Assay Detail
Binding
CHEMBL4670407
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Biased agonist activity at Gal4-VP16 transcription factor linked human 5-HT1A receptor expressed in human U2OS cells assessed as induction of beta-arrestin2 recruitment measured after 5 hrs by Tango assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | U2OS |
| 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 | 7.52 | 10.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4752177 | — | — | 1 | 10.60 |
| CHEMBL4796345 | — | — | 1 | 10.05 |
| CHEMBL4790600 | — | — | 1 | 9.49 |
| CHEMBL4751777 | — | — | 1 | 9.43 |
| CHEMBL4786067 | — | — | 1 | 8.64 |
| CHEMBL4777581 | — | — | 1 | 8.55 |
| CHEMBL4750444 | — | — | 1 | 8.08 |
| CHEMBL4741857 | — | — | 1 | 7.98 |
| CHEMBL56 | 8-OH-DPAT | — | 1 | 7.84 |
| CHEMBL4746386 | — | — | 1 | 7.76 |
| CHEMBL4760271 | — | — | 1 | 7.61 |
| CHEMBL4739908 | — | — | 1 | 7.46 |
| CHEMBL4760621 | — | — | 1 | 7.27 |
| CHEMBL4760666 | — | — | 1 | 7.22 |
| CHEMBL4747425 | — | — | 1 | 7.06 |
| CHEMBL4790662 | — | — | 1 | 6.91 |
| CHEMBL39 | SEROTONIN | 3.0 | 1 | 6.89 |
| CHEMBL4781985 | — | — | 1 | 6.79 |
| CHEMBL49 | BUSPIRONE | 4.0 | 1 | 6.73 |
| CHEMBL230963 | — | — | 1 | 6.71 |
| CHEMBL4797282 | — | — | 1 | 6.65 |
| CHEMBL4752833 | — | — | 1 | 6.21 |
| CHEMBL4740430 | — | — | 1 | 6.14 |
| CHEMBL4797752 | — | — | 1 | 6.01 |
| CHEMBL4747083 | — | — | 1 | 5.79 |
| CHEMBL4753394 | — | — | 1 | 5.60 |
| CHEMBL4755058 | — | — | 1 | - |
| CHEMBL4756041 | — | — | 1 | - |
| CHEMBL4756233 | — | — | 1 | - |
| CHEMBL4757755 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4752177 | — | EC50 | = | 0.02512 | nM | 10.60 |
| CHEMBL4796345 | — | EC50 | = | 0.08913 | nM | 10.05 |
| CHEMBL4790600 | — | EC50 | = | 0.3236 | nM | 9.49 |
| CHEMBL4751777 | — | EC50 | = | 0.3715 | nM | 9.43 |
| CHEMBL4786067 | — | EC50 | = | 2.291 | nM | 8.64 |
| CHEMBL4777581 | — | EC50 | = | 2.818 | nM | 8.55 |
| CHEMBL4750444 | — | EC50 | = | 8.318 | nM | 8.08 |
| CHEMBL4741857 | — | EC50 | = | 10.47 | nM | 7.98 |
| CHEMBL56 | 8-OH-DPAT | EC50 | = | 14.45 | nM | 7.84 |
| CHEMBL4746386 | — | EC50 | = | 17.38 | nM | 7.76 |
| CHEMBL4760271 | — | EC50 | = | 24.55 | nM | 7.61 |
| CHEMBL4739908 | — | EC50 | = | 34.67 | nM | 7.46 |
| CHEMBL4760621 | — | EC50 | = | 53.7 | nM | 7.27 |
| CHEMBL4760666 | — | EC50 | = | 60.26 | nM | 7.22 |
| CHEMBL4747425 | — | EC50 | = | 87.1 | nM | 7.06 |
| CHEMBL4790662 | — | EC50 | = | 123.03 | nM | 6.91 |
| CHEMBL39 | SEROTONIN | EC50 | = | 128.82 | nM | 6.89 |
| CHEMBL4781985 | — | EC50 | = | 162.18 | nM | 6.79 |
| CHEMBL49 | BUSPIRONE | EC50 | = | 186.21 | nM | 6.73 |
| CHEMBL230963 | — | EC50 | = | 194.98 | nM | 6.71 |
| CHEMBL4797282 | — | EC50 | = | 223.87 | nM | 6.65 |
| CHEMBL4752833 | — | EC50 | = | 616.6 | nM | 6.21 |
| CHEMBL4740430 | — | EC50 | = | 724.44 | nM | 6.14 |
| CHEMBL4797752 | — | EC50 | = | 977.24 | nM | 6.01 |
| CHEMBL4747083 | — | EC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL4753394 | — | EC50 | = | 2511.89 | nM | 5.60 |
| CHEMBL4755058 | — | EC50 | = | 0.0002089 | nM | - |
| CHEMBL4756041 | — | EC50 | = | 0.001479 | nM | - |
| CHEMBL4756233 | — | EC50 | = | 2.138e-05 | nM | - |
| CHEMBL4757755 | — | EC50 | = | 0.005129 | nM | - |