Assay Detail
Functional
CHEMBL812204
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Compound was tested for inhibition of daunomycin efflux in the resistant human T-lymphoblast cell line CEM vcr1000.
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Cell Type | CCRF-CEM |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Substituted 4-acylpyrazoles and 4-acylpyrazolones: synthesis and multidrug resistance-modulating activity.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 24 | 5.37 | 7.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2051956 | DEXNIGULDIPINE | 2.0 | 1 | 7.22 |
| CHEMBL6966 | VERAPAMIL | 4.0 | 1 | 6.92 |
| CHEMBL131005 | — | — | 1 | 6.68 |
| CHEMBL631 | PROPAFENONE | 4.0 | 1 | 6.50 |
| CHEMBL335658 | — | — | 1 | 6.17 |
| CHEMBL336833 | — | — | 1 | 6.05 |
| CHEMBL339825 | — | — | 1 | 5.97 |
| CHEMBL131459 | — | — | 1 | 5.92 |
| CHEMBL128333 | — | — | 1 | 5.57 |
| CHEMBL3144686 | — | — | 1 | 5.42 |
| CHEMBL340648 | — | — | 1 | 5.20 |
| CHEMBL446161 | — | — | 1 | 5.11 |
| CHEMBL128129 | — | — | 1 | 5.08 |
| CHEMBL435593 | — | — | 1 | 4.96 |
| CHEMBL339154 | — | — | 1 | 4.93 |
| CHEMBL130241 | — | — | 1 | 4.90 |
| CHEMBL130016 | — | — | 1 | 4.62 |
| CHEMBL128085 | — | — | 1 | 4.55 |
| CHEMBL338678 | — | — | 1 | 4.14 |
| CHEMBL338120 | — | — | 1 | 4.14 |
| CHEMBL339252 | — | — | 1 | 4.09 |
| CHEMBL129228 | — | — | 1 | 4.08 |
| CHEMBL129427 | — | — | 1 | - |
| CHEMBL3144687 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2051956 | DEXNIGULDIPINE | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL6966 | VERAPAMIL | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL131005 | — | EC50 | = | 210.0 | nM | 6.68 |
| CHEMBL631 | PROPAFENONE | EC50 | = | 320.0 | nM | 6.50 |
| CHEMBL335658 | — | EC50 | = | 680.0 | nM | 6.17 |
| CHEMBL336833 | — | EC50 | = | 890.0 | nM | 6.05 |
| CHEMBL339825 | — | EC50 | = | 1060.0 | nM | 5.97 |
| CHEMBL131459 | — | EC50 | = | 1210.0 | nM | 5.92 |
| CHEMBL128333 | — | EC50 | = | 2690.0 | nM | 5.57 |
| CHEMBL3144686 | — | EC50 | = | 3790.0 | nM | 5.42 |
| CHEMBL340648 | — | EC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL446161 | — | EC50 | = | 7760.0 | nM | 5.11 |
| CHEMBL128129 | — | EC50 | = | 8380.0 | nM | 5.08 |
| CHEMBL435593 | — | EC50 | = | 11030.0 | nM | 4.96 |
| CHEMBL339154 | — | EC50 | = | 11750.0 | nM | 4.93 |
| CHEMBL130241 | — | EC50 | = | 12590.0 | nM | 4.90 |
| CHEMBL130016 | — | EC50 | = | 24120.0 | nM | 4.62 |
| CHEMBL128085 | — | EC50 | = | 28210.0 | nM | 4.55 |
| CHEMBL338678 | — | EC50 | = | 72440.0 | nM | 4.14 |
| CHEMBL338120 | — | EC50 | = | 72440.0 | nM | 4.14 |
| CHEMBL339252 | — | EC50 | = | 81280.0 | nM | 4.09 |
| CHEMBL129228 | — | EC50 | = | 83180.0 | nM | 4.08 |
| CHEMBL129427 | — | EC50 | = | 123030.0 | nM | - |
| CHEMBL3144687 | — | EC50 | = | 272500.0 | nM | - |