Assay Detail
Binding
CHEMBL5147694
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human Nav 1.7 expressed in HEK293F cells incubated for 3 mins by FRET based membrane potential assay
49
Total Activities
49
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293F |
| Subcellular | Cell membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Sodium channel protein type 7 subunit alpha (CHEMBL3585) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of (R)-(3-fluoropyrrolidin-1-yl)(6-((5-(trifluoromethyl)pyridin-2-yl)oxy)quinolin-2-yl)methanone (ABBV-318) and analogs as small molecule Na<sub>v</sub>1.7/ Nav1.8 blockers for the treatment of pain.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 49 | 5.84 | 7.25 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | 4.0 | 1 | 7.25 |
| CHEMBL5196338 | — | — | 1 | 7.16 |
| CHEMBL5208962 | — | — | 1 | 7.10 |
| CHEMBL5178152 | — | — | 1 | 7.10 |
| CHEMBL5202508 | — | — | 1 | 7.05 |
| CHEMBL5194066 | — | — | 1 | 6.62 |
| CHEMBL5197315 | — | — | 1 | 6.58 |
| CHEMBL5173050 | — | — | 1 | 6.50 |
| CHEMBL5203589 | — | — | 1 | 6.32 |
| CHEMBL5173502 | — | — | 1 | 6.26 |
| CHEMBL5194991 | — | — | 1 | 6.25 |
| CHEMBL3947741 | — | — | 1 | 6.11 |
| CHEMBL3971777 | — | — | 1 | 6.09 |
| CHEMBL3926656 | — | — | 1 | 6.05 |
| CHEMBL3957193 | — | — | 1 | 6.04 |
| CHEMBL3896057 | — | — | 1 | 6.04 |
| CHEMBL5182301 | — | — | 1 | 6.03 |
| CHEMBL5170090 | — | — | 1 | 6.02 |
| CHEMBL3965189 | — | — | 1 | 6.01 |
| CHEMBL5186539 | — | — | 1 | 6.00 |
| CHEMBL3924034 | — | — | 1 | 5.96 |
| CHEMBL3929432 | — | — | 1 | 5.92 |
| CHEMBL3964900 | — | — | 1 | 5.83 |
| CHEMBL3950180 | — | — | 1 | 5.75 |
| CHEMBL3969113 | — | — | 1 | 5.74 |
| CHEMBL5179783 | — | — | 1 | 5.74 |
| CHEMBL5186480 | — | — | 1 | 5.73 |
| CHEMBL5180334 | — | — | 1 | 5.72 |
| CHEMBL3962762 | — | — | 1 | 5.70 |
| CHEMBL3960534 | — | — | 1 | 5.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL698 | TETRACAINE | IC50 | = | 56.0 | nM | 7.25 |
| CHEMBL5196338 | — | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL5178152 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5208962 | — | IC50 | = | 80.0 | nM | 7.10 |
| CHEMBL5202508 | — | IC50 | = | 90.0 | nM | 7.05 |
| CHEMBL5194066 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL5197315 | — | IC50 | = | 260.0 | nM | 6.58 |
| CHEMBL5173050 | — | IC50 | = | 320.0 | nM | 6.50 |
| CHEMBL5203589 | — | IC50 | = | 480.0 | nM | 6.32 |
| CHEMBL5173502 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL5194991 | — | IC50 | = | 560.0 | nM | 6.25 |
| CHEMBL3947741 | — | IC50 | = | 780.0 | nM | 6.11 |
| CHEMBL3971777 | — | IC50 | = | 810.0 | nM | 6.09 |
| CHEMBL3926656 | — | IC50 | = | 900.0 | nM | 6.05 |
| CHEMBL3896057 | — | IC50 | = | 910.0 | nM | 6.04 |
| CHEMBL3957193 | — | IC50 | = | 920.0 | nM | 6.04 |
| CHEMBL5182301 | — | IC50 | = | 940.0 | nM | 6.03 |
| CHEMBL5170090 | — | IC50 | = | 960.0 | nM | 6.02 |
| CHEMBL3965189 | — | IC50 | = | 980.0 | nM | 6.01 |
| CHEMBL5186539 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL3924034 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL3929432 | — | IC50 | = | 1190.0 | nM | 5.92 |
| CHEMBL3964900 | — | IC50 | = | 1470.0 | nM | 5.83 |
| CHEMBL3950180 | — | IC50 | = | 1760.0 | nM | 5.75 |
| CHEMBL3969113 | — | IC50 | = | 1820.0 | nM | 5.74 |
| CHEMBL5179783 | — | IC50 | = | 1840.0 | nM | 5.74 |
| CHEMBL5186480 | — | IC50 | = | 1860.0 | nM | 5.73 |
| CHEMBL5180334 | — | IC50 | = | 1910.0 | nM | 5.72 |
| CHEMBL3962762 | — | IC50 | = | 2010.0 | nM | 5.70 |
| CHEMBL3960534 | — | IC50 | = | 2070.0 | nM | 5.68 |
| CHEMBL3910270 | — | IC50 | = | 2380.0 | nM | 5.62 |
| CHEMBL3939162 | — | IC50 | = | 2480.0 | nM | 5.61 |
| CHEMBL3893530 | — | IC50 | = | 2440.0 | nM | 5.61 |
| CHEMBL3970885 | — | IC50 | = | 2800.0 | nM | 5.55 |
| CHEMBL3942849 | — | IC50 | = | 3010.0 | nM | 5.52 |
| CHEMBL3891495 | — | IC50 | = | 3300.0 | nM | 5.48 |
| CHEMBL3935365 | — | IC50 | = | 3280.0 | nM | 5.48 |
| CHEMBL3971533 | — | IC50 | = | 3480.0 | nM | 5.46 |
| CHEMBL3934019 | — | IC50 | = | 3650.0 | nM | 5.44 |
| CHEMBL5197085 | — | IC50 | = | 3860.0 | nM | 5.41 |
| CHEMBL3896584 | — | IC50 | = | 4600.0 | nM | 5.34 |
| CHEMBL3928398 | — | IC50 | = | 4630.0 | nM | 5.33 |
| CHEMBL3935612 | — | IC50 | = | 7120.0 | nM | 5.15 |
| CHEMBL3946117 | — | IC50 | = | 10500.0 | nM | 4.98 |
| CHEMBL5195306 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL3917696 | — | IC50 | = | 13300.0 | nM | 4.88 |
| CHEMBL5177918 | — | IC50 | = | 16000.0 | nM | 4.80 |
| CHEMBL3903851 | — | IC50 | = | 20000.0 | nM | 4.70 |
| CHEMBL5174656 | — | IC50 | = | 20000.0 | nM | 4.70 |