Assay Detail
Binding
CHEMBL4236905
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells by Barracuda automated patch clamp assay
30
Total Activities
29
Compounds Tested
2
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
Discovery of ( S)-3-(3-(3,5-Dimethyl-1 H-pyrazol-1-yl)phenyl)-4-(( R)-3-(2-(5,6,7,8-tetrahydro-1,8-naphthyridin-2-yl)ethyl)pyrrolidin-1-yl)butanoic Acid, a Nonpeptidic αvβ6 Integrin Inhibitor for the Inhaled Treatment of Idiopathic Pulmonary Fibrosis.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 4.73 | 5.90 |
| pIC50 | 4 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4242175 | — | — | 1 | 5.90 |
| CHEMBL4242635 | — | — | 1 | 5.30 |
| CHEMBL4247617 | — | — | 1 | 5.00 |
| CHEMBL4241824 | GSK-3008348 FREE BASE | 1.0 | 1 | 4.50 |
| CHEMBL4249172 | — | — | 1 | 4.50 |
| CHEMBL4250148 | — | — | 1 | 4.50 |
| CHEMBL4244784 | — | — | 2 | 4.40 |
| CHEMBL4247149 | — | — | 1 | 4.40 |
| CHEMBL4239085 | — | — | 1 | 4.40 |
| CHEMBL4237868 | — | — | 1 | - |
| CHEMBL4243686 | — | — | 1 | - |
| CHEMBL4246111 | — | — | 1 | - |
| CHEMBL4240155 | — | — | 1 | - |
| CHEMBL4239588 | — | — | 1 | - |
| CHEMBL4243367 | — | — | 1 | - |
| CHEMBL4251444 | — | — | 1 | - |
| CHEMBL4248953 | — | — | 1 | - |
| CHEMBL4238909 | — | — | 1 | - |
| CHEMBL4238482 | — | — | 1 | - |
| CHEMBL4237919 | — | — | 1 | - |
| CHEMBL4241584 | — | — | 1 | - |
| CHEMBL4248589 | — | — | 1 | - |
| CHEMBL4238556 | — | — | 1 | - |
| CHEMBL4242732 | — | — | 1 | - |
| CHEMBL4237498 | — | — | 1 | - |
| CHEMBL4249629 | — | — | 1 | - |
| CHEMBL4245368 | — | — | 1 | - |
| CHEMBL4242263 | — | — | 1 | - |
| CHEMBL4245829 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4242175 | — | IC50 | = | 1258.93 | nM | 5.90 |
| CHEMBL4242635 | — | IC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL4247617 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4241824 | GSK-3008348 FREE BASE | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4249172 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4250148 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4247149 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL4244784 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL4244784 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL4239085 | — | IC50 | = | 39810.72 | nM | 4.40 |
| CHEMBL4237868 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4243686 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4246111 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4240155 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4239588 | — | pIC50 | - | — | - | |
| CHEMBL4243367 | — | IC50 | > | 63095.73 | nM | - |
| CHEMBL4251444 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4248953 | — | pIC50 | - | — | - | |
| CHEMBL4238909 | — | IC50 | > | 63095.73 | nM | - |
| CHEMBL4238482 | — | pIC50 | - | — | - | |
| CHEMBL4237919 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4241584 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4245829 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4245368 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4249629 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4248589 | — | IC50 | > | 63095.73 | nM | - |
| CHEMBL4238556 | — | pIC50 | - | — | - | |
| CHEMBL4237498 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4242732 | — | IC50 | > | 50118.72 | nM | - |
| CHEMBL4242263 | — | IC50 | > | 63095.73 | nM | - |