Assay Detail
Binding
CHEMBL4714778
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant wild type human KNa1.1 expressed in human HEK-TREX cells at -80 mV holding potential by automated patch clamp assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | T-REx-293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Potassium channel subfamily T member 1 (CHEMBL4739688) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Discovery of the First Orally Available, Selective K1.1 Inhibitor: In Vitro and In Vivo Activity of an Oxadiazole Series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 6.12 | 7.80 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4763955 | — | — | 1 | 7.80 |
| CHEMBL4788669 | — | — | 1 | 7.57 |
| CHEMBL4741793 | — | — | 1 | 7.40 |
| CHEMBL4754084 | — | — | 1 | 7.21 |
| CHEMBL4783741 | — | — | 1 | 6.87 |
| CHEMBL4793291 | — | — | 1 | 6.78 |
| CHEMBL4786255 | — | — | 1 | 6.78 |
| CHEMBL4793279 | — | — | 1 | 6.71 |
| CHEMBL4750925 | — | — | 1 | 6.49 |
| CHEMBL4783466 | — | — | 1 | 6.47 |
| CHEMBL4795194 | — | — | 1 | 6.34 |
| CHEMBL4743249 | — | — | 1 | 6.30 |
| CHEMBL4781553 | — | — | 1 | 6.24 |
| CHEMBL4745211 | — | — | 1 | 6.13 |
| CHEMBL4758890 | — | — | 1 | 6.11 |
| CHEMBL4779088 | — | — | 1 | 6.01 |
| CHEMBL4750826 | — | — | 1 | 5.86 |
| CHEMBL4744857 | — | — | 1 | 5.85 |
| CHEMBL4789512 | — | — | 1 | 5.80 |
| CHEMBL4750807 | — | — | 1 | 5.73 |
| CHEMBL4740667 | — | — | 1 | 5.58 |
| CHEMBL4763819 | — | — | 1 | 5.48 |
| CHEMBL4777757 | — | — | 1 | 5.35 |
| CHEMBL4751954 | — | — | 1 | 5.28 |
| CHEMBL4776478 | — | — | 1 | 5.20 |
| CHEMBL4759833 | — | — | 1 | 5.19 |
| CHEMBL4744290 | — | — | 1 | 5.03 |
| CHEMBL4793050 | — | — | 1 | 4.94 |
| CHEMBL4755742 | — | — | 1 | 4.93 |
| CHEMBL4797412 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4763955 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4788669 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL4741793 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL4754084 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4783741 | — | IC50 | = | 136.0 | nM | 6.87 |
| CHEMBL4793291 | — | IC50 | = | 167.0 | nM | 6.78 |
| CHEMBL4786255 | — | IC50 | = | 165.0 | nM | 6.78 |
| CHEMBL4793279 | — | IC50 | = | 195.0 | nM | 6.71 |
| CHEMBL4750925 | — | IC50 | = | 322.0 | nM | 6.49 |
| CHEMBL4783466 | — | IC50 | = | 335.0 | nM | 6.47 |
| CHEMBL4795194 | — | IC50 | = | 454.0 | nM | 6.34 |
| CHEMBL4743249 | — | IC50 | = | 505.0 | nM | 6.30 |
| CHEMBL4781553 | — | IC50 | = | 573.0 | nM | 6.24 |
| CHEMBL4745211 | — | IC50 | = | 744.0 | nM | 6.13 |
| CHEMBL4758890 | — | IC50 | = | 778.0 | nM | 6.11 |
| CHEMBL4779088 | — | IC50 | = | 977.0 | nM | 6.01 |
| CHEMBL4750826 | — | IC50 | = | 1373.0 | nM | 5.86 |
| CHEMBL4744857 | — | IC50 | = | 1410.0 | nM | 5.85 |
| CHEMBL4789512 | — | IC50 | = | 1597.0 | nM | 5.80 |
| CHEMBL4750807 | — | IC50 | = | 1876.0 | nM | 5.73 |
| CHEMBL4740667 | — | IC50 | = | 2642.0 | nM | 5.58 |
| CHEMBL4763819 | — | IC50 | = | 3314.0 | nM | 5.48 |
| CHEMBL4777757 | — | IC50 | = | 4466.0 | nM | 5.35 |
| CHEMBL4751954 | — | IC50 | = | 5245.0 | nM | 5.28 |
| CHEMBL4776478 | — | IC50 | = | 6282.0 | nM | 5.20 |
| CHEMBL4759833 | — | IC50 | = | 6489.0 | nM | 5.19 |
| CHEMBL4744290 | — | IC50 | = | 9285.0 | nM | 5.03 |
| CHEMBL4793050 | — | IC50 | = | 11430.0 | nM | 4.94 |
| CHEMBL4755742 | — | IC50 | = | 11800.0 | nM | 4.93 |
| CHEMBL4797412 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4753774 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4743513 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4781377 | — | IC50 | > | 30000.0 | nM | - |
| CHEMBL4780006 | — | IC50 | > | 30000.0 | nM | - |