Assay Detail
Binding
CHEMBL4670403
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Biased agonist activity at human 5-HT1A receptor stably expressed in CHO-K1 cells assessed as increase in ERK1/2 phosphorylation after 15 mins by Alphalisa assay
30
Total Activities
30
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| 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 | 28 | 8.61 | 10.99 |
| pEC50 | 2 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4790600 | — | — | 1 | 10.99 |
| CHEMBL4756233 | — | — | 1 | 10.53 |
| CHEMBL4796345 | — | — | 1 | 10.13 |
| CHEMBL4755058 | — | — | 1 | 9.75 |
| CHEMBL4777581 | — | — | 1 | 9.74 |
| CHEMBL4786067 | — | — | 1 | 9.40 |
| CHEMBL4756041 | — | — | 1 | 9.30 |
| CHEMBL4752177 | — | — | 1 | 9.23 |
| CHEMBL4741857 | — | — | 1 | 9.10 |
| CHEMBL4781985 | — | — | 1 | 8.86 |
| CHEMBL4760621 | — | — | 1 | 8.72 |
| CHEMBL4750444 | — | — | 1 | 8.68 |
| CHEMBL4739908 | — | — | 1 | 8.64 |
| CHEMBL230963 | — | — | 1 | 8.33 |
| CHEMBL4760271 | — | — | 1 | 8.24 |
| CHEMBL4747425 | — | — | 1 | 8.24 |
| CHEMBL4760666 | — | — | 1 | 8.22 |
| CHEMBL4790662 | — | — | 1 | 8.14 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 8.09 |
| CHEMBL4797282 | — | — | 1 | 7.99 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 7.82 |
| CHEMBL4752833 | — | — | 1 | 7.70 |
| CHEMBL4747083 | — | — | 1 | 7.68 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 7.48 |
| CHEMBL4753394 | — | — | 1 | 7.32 |
| CHEMBL4740430 | — | — | 1 | 7.25 |
| CHEMBL4797752 | — | — | 1 | 6.93 |
| CHEMBL4751777 | — | — | 1 | - |
| CHEMBL4746386 | — | — | 1 | - |
| CHEMBL4757755 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4790600 | — | EC50 | = | 0.01023 | nM | 10.99 |
| CHEMBL4756233 | — | EC50 | = | 0.02951 | nM | 10.53 |
| CHEMBL4796345 | — | EC50 | = | 0.07413 | nM | 10.13 |
| CHEMBL4755058 | — | EC50 | = | 0.1778 | nM | 9.75 |
| CHEMBL4777581 | — | EC50 | = | 0.182 | nM | 9.74 |
| CHEMBL4786067 | — | EC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL4756041 | — | EC50 | = | 0.5012 | nM | 9.30 |
| CHEMBL4752177 | — | EC50 | = | 0.5888 | nM | 9.23 |
| CHEMBL4741857 | — | EC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL4781985 | — | EC50 | = | 1.38 | nM | 8.86 |
| CHEMBL4760621 | — | EC50 | = | 1.905 | nM | 8.72 |
| CHEMBL4750444 | — | EC50 | = | 2.089 | nM | 8.68 |
| CHEMBL4739908 | — | EC50 | = | 2.291 | nM | 8.64 |
| CHEMBL230963 | — | EC50 | = | 4.677 | nM | 8.33 |
| CHEMBL4760271 | — | EC50 | = | 5.754 | nM | 8.24 |
| CHEMBL4747425 | — | EC50 | = | 5.754 | nM | 8.24 |
| CHEMBL4760666 | — | EC50 | = | 6.026 | nM | 8.22 |
| CHEMBL4790662 | — | EC50 | = | 7.244 | nM | 8.14 |
| CHEMBL56 | 8-OH-DPAT | EC50 | = | 8.128 | nM | 8.09 |
| CHEMBL4797282 | — | EC50 | = | 10.23 | nM | 7.99 |
| CHEMBL49 | BUSPIRONE | EC50 | = | 15.14 | nM | 7.82 |
| CHEMBL4752833 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL4747083 | — | EC50 | = | 20.89 | nM | 7.68 |
| CHEMBL39 | SEROTONIN | EC50 | = | 33.11 | nM | 7.48 |
| CHEMBL4753394 | — | EC50 | = | 47.86 | nM | 7.32 |
| CHEMBL4740430 | — | EC50 | = | 56.23 | nM | 7.25 |
| CHEMBL4797752 | — | EC50 | = | 117.49 | nM | 6.93 |
| CHEMBL4751777 | — | pEC50 | - | — | - | |
| CHEMBL4746386 | — | pEC50 | - | — | - | |
| CHEMBL4757755 | — | EC50 | = | 0.003631 | nM | - |