Assay Detail
Binding
CHEMBL5737065
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Automated Whole-Cell Patch Clamp Assay to Detect TMEM16A Activity in Recombinant Cells: Compound activity was quantified by measuring the increase in current upon compound addition and expressing this as a percentage increase of baseline TMEM16A current level. Percentage increases in current were determined for each concentration and the data plotted as a function of concentration using either the Qpatch software or Graphpad Prism v6.05 providing the concentration which gave 50% of its maximal effect (EC50) and maximum efficacy (percentage of baseline increase). The method of calculating the results is illustrated in FIG. 1, which shows an example trace from the Qpatch TMEM16A assay. In FIG. 1, IBL equals baseline current, I[#1] equals the peak current during test compound concentration 1 incubation period and so on.
699
Total Activities
228
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
COMPOUNDS
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 233 | 6.47 | 8.00 |
| kon | 233 | - | - |
| k_off | 233 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5987751 | — | — | 3 | 8.00 |
| CHEMBL5748528 | — | — | 3 | 8.00 |
| CHEMBL5818335 | — | — | 3 | 8.00 |
| CHEMBL5923346 | — | — | 3 | 7.70 |
| CHEMBL5888912 | — | — | 3 | 7.70 |
| CHEMBL6035973 | — | — | 3 | 7.70 |
| CHEMBL6063625 | — | — | 3 | 7.70 |
| CHEMBL6027216 | — | — | 3 | 7.70 |
| CHEMBL5886634 | — | — | 3 | 7.40 |
| CHEMBL5751293 | — | — | 3 | 7.40 |
| CHEMBL5867107 | — | — | 3 | 7.40 |
| CHEMBL5794087 | — | — | 3 | 7.40 |
| CHEMBL5924873 | — | — | 3 | 7.30 |
| CHEMBL5874757 | — | — | 3 | 7.30 |
| CHEMBL5793913 | — | — | 3 | 7.30 |
| CHEMBL5854301 | — | — | 3 | 7.30 |
| CHEMBL5875064 | — | — | 3 | 7.30 |
| CHEMBL5974117 | — | — | 3 | 7.22 |
| CHEMBL5758425 | — | — | 3 | 7.22 |
| CHEMBL5911037 | — | — | 3 | 7.22 |
| CHEMBL6039401 | — | — | 3 | 7.22 |
| CHEMBL5869137 | — | — | 3 | 7.16 |
| CHEMBL6057591 | — | — | 3 | 7.16 |
| CHEMBL5965278 | — | — | 3 | 7.10 |
| CHEMBL5789360 | — | — | 3 | 7.05 |
| CHEMBL5957346 | — | — | 3 | 7.05 |
| CHEMBL6028707 | — | — | 3 | 7.05 |
| CHEMBL6061522 | — | — | 3 | 7.00 |
| CHEMBL5769067 | — | — | 6 | 7.00 |
| CHEMBL5979945 | — | — | 3 | 7.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5818335 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5987751 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL5748528 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6035973 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL6027216 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5888912 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5923346 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL6063625 | — | EC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5751293 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5867107 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5886634 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5794087 | — | EC50 | = | 40.0 | nM | 7.40 |
| CHEMBL5793913 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5874757 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5854301 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5875064 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5924873 | — | EC50 | = | 50.0 | nM | 7.30 |
| CHEMBL5911037 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5758425 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL6039401 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL5974117 | — | EC50 | = | 60.0 | nM | 7.22 |
| CHEMBL6057591 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5869137 | — | EC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5965278 | — | EC50 | = | 80.0 | nM | 7.10 |
| CHEMBL6028707 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5957346 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5789360 | — | EC50 | = | 90.0 | nM | 7.05 |
| CHEMBL6043593 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5979945 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5769067 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL6061522 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5912840 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL5985276 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL6055475 | — | EC50 | = | 110.0 | nM | 6.96 |
| CHEMBL6036293 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5872142 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5947400 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5822025 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL5775948 | — | EC50 | = | 120.0 | nM | 6.92 |
| CHEMBL6061429 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL5965194 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL6061358 | — | EC50 | = | 130.0 | nM | 6.89 |
| CHEMBL6027996 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5751623 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5937186 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5944799 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL5754879 | — | EC50 | = | 140.0 | nM | 6.85 |
| CHEMBL6033691 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5746392 | — | EC50 | = | 150.0 | nM | 6.82 |
| CHEMBL5928244 | — | EC50 | = | 150.0 | nM | 6.82 |