Assay Detail
Binding
CHEMBL3707997
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibitory Assay: FCPIA Characterization of RGS Inhibitory Activity: CCG-50014 (FIG. 1) was originally identified as a potential inhibitor of RGS8 and RGS16 in a polyplex high throughput screen to identify inhibitors of the RGS-Gα interaction [4]. This activity was confirmed by analyzing the effect of CCG-50014 on several different RGS proteins with freshly reordered compound using multiplexed FCPIA. CCG-50014 fully inhibited several different RGS proteins including RGS4, 8, 16, and 19, but did not have activity on RGS7 or a mutated form of RGS4 that lacks cysteine residues.
4
Total Activities
4
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
Regulator of G-protein signaling 8 (CHEMBL2034803) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Small molecule inhibitors of RGS proteins
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 4.96 | 4.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1917204 | — | — | 1 | 4.96 |
| CHEMBL2037370 | — | — | 1 | - |
| CHEMBL3653656 | — | — | 1 | - |
| CHEMBL2037371 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1917204 | — | IC50 | = | 11000.0 | nM | 4.96 |
| CHEMBL2037370 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL3653656 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL2037371 | — | IC50 | > | 100000.0 | nM | - |