Assay Detail
Functional
CHEMBL664980
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of recombinant human corticotropin releasing factor receptor 2 beta (CRF2beta) assayed using nonselective [125I]-labeled agonist [Tyr0,Glu1,Nle17]-sauvagine as radioligand
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Target
Corticotropin-releasing factor receptor 2 (CHEMBL4069) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Potent and long-acting corticotropin releasing factor (CRF) receptor 2 selective peptide competitive antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 28 | 8.51 | 9.38 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL2368116 | — | — | 1 | 9.38 |
| CHEMBL2370929 | — | — | 1 | 9.29 |
| CHEMBL2370916 | — | — | 1 | 9.24 |
| CHEMBL2370926 | — | — | 1 | 9.22 |
| CHEMBL2370933 | — | — | 1 | 9.21 |
| CHEMBL1794009 | — | — | 1 | 9.21 |
| CHEMBL2370938 | — | — | 1 | 9.14 |
| CHEMBL2370927 | — | — | 1 | 9.04 |
| CHEMBL2370915 | — | — | 1 | 8.96 |
| CHEMBL2370939 | — | — | 1 | 8.92 |
| CHEMBL2370940 | — | — | 1 | 8.89 |
| CHEMBL2370917 | — | — | 1 | 8.89 |
| CHEMBL439883 | SAUVAGINE | — | 1 | 8.80 |
| CHEMBL2370914 | — | — | 1 | 8.72 |
| CHEMBL2369694 | — | — | 1 | 8.31 |
| CHEMBL2369741 | — | — | 1 | 8.30 |
| CHEMBL2370931 | — | — | 1 | 8.26 |
| CHEMBL440057 | HUMAN CORTICOTROPIN RELEASING FACTOR | — | 1 | 8.21 |
| CHEMBL2370930 | — | — | 1 | 8.21 |
| CHEMBL1794010 | — | — | 1 | 8.00 |
| CHEMBL2370920 | — | — | 1 | 7.75 |
| CHEMBL1794007 | — | — | 1 | 7.34 |
| CHEMBL2369693 | — | — | 1 | 7.22 |
| CHEMBL1794006 | LENEAR ASTRESSIN | — | 1 | 7.16 |
| CHEMBL2370924 | — | — | 1 | 7.09 |
| CHEMBL2369740 | — | — | 1 | - |
| CHEMBL2370921 | — | — | 1 | - |
| CHEMBL2370941 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL2368116 | — | IC50 | = | 0.42 | nM | 9.38 |
| CHEMBL2370929 | — | IC50 | = | 0.51 | nM | 9.29 |
| CHEMBL2370916 | — | IC50 | = | 0.57 | nM | 9.24 |
| CHEMBL2370926 | — | IC50 | = | 0.6 | nM | 9.22 |
| CHEMBL2370933 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL1794009 | — | IC50 | = | 0.62 | nM | 9.21 |
| CHEMBL2370938 | — | IC50 | = | 0.72 | nM | 9.14 |
| CHEMBL2370927 | — | IC50 | = | 0.92 | nM | 9.04 |
| CHEMBL2370915 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL2370939 | — | IC50 | = | 1.2 | nM | 8.92 |
| CHEMBL2370940 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL2370917 | — | IC50 | = | 1.3 | nM | 8.89 |
| CHEMBL439883 | SAUVAGINE | IC50 | = | 1.6 | nM | 8.80 |
| CHEMBL2370914 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL2369694 | — | IC50 | = | 4.9 | nM | 8.31 |
| CHEMBL2369741 | — | IC50 | = | 5.0 | nM | 8.30 |
| CHEMBL2370931 | — | IC50 | = | 5.5 | nM | 8.26 |
| CHEMBL440057 | HUMAN CORTICOTROPIN RELEASING FACTOR | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL2370930 | — | IC50 | = | 6.2 | nM | 8.21 |
| CHEMBL1794010 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL2370920 | — | IC50 | = | 17.8 | nM | 7.75 |
| CHEMBL1794007 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL2369693 | — | IC50 | = | 60.0 | nM | 7.22 |
| CHEMBL1794006 | LENEAR ASTRESSIN | IC50 | = | 69.0 | nM | 7.16 |
| CHEMBL2370924 | — | IC50 | = | 81.0 | nM | 7.09 |
| CHEMBL2369740 | — | IC50 | > | 500.0 | nM | - |
| CHEMBL2370921 | — | IC50 | > | 100.0 | nM | - |
| CHEMBL2370941 | — | IC50 | > | 100.0 | nM | - |