Assay Detail
Functional
CHEMBL5665202
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at MRGPRX2 (unknown origin) expressed in HTLA cells assessed as induction of beta-arrestin 2 recruitment incubated for 18 to 24 hrs by PRESTO-Tango assay
100
Total Activities
96
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HTLA |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Mas-related G-protein coupled receptor member X2 (CHEMBL5849) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
In silico design of novel probes for the atypical opioid receptor MRGPRX2.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 54 | 5.12 | 6.84 |
| pEC50 | 46 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5192321 | — | — | 1 | 6.84 |
| CHEMBL327745 | — | — | 1 | 6.37 |
| CHEMBL1644379 | COMPLANADINE A | — | 1 | 6.16 |
| CHEMBL4520293 | (R)-ZINC-3573 | — | 1 | 6.13 |
| CHEMBL1200490 | CETRORELIX | 4.0 | 1 | 6.09 |
| CHEMBL5665379 | — | — | 1 | 5.74 |
| CHEMBL5665388 | — | — | 1 | 5.52 |
| CHEMBL5665416 | — | — | 1 | 5.50 |
| CHEMBL52440 | DEXTROMETHORPHAN | 4.0 | 1 | 5.49 |
| CHEMBL5665374 | — | — | 1 | 5.47 |
| CHEMBL1254766 | DEXTRORPHAN | 2.0 | 2 | 5.38 |
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 5.29 |
| CHEMBL494480 | ADL-5859 | 2.0 | 1 | 5.29 |
| CHEMBL248095 | SINOMENINE | 3.0 | 1 | 5.27 |
| CHEMBL5665410 | — | — | 1 | 5.26 |
| CHEMBL70 | MORPHINE | 4.0 | 2 | 5.21 |
| CHEMBL485 | CODEINE | 4.0 | 1 | 5.17 |
| CHEMBL3307199 | — | — | 1 | 5.14 |
| CHEMBL3343989 | — | — | 1 | 4.95 |
| CHEMBL5665378 | — | — | 1 | 4.95 |
| CHEMBL5665375 | — | — | 1 | 4.92 |
| CHEMBL5665367 | — | — | 1 | 4.84 |
| CHEMBL1738990 | LEVOPROPOXYPHENE | 4.0 | 1 | 4.82 |
| CHEMBL1908321 | NORCODEINE | 2.0 | 1 | 4.79 |
| CHEMBL1457 | HYDROCODONE | 4.0 | 1 | 4.73 |
| CHEMBL1270282 | — | — | 1 | 4.73 |
| CHEMBL5665368 | — | — | 1 | 4.72 |
| CHEMBL323503 | — | — | 1 | 4.72 |
| CHEMBL1330 | MORPHINE GLUCURONIDE | 2.0 | 1 | 4.72 |
| CHEMBL2028997 | — | — | 1 | 4.68 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5192321 | — | EC50 | = | 144.54 | nM | 6.84 |
| CHEMBL327745 | — | EC50 | = | 426.58 | nM | 6.37 |
| CHEMBL1644379 | COMPLANADINE A | EC50 | = | 691.83 | nM | 6.16 |
| CHEMBL4520293 | (R)-ZINC-3573 | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL1200490 | CETRORELIX | EC50 | = | 812.83 | nM | 6.09 |
| CHEMBL5665379 | — | EC50 | = | 1819.7 | nM | 5.74 |
| CHEMBL5665388 | — | EC50 | = | 3000.0 | nM | 5.52 |
| CHEMBL5665416 | — | EC50 | = | 3162.28 | nM | 5.50 |
| CHEMBL52440 | DEXTROMETHORPHAN | EC50 | = | 3235.94 | nM | 5.49 |
| CHEMBL5665374 | — | EC50 | = | 3388.44 | nM | 5.47 |
| CHEMBL1254766 | DEXTRORPHAN | EC50 | = | 4168.69 | nM | 5.38 |
| CHEMBL1254766 | DEXTRORPHAN | EC50 | = | 4300.0 | nM | 5.37 |
| CHEMBL494480 | ADL-5859 | EC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL235363 | SUBSTANCE P | EC50 | = | 5128.61 | nM | 5.29 |
| CHEMBL248095 | SINOMENINE | EC50 | = | 5370.32 | nM | 5.27 |
| CHEMBL5665410 | — | EC50 | = | 5495.41 | nM | 5.26 |
| CHEMBL70 | MORPHINE | EC50 | = | 6165.95 | nM | 5.21 |
| CHEMBL70 | MORPHINE | EC50 | = | 6400.0 | nM | 5.19 |
| CHEMBL485 | CODEINE | EC50 | = | 6760.83 | nM | 5.17 |
| CHEMBL3307199 | — | EC50 | = | 7244.36 | nM | 5.14 |
| CHEMBL5665378 | — | EC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL3343989 | — | EC50 | = | 11220.18 | nM | 4.95 |
| CHEMBL5665375 | — | EC50 | = | 12022.64 | nM | 4.92 |
| CHEMBL5665367 | — | EC50 | = | 14454.4 | nM | 4.84 |
| CHEMBL1738990 | LEVOPROPOXYPHENE | EC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL1908321 | NORCODEINE | EC50 | = | 16218.1 | nM | 4.79 |
| CHEMBL1457 | HYDROCODONE | EC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL1270282 | — | EC50 | = | 18620.87 | nM | 4.73 |
| CHEMBL1330 | MORPHINE GLUCURONIDE | EC50 | = | 19054.61 | nM | 4.72 |
| CHEMBL5665368 | — | EC50 | = | 19054.61 | nM | 4.72 |
| CHEMBL323503 | — | EC50 | = | 19054.61 | nM | 4.72 |
| CHEMBL2028997 | — | EC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL592 | LEVORPHANOL | EC50 | = | 22387.21 | nM | 4.65 |
| CHEMBL592 | LEVORPHANOL | EC50 | = | 24000.0 | nM | 4.62 |
| CHEMBL5665418 | — | EC50 | = | 27542.29 | nM | 4.56 |
| CHEMBL5665418 | — | EC50 | = | 28000.0 | nM | 4.55 |
| CHEMBL405618 | ANALOG OF DYNORPHIN A | EC50 | = | 30199.52 | nM | 4.52 |
| CHEMBL500830 | DYNORPHIN B | EC50 | = | 33113.11 | nM | 4.48 |
| CHEMBL651 | METHADONE | EC50 | = | 43651.58 | nM | 4.36 |
| CHEMBL5665426 | — | EC50 | = | 43651.58 | nM | 4.36 |
| CHEMBL5665438 | — | EC50 | = | 50118.72 | nM | 4.30 |
| CHEMBL1360 | ATRACURIUM | EC50 | > | 31622.78 | nM | - |
| CHEMBL2381583 | 22-THIOCYANATOSALVINORIN A | pEC50 | - | — | - | |
| CHEMBL445332 | SALVINORIN A | pEC50 | - | — | - | |
| CHEMBL5665380 | — | pEC50 | - | — | - | |
| CHEMBL560 | — | pEC50 | - | — | - | |
| CHEMBL80 | NALOXONE | pEC50 | - | — | - | |
| CHEMBL74019 | — | pEC50 | - | — | - | |
| CHEMBL5665430 | — | pEC50 | = | 1.84 | 10^-6No_unit | - |
| CHEMBL1685 | DEZOCINE | pEC50 | - | — | - |