Assay Detail
Binding
CHEMBL948111
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Inhibition of Gardos channel in human RBC assessed as inhibition of ionomycin-stimulated [86Rb] efflux
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Intermediate conductance calcium-activated potassium channel protein 4 (CHEMBL4305) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Novel inhibitors of the Gardos channel for the treatment of sickle cell disease.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 23 | 7.24 | 8.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL42205 | — | — | 1 | 8.05 |
| CHEMBL272039 | — | — | 1 | 8.00 |
| CHEMBL405821 | SENICAPOC | 3.0 | 1 | 7.92 |
| CHEMBL260736 | — | — | 1 | 7.89 |
| CHEMBL272040 | — | — | 1 | 7.85 |
| CHEMBL270704 | — | — | 1 | 7.85 |
| CHEMBL273092 | — | — | 1 | 7.82 |
| CHEMBL270071 | — | — | 1 | 7.82 |
| CHEMBL408700 | — | — | 1 | 7.82 |
| CHEMBL260953 | — | — | 1 | 7.77 |
| CHEMBL406683 | — | — | 1 | 7.70 |
| CHEMBL261828 | — | — | 1 | 7.52 |
| CHEMBL261606 | — | — | 1 | 7.52 |
| CHEMBL270913 | — | — | 1 | 7.47 |
| CHEMBL258604 | — | — | 1 | 7.40 |
| CHEMBL272255 | TRIPHENYLMETHANAMINE | — | 1 | 7.16 |
| CHEMBL270495 | TRIPHENYLACETIC ACID METHYL ESTER | — | 1 | 6.48 |
| CHEMBL104 | CLOTRIMAZOLE | 4.0 | 1 | 6.44 |
| CHEMBL270288 | — | — | 1 | 6.26 |
| CHEMBL260107 | — | — | 1 | 5.76 |
| CHEMBL259899 | — | — | 1 | 5.50 |
| CHEMBL271167 | — | — | 1 | 5.37 |
| CHEMBL271207 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL42205 | — | IC50 | = | 9.0 | nM | 8.05 |
| CHEMBL272039 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL405821 | SENICAPOC | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL260736 | — | IC50 | = | 13.0 | nM | 7.89 |
| CHEMBL272040 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL270704 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL273092 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL270071 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL408700 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL260953 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL406683 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL261828 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL261606 | — | IC50 | = | 30.0 | nM | 7.52 |
| CHEMBL270913 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL258604 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL272255 | TRIPHENYLMETHANAMINE | IC50 | = | 70.0 | nM | 7.16 |
| CHEMBL270495 | TRIPHENYLACETIC ACID METHYL ESTER | IC50 | = | 330.0 | nM | 6.48 |
| CHEMBL104 | CLOTRIMAZOLE | IC50 | = | 360.0 | nM | 6.44 |
| CHEMBL270288 | — | IC50 | = | 550.0 | nM | 6.26 |
| CHEMBL260107 | — | IC50 | = | 1750.0 | nM | 5.76 |
| CHEMBL259899 | — | IC50 | = | 3150.0 | nM | 5.50 |
| CHEMBL271167 | — | IC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL271207 | — | IC50 | > | 10000.0 | nM | - |