Assay Detail
Binding
CHEMBL2072491
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [35S]MK499 from human Erg expressed in HEK293 cells after 60 mins by scintillation counting
15
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Voltage-gated inwardly rectifying potassium channel KCNH2 (CHEMBL240) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Stimulation of Glucose-Dependent Insulin Secretion by a Potent, Selective sst3 Antagonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 6.50 | 7.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2069504 | — | — | 2 | 7.60 |
| CHEMBL2069500 | — | — | 1 | 7.11 |
| CHEMBL2069506 | — | — | 1 | 7.00 |
| CHEMBL2069507 | — | — | 1 | 7.00 |
| CHEMBL2069505 | — | — | 1 | 6.92 |
| CHEMBL2069499 | — | — | 1 | 6.82 |
| CHEMBL2069501 | — | — | 1 | 6.75 |
| CHEMBL2069513 | — | — | 1 | 6.62 |
| CHEMBL2069502 | — | — | 1 | 6.42 |
| CHEMBL2069512 | — | — | 1 | 6.16 |
| CHEMBL2069503 | — | — | 1 | 6.14 |
| CHEMBL2069511 | — | — | 1 | 5.46 |
| CHEMBL2069509 | — | — | 1 | 5.29 |
| CHEMBL2069510 | — | — | 1 | 5.01 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2069504 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL2069504 | — | IC50 | = | 64.0 | nM | 7.19 |
| CHEMBL2069500 | — | IC50 | = | 77.0 | nM | 7.11 |
| CHEMBL2069506 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2069507 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL2069505 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL2069499 | — | IC50 | = | 150.0 | nM | 6.82 |
| CHEMBL2069501 | — | IC50 | = | 176.0 | nM | 6.75 |
| CHEMBL2069513 | — | IC50 | = | 240.0 | nM | 6.62 |
| CHEMBL2069502 | — | IC50 | = | 380.0 | nM | 6.42 |
| CHEMBL2069512 | — | IC50 | = | 700.0 | nM | 6.16 |
| CHEMBL2069503 | — | IC50 | = | 730.0 | nM | 6.14 |
| CHEMBL2069511 | — | IC50 | = | 3500.0 | nM | 5.46 |
| CHEMBL2069509 | — | IC50 | = | 5100.0 | nM | 5.29 |
| CHEMBL2069510 | — | IC50 | = | 9800.0 | nM | 5.01 |