Assay Detail
Binding
CHEMBL5731393
Review assay metadata, readout intent, target linkage, and publication context from the same page.
E-VIPR Optical Membrane Potential Assay: Sodium channels are voltage-dependent proteins that can be activated by inducing membrane voltage changes by applying electric fields. The electrical stimulation instrument and methods of use are described in Ion Channel Assay Methods PCT/US01/21652, herein incorporated by reference and are referred to as E-VIPR. The instrument comprises a microtiter plate handler, an optical system for exciting the coumarin dye while simultaneously recording the coumarin and oxonol emissions, a waveform generator, a current- or voltage-controlled amplifier, and a device for inserting electrodes in well. Under integrated computer control, this instrument passes user-programmed electrical stimulus protocols to cells within the wells of the microtiter plate.
480
Total Activities
158
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Pyridone amides as modulators of sodium channels
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 160 | 6.64 | 9.00 |
| kon | 160 | - | - |
| k_off | 160 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3678273 | — | — | 3 | 9.00 |
| CHEMBL3683097 | — | — | 3 | 8.70 |
| CHEMBL3678270 | — | — | 3 | 8.52 |
| CHEMBL3683093 | — | — | 3 | 8.30 |
| CHEMBL3678272 | — | — | 3 | 8.22 |
| CHEMBL3678274 | — | — | 3 | 8.15 |
| CHEMBL3683092 | — | — | 3 | 8.00 |
| CHEMBL3678193 | — | — | 3 | 7.96 |
| CHEMBL5956589 | — | — | 3 | 7.96 |
| CHEMBL3683094 | — | — | 3 | 7.96 |
| CHEMBL3678248 | — | — | 3 | 7.92 |
| CHEMBL6036660 | — | — | 3 | 7.89 |
| CHEMBL3678234 | — | — | 3 | 7.89 |
| CHEMBL3678173 | — | — | 3 | 7.85 |
| CHEMBL3678179 | — | — | 3 | 7.85 |
| CHEMBL3678249 | — | — | 3 | 7.80 |
| CHEMBL3678271 | — | — | 3 | 7.80 |
| CHEMBL3678194 | — | — | 6 | 7.77 |
| CHEMBL3678225 | — | — | 3 | 7.75 |
| CHEMBL3678213 | — | — | 3 | 7.72 |
| CHEMBL3678268 | — | — | 3 | 7.72 |
| CHEMBL3678207 | — | — | 3 | 7.70 |
| CHEMBL5795728 | — | — | 3 | 7.62 |
| CHEMBL3678242 | — | — | 3 | 7.58 |
| CHEMBL3678250 | — | — | 3 | 7.58 |
| CHEMBL3678247 | — | — | 3 | 7.57 |
| CHEMBL3678192 | — | — | 3 | 7.55 |
| CHEMBL3678238 | — | — | 3 | 7.54 |
| CHEMBL3678183 | — | — | 3 | 7.52 |
| CHEMBL3678217 | — | — | 3 | 7.52 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3678273 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL3683097 | — | IC50 | = | 2.0 | nM | 8.70 |
| CHEMBL3678270 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL3683093 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL3678272 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL3678274 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL3683092 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL3678193 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3683094 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL5956589 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL3678248 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL6036660 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3678234 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL3678179 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3678173 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL3678249 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3678271 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL3678194 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL3678225 | — | IC50 | = | 18.0 | nM | 7.75 |
| CHEMBL3678213 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3678268 | — | IC50 | = | 19.0 | nM | 7.72 |
| CHEMBL3678207 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5795728 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL3678250 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3678242 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL3678247 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL3678192 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL3678238 | — | IC50 | = | 29.0 | nM | 7.54 |
| CHEMBL3678217 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3678230 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3678183 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL3678239 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL3678221 | — | IC50 | = | 32.0 | nM | 7.50 |
| CHEMBL3678224 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL6032483 | — | IC50 | = | 35.0 | nM | 7.46 |
| CHEMBL5909547 | — | IC50 | = | 36.0 | nM | 7.44 |
| CHEMBL3678228 | — | IC50 | = | 37.0 | nM | 7.43 |
| CHEMBL3678168 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL3678203 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL3678191 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3683091 | — | IC50 | = | 44.0 | nM | 7.36 |
| CHEMBL3678244 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3678243 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL3678216 | — | IC50 | = | 47.0 | nM | 7.33 |
| CHEMBL3678170 | — | IC50 | = | 50.0 | nM | 7.30 |
| CHEMBL3678200 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3678236 | — | IC50 | = | 51.0 | nM | 7.29 |
| CHEMBL3683095 | — | IC50 | = | 52.0 | nM | 7.28 |
| CHEMBL3639770 | — | IC50 | = | 54.0 | nM | 7.27 |
| CHEMBL3678237 | — | IC50 | = | 54.0 | nM | 7.27 |