Assay Detail
Functional
CHEMBL4670409
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells co-expressing Galpha16/GPCR assessed as increase in calcium mobilization measured for 30 secs in presence of coelenterazine by aequorin-reporter gene based luminescence assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO-K1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Novel pERK1/2- or β-Arrestin-Preferring 5-HT Receptor-Biased Agonists: Diversified Therapeutic-like versus Side Effect Profile.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 7.08 | 9.52 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4751777 | — | — | 1 | 9.52 |
| CHEMBL4757755 | — | — | 1 | 8.45 |
| CHEMBL4756041 | — | — | 1 | 7.87 |
| CHEMBL4756233 | — | — | 1 | 7.84 |
| CHEMBL4755058 | — | — | 1 | 7.66 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 7.66 |
| CHEMBL4750444 | — | — | 1 | 7.53 |
| CHEMBL4796345 | — | — | 1 | 7.49 |
| CHEMBL4777581 | — | — | 1 | 7.42 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.42 |
| CHEMBL4752177 | — | — | 1 | 7.36 |
| CHEMBL4790600 | — | — | 1 | 7.27 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 7.23 |
| CHEMBL4741857 | — | — | 1 | 7.20 |
| CHEMBL4739908 | — | — | 1 | 7.16 |
| CHEMBL4786067 | — | — | 1 | 7.15 |
| CHEMBL4747425 | — | — | 1 | 7.00 |
| CHEMBL4781985 | — | — | 1 | 6.99 |
| CHEMBL4760666 | — | — | 1 | 6.86 |
| CHEMBL4760621 | — | — | 1 | 6.83 |
| CHEMBL4760271 | — | — | 1 | 6.82 |
| CHEMBL4797282 | — | — | 1 | 6.60 |
| CHEMBL230963 | — | — | 1 | 6.52 |
| CHEMBL4790662 | — | — | 1 | 6.50 |
| CHEMBL4746386 | — | — | 1 | 6.26 |
| CHEMBL4747083 | — | — | 1 | 6.21 |
| CHEMBL4752833 | — | — | 1 | 6.19 |
| CHEMBL4740430 | — | — | 1 | 6.14 |
| CHEMBL4753394 | — | — | 1 | 5.88 |
| CHEMBL4797752 | — | — | 1 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4751777 | — | EC50 | = | 0.302 | nM | 9.52 |
| CHEMBL4757755 | — | EC50 | = | 3.548 | nM | 8.45 |
| CHEMBL4756041 | — | EC50 | = | 13.49 | nM | 7.87 |
| CHEMBL4756233 | — | EC50 | = | 14.45 | nM | 7.84 |
| CHEMBL4755058 | — | EC50 | = | 21.88 | nM | 7.66 |
| CHEMBL56 | 8-OH-DPAT | EC50 | = | 21.88 | nM | 7.66 |
| CHEMBL4750444 | — | EC50 | = | 29.51 | nM | 7.53 |
| CHEMBL4796345 | — | EC50 | = | 32.36 | nM | 7.49 |
| CHEMBL4777581 | — | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL49 | BUSPIRONE | EC50 | = | 38.02 | nM | 7.42 |
| CHEMBL4752177 | — | EC50 | = | 43.65 | nM | 7.36 |
| CHEMBL4790600 | — | EC50 | = | 53.7 | nM | 7.27 |
| CHEMBL39 | SEROTONIN | EC50 | = | 58.88 | nM | 7.23 |
| CHEMBL4741857 | — | EC50 | = | 63.1 | nM | 7.20 |
| CHEMBL4739908 | — | EC50 | = | 69.18 | nM | 7.16 |
| CHEMBL4786067 | — | EC50 | = | 70.79 | nM | 7.15 |
| CHEMBL4747425 | — | EC50 | = | 100.0 | nM | 7.00 |
| CHEMBL4781985 | — | EC50 | = | 102.33 | nM | 6.99 |
| CHEMBL4760666 | — | EC50 | = | 138.04 | nM | 6.86 |
| CHEMBL4760621 | — | EC50 | = | 147.91 | nM | 6.83 |
| CHEMBL4760271 | — | EC50 | = | 151.36 | nM | 6.82 |
| CHEMBL4797282 | — | EC50 | = | 251.19 | nM | 6.60 |
| CHEMBL230963 | — | EC50 | = | 302.0 | nM | 6.52 |
| CHEMBL4790662 | — | EC50 | = | 316.23 | nM | 6.50 |
| CHEMBL4746386 | — | EC50 | = | 549.54 | nM | 6.26 |
| CHEMBL4747083 | — | EC50 | = | 616.6 | nM | 6.21 |
| CHEMBL4752833 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL4740430 | — | EC50 | = | 724.44 | nM | 6.14 |
| CHEMBL4753394 | — | EC50 | = | 1318.26 | nM | 5.88 |
| CHEMBL4797752 | — | EC50 | = | 5248.07 | nM | 5.28 |