Assay Detail
Functional
CHEMBL4844083
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Reversal of 5-FU resistance against human HCT-116 cells overexpressing DPD assessed as inhibition of cell proliferation measured after 72 hrs in presence of 5-FU by MTT assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HCT-116 |
| Confidence | 1 — Organism |
| Curated By | Autocuration |
Publication
Design, synthesis and biological evaluation of sphingosine-1-phosphate receptor 2 antagonists as potent 5-FU-resistance reversal agents for the treatment of colorectal cancer.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 22 | 4.96 | 6.75 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4871603 | — | — | 1 | 6.75 |
| CHEMBL4861095 | — | — | 1 | 5.29 |
| CHEMBL4858074 | — | — | 1 | 5.29 |
| CHEMBL4878547 | — | — | 1 | 5.29 |
| CHEMBL4874765 | — | — | 1 | 5.28 |
| CHEMBL4858060 | — | — | 1 | 5.28 |
| CHEMBL4852333 | — | — | 1 | 5.27 |
| CHEMBL4853969 | — | — | 1 | 5.21 |
| CHEMBL4846520 | — | — | 1 | 4.95 |
| CHEMBL4847029 | — | — | 1 | 4.94 |
| CHEMBL4865240 | — | — | 1 | 4.79 |
| CHEMBL1368758 | — | — | 1 | 4.77 |
| CHEMBL4862332 | — | — | 1 | 4.63 |
| CHEMBL4870233 | — | — | 1 | 4.63 |
| CHEMBL4846434 | — | — | 1 | 4.38 |
| CHEMBL4879008 | — | — | 1 | 4.38 |
| CHEMBL4866321 | — | — | 1 | 4.06 |
| CHEMBL4850828 | — | — | 1 | 4.03 |
| CHEMBL4855889 | — | — | 1 | - |
| CHEMBL4858648 | — | — | 1 | - |
| CHEMBL4855447 | — | — | 1 | - |
| CHEMBL185 | FLUOROURACIL | 4.0 | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4871603 | — | EC50 | = | 180.0 | nM | 6.75 |
| CHEMBL4861095 | — | EC50 | = | 5120.0 | nM | 5.29 |
| CHEMBL4858074 | — | EC50 | = | 5130.0 | nM | 5.29 |
| CHEMBL4878547 | — | EC50 | = | 5130.0 | nM | 5.29 |
| CHEMBL4874765 | — | EC50 | = | 5230.0 | nM | 5.28 |
| CHEMBL4858060 | — | EC50 | = | 5260.0 | nM | 5.28 |
| CHEMBL4852333 | — | EC50 | = | 5350.0 | nM | 5.27 |
| CHEMBL4853969 | — | EC50 | = | 6130.0 | nM | 5.21 |
| CHEMBL4846520 | — | EC50 | = | 11180.0 | nM | 4.95 |
| CHEMBL4847029 | — | EC50 | = | 11400.0 | nM | 4.94 |
| CHEMBL4865240 | — | EC50 | = | 16130.0 | nM | 4.79 |
| CHEMBL1368758 | — | EC50 | = | 17130.0 | nM | 4.77 |
| CHEMBL4862332 | — | EC50 | = | 23160.0 | nM | 4.63 |
| CHEMBL4870233 | — | EC50 | = | 23400.0 | nM | 4.63 |
| CHEMBL4846434 | — | EC50 | = | 41500.0 | nM | 4.38 |
| CHEMBL4879008 | — | EC50 | = | 41500.0 | nM | 4.38 |
| CHEMBL4866321 | — | EC50 | = | 86210.0 | nM | 4.06 |
| CHEMBL4850828 | — | EC50 | = | 94210.0 | nM | 4.03 |
| CHEMBL4855889 | — | EC50 | = | 141500.0 | nM | - |
| CHEMBL4858648 | — | EC50 | = | 660120.0 | nM | - |
| CHEMBL4855447 | — | EC50 | = | 449270.0 | nM | - |
| CHEMBL185 | FLUOROURACIL | EC50 | > | 1000000.0 | nM | - |