Assay Detail
Binding
CHEMBL2174319
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I]26RFa from human GPR103 expressed in HEK293 cells incubated for 1 h by gamma counter based method
4
Total Activities
4
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
Pyroglutamylated RF-amide peptide receptor (CHEMBL5852) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Rational design of a low molecular weight, stable, potent, and long-lasting GPR103 aza-β3-pseudopeptide agonist.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 4 | 6.30 | 8.90 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1802413 | — | — | 1 | 8.90 |
| CHEMBL2170403 | — | — | 1 | 5.70 |
| CHEMBL2170390 | — | — | 1 | 5.53 |
| CHEMBL1802425 | — | — | 1 | 5.06 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1802413 | — | IC50 | = | 1.26 | nM | 8.90 |
| CHEMBL2170403 | — | IC50 | = | 1994.0 | nM | 5.70 |
| CHEMBL2170390 | — | IC50 | = | 2987.0 | nM | 5.53 |
| CHEMBL1802425 | — | IC50 | = | 8730.0 | nM | 5.06 |