Assay Detail
Functional
CHEMBL5442700
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCR PRESTO-Tango dose-response in antagonist mode with target: CX3CR1
32
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HTLA |
| Category | GPCR beta-arrestin recruitment assay |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
EUbOPEN Chemogenomics Library - GPCR Dose-Respose
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 24 | 5.51 | 5.80 |
| EC50 | 8 | 5.69 | 6.51 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL403225 | — | — | 1 | 6.51 |
| CHEMBL3819292 | — | — | 1 | 6.41 |
| CHEMBL3039531 | DANIRIXIN | 2.0 | 1 | 6.10 |
| CHEMBL3310783 | — | — | 1 | 5.85 |
| CHEMBL1256876 | — | — | 1 | 5.80 |
| CHEMBL2018875 | — | — | 1 | 5.67 |
| CHEMBL531742 | — | — | 1 | 5.58 |
| CHEMBL5075931 | — | — | 1 | 5.53 |
| CHEMBL567 | PERPHENAZINE | 4.0 | 1 | 5.53 |
| CHEMBL1201082 | FLUOXETINE HYDROCHLORIDE | 4.0 | 1 | 5.52 |
| CHEMBL1263 | SALMETEROL | 4.0 | 1 | 5.50 |
| CHEMBL2111101 | PIMAVANSERIN | 4.0 | 1 | 5.49 |
| CHEMBL543113 | — | — | 1 | 5.48 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | 4.0 | 1 | 5.43 |
| CHEMBL1256645 | — | — | 1 | 5.42 |
| CHEMBL542139 | — | — | 1 | 5.42 |
| CHEMBL4760718 | — | — | 1 | 5.41 |
| CHEMBL1474387 | — | — | 1 | 5.21 |
| CHEMBL502182 | ELAGOLIX SODIUM | 4.0 | 1 | 5.04 |
| CHEMBL484929 | — | — | 1 | 4.75 |
| CHEMBL2164327 | — | — | 1 | - |
| CHEMBL1200411 | ROPINIROLE HYDROCHLORIDE | 4.0 | 1 | - |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | 4.0 | 1 | - |
| CHEMBL5089526 | — | — | 1 | - |
| CHEMBL469695 | — | — | 1 | - |
| CHEMBL267495 | NALFURAFINE | 4.0 | 1 | - |
| CHEMBL540612 | — | — | 1 | - |
| CHEMBL5079621 | — | — | 1 | - |
| CHEMBL1368005 | — | — | 1 | - |
| CHEMBL2018969 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL403225 | — | EC50 | = | 307.81 | nM | 6.51 |
| CHEMBL3819292 | — | EC50 | = | 385.94 | nM | 6.41 |
| CHEMBL3039531 | DANIRIXIN | EC50 | = | 800.53 | nM | 6.10 |
| CHEMBL3310783 | — | EC50 | = | 1424.24 | nM | 5.85 |
| CHEMBL1256876 | — | IC50 | = | 1575.75 | nM | 5.80 |
| CHEMBL2018875 | — | IC50 | = | 2142.54 | nM | 5.67 |
| CHEMBL531742 | — | IC50 | = | 2597.49 | nM | 5.58 |
| CHEMBL5075931 | — | IC50 | = | 2929.37 | nM | 5.53 |
| CHEMBL567 | PERPHENAZINE | IC50 | = | 2949.1 | nM | 5.53 |
| CHEMBL1201082 | FLUOXETINE HYDROCHLORIDE | IC50 | = | 3001.59 | nM | 5.52 |
| CHEMBL1263 | SALMETEROL | IC50 | = | 3138.6 | nM | 5.50 |
| CHEMBL2111101 | PIMAVANSERIN | IC50 | = | 3258.17 | nM | 5.49 |
| CHEMBL543113 | — | IC50 | = | 3341.56 | nM | 5.48 |
| CHEMBL1722209 | TOLTERODINE TARTRATE | EC50 | = | 3737.22 | nM | 5.43 |
| CHEMBL542139 | — | IC50 | = | 3831.6 | nM | 5.42 |
| CHEMBL1256645 | — | EC50 | = | 3833.9 | nM | 5.42 |
| CHEMBL4760718 | — | IC50 | = | 3932.99 | nM | 5.41 |
| CHEMBL1474387 | — | IC50 | = | 6124.84 | nM | 5.21 |
| CHEMBL502182 | ELAGOLIX SODIUM | EC50 | = | 9206.41 | nM | 5.04 |
| CHEMBL484929 | — | EC50 | = | 17564.2 | nM | 4.75 |
| CHEMBL2164327 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1200411 | ROPINIROLE HYDROCHLORIDE | IC50 | > | 10000.0 | nM | - |
| CHEMBL1200517 | DIHYDROERGOTAMINE MESYLATE | IC50 | > | 10000.0 | nM | - |
| CHEMBL5089526 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL469695 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL267495 | NALFURAFINE | IC50 | > | 10000.0 | nM | - |
| CHEMBL540612 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL5079621 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL1368005 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL2018969 | — | IC50 | > | 10000.0 | nM | - |
| CHEMBL582857 | NELIVAPTAN | IC50 | > | 10000.0 | nM | - |
| CHEMBL38182 | — | IC50 | > | 10000.0 | nM | - |