Assay Detail
Binding
CHEMBL4236906
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of human ERG expressed in HEK293 cells by Q-patch 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 | 23 | 4.97 | 6.10 |
| pIC50 | 7 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4251444 | — | — | 1 | 6.10 |
| CHEMBL4242635 | — | — | 1 | 5.70 |
| CHEMBL4242732 | — | — | 1 | 5.10 |
| CHEMBL4247149 | — | — | 1 | 5.00 |
| CHEMBL4241824 | GSK-3008348 FREE BASE | 1.0 | 1 | 4.90 |
| CHEMBL4250148 | — | — | 1 | 4.90 |
| CHEMBL4244784 | — | — | 2 | 4.90 |
| CHEMBL4249172 | — | — | 1 | 4.80 |
| CHEMBL4243367 | — | — | 1 | 4.60 |
| CHEMBL4240155 | — | — | 1 | 4.60 |
| CHEMBL4239085 | — | — | 1 | 4.50 |
| CHEMBL4238482 | — | — | 1 | - |
| CHEMBL4238909 | — | — | 1 | - |
| CHEMBL4248953 | — | — | 1 | - |
| CHEMBL4247617 | — | — | 1 | - |
| CHEMBL4239588 | — | — | 1 | - |
| CHEMBL4246111 | — | — | 1 | - |
| CHEMBL4243686 | — | — | 1 | - |
| CHEMBL4237868 | — | — | 1 | - |
| CHEMBL4237919 | — | — | 1 | - |
| CHEMBL4241584 | — | — | 1 | - |
| CHEMBL4245829 | — | — | 1 | - |
| CHEMBL4245368 | — | — | 1 | - |
| CHEMBL4249629 | — | — | 1 | - |
| CHEMBL4237498 | — | — | 1 | - |
| CHEMBL4242175 | — | — | 1 | - |
| CHEMBL4248589 | — | — | 1 | - |
| CHEMBL4242263 | — | — | 1 | - |
| CHEMBL4238556 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4251444 | — | IC50 | = | 794.33 | nM | 6.10 |
| CHEMBL4242635 | — | IC50 | = | 1995.26 | nM | 5.70 |
| CHEMBL4242732 | — | IC50 | = | 7943.28 | nM | 5.10 |
| CHEMBL4247149 | — | IC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL4241824 | GSK-3008348 FREE BASE | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4250148 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4244784 | — | IC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL4249172 | — | IC50 | = | 15848.93 | nM | 4.80 |
| CHEMBL4243367 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4240155 | — | IC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL4244784 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4239085 | — | IC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL4238482 | — | pIC50 | - | — | - | |
| CHEMBL4238909 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4248953 | — | pIC50 | - | — | - | |
| CHEMBL4247617 | — | pIC50 | - | — | - | |
| CHEMBL4239588 | — | pIC50 | - | — | - | |
| CHEMBL4246111 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4243686 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4237868 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4237919 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4241584 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4245829 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4245368 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4249629 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4237498 | — | IC50 | > | 31622.78 | nM | - |
| CHEMBL4242175 | — | pIC50 | - | — | - | |
| CHEMBL4248589 | — | pIC50 | - | — | - | |
| CHEMBL4238556 | — | pIC50 | - | — | - | |
| CHEMBL4242263 | — | IC50 | > | 31622.78 | nM | - |