC, FRalpha and PCFT assessed as reduction of viable cells after 96 hrs
9
Total Activities
9
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, biological, and antitumor activity of a highly potent 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitor with proton-coupled folate transporter and folate receptor selectivity over the reduced folate carrier that inhibits β-glycinamide ribonucleotide formyltransferase.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 9 | 8.39 | 9.59 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1834488 | — | — | 1 | 9.59 |
| CHEMBL590740 | — | — | 1 | 9.26 |
| CHEMBL34412 | LOMETREXOL | 2.0 | 1 | 8.92 |
| CHEMBL1834487 | — | — | 1 | 8.49 |
| CHEMBL590985 | TALOTREXIN | 2.0 | 1 | 8.28 |
| CHEMBL225071 | RALTITREXED | 4.0 | 1 | 8.23 |
| CHEMBL34259 | METHOTREXATE | 4.0 | 1 | 8.22 |
| CHEMBL1834486 | — | — | 1 | 7.38 |
| CHEMBL225072 | PEMETREXED | 4.0 | 1 | 7.17 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1834488 | — | IC50 | = | 0.26 | nM | 9.59 |
| CHEMBL590740 | — | IC50 | = | 0.55 | nM | 9.26 |
| CHEMBL34412 | LOMETREXOL | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL1834487 | — | IC50 | = | 3.22 | nM | 8.49 |
| CHEMBL590985 | TALOTREXIN | IC50 | = | 5.26 | nM | 8.28 |
| CHEMBL225071 | RALTITREXED | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL34259 | METHOTREXATE | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL1834486 | — | IC50 | = | 41.9 | nM | 7.38 |
| CHEMBL225072 | PEMETREXED | IC50 | = | 68.0 | nM | 7.17 |