Assay Detail
Functional
CHEMBL1811488
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Cytotoxic activity against drug-resistant MDR1-deficient human NCI/ADR cells expressing Pgp after 48 hrs by sulforhodamine B assay
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | NCI/ADR |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
2-Amino-4-methyl-5-phenylethyl substituted-7-N-benzyl-pyrrolo[2,3-d]pyrimidines as novel antitumor antimitotic agents that also reverse tumor resistance.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 5.13 | 6.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388289 | — | — | 1 | 6.60 |
| CHEMBL428647 | PACLITAXEL | 4.0 | 1 | 5.57 |
| CHEMBL227262 | — | — | 1 | 5.57 |
| CHEMBL1808056 | — | — | 1 | 5.30 |
| CHEMBL1808057 | — | — | 1 | 5.22 |
| CHEMBL1808061 | — | — | 1 | 5.16 |
| CHEMBL1808062 | — | — | 1 | 5.00 |
| CHEMBL1808060 | — | — | 1 | 4.96 |
| CHEMBL1808058 | — | — | 1 | 4.96 |
| CHEMBL1808059 | — | — | 1 | 4.92 |
| CHEMBL1808055 | — | — | 1 | 4.92 |
| CHEMBL1808063 | — | — | 1 | 4.48 |
| CHEMBL90555 | VINCRISTINE | 4.0 | 1 | 4.00 |
| CHEMBL159 | VINBLASTINE | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388289 | — | IC50 | = | 250.0 | nM | 6.60 |
| CHEMBL428647 | PACLITAXEL | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL227262 | — | IC50 | = | 2700.0 | nM | 5.57 |
| CHEMBL1808056 | — | IC50 | = | 5000.0 | nM | 5.30 |
| CHEMBL1808057 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL1808061 | — | IC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL1808062 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL1808060 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1808058 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL1808059 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1808055 | — | IC50 | = | 12000.0 | nM | 4.92 |
| CHEMBL1808063 | — | IC50 | = | 33000.0 | nM | 4.48 |
| CHEMBL90555 | VINCRISTINE | IC50 | = | 100000.0 | nM | 4.00 |
| CHEMBL159 | VINBLASTINE | IC50 | > | 375000.0 | nM | - |