Assay Detail
Functional
CHEMBL5665199
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at N-terminal Flag-tagged human MRGPRX2 receptor expressed in tetracycline-induced FLP-IN/T-REX 293 cells assessed as increase in intracellular calcium release by FLIPR assay
107
Total Activities
95
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | Flp-In-T-REx-293 |
| 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 | 57 | 5.30 | 6.86 |
| pEC50 | 50 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5665416 | — | — | 1 | 6.86 |
| CHEMBL327745 | — | — | 2 | 6.54 |
| CHEMBL5665419 | — | — | 1 | 6.42 |
| CHEMBL5192321 | — | — | 1 | 6.38 |
| CHEMBL1200490 | CETRORELIX | 4.0 | 1 | 6.21 |
| CHEMBL5665379 | — | — | 2 | 6.19 |
| CHEMBL4520293 | (R)-ZINC-3573 | — | 1 | 6.00 |
| CHEMBL405618 | ANALOG OF DYNORPHIN A | — | 2 | 5.98 |
| CHEMBL235363 | SUBSTANCE P | 1.0 | 1 | 5.97 |
| CHEMBL5665430 | — | — | 1 | 5.79 |
| CHEMBL2028997 | — | — | 2 | 5.64 |
| CHEMBL1254766 | DEXTRORPHAN | 2.0 | 2 | 5.41 |
| CHEMBL248095 | SINOMENINE | 3.0 | 1 | 5.40 |
| CHEMBL5665408 | — | — | 1 | 5.37 |
| CHEMBL5665374 | — | — | 1 | 5.30 |
| CHEMBL52440 | DEXTROMETHORPHAN | 4.0 | 1 | 5.23 |
| CHEMBL500830 | DYNORPHIN B | — | 2 | 5.19 |
| CHEMBL70 | MORPHINE | 4.0 | 2 | 5.18 |
| CHEMBL3343989 | — | — | 1 | 5.05 |
| CHEMBL3307199 | — | — | 1 | 5.03 |
| CHEMBL485 | CODEINE | 4.0 | 1 | 5.00 |
| CHEMBL407832 | — | — | 2 | 4.97 |
| CHEMBL1457 | HYDROCODONE | 4.0 | 1 | 4.96 |
| CHEMBL5665421 | — | — | 2 | 4.94 |
| CHEMBL2370408 | — | — | 1 | 4.93 |
| CHEMBL592 | LEVORPHANOL | 4.0 | 2 | 4.90 |
| CHEMBL5665367 | — | — | 1 | 4.87 |
| CHEMBL5665410 | — | — | 1 | 4.86 |
| CHEMBL323503 | — | — | 1 | 4.82 |
| CHEMBL1644379 | COMPLANADINE A | — | 2 | 4.75 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5665416 | — | EC50 | = | 138.04 | nM | 6.86 |
| CHEMBL327745 | — | EC50 | = | 290.0 | nM | 6.54 |
| CHEMBL327745 | — | EC50 | = | 288.4 | nM | 6.54 |
| CHEMBL5665419 | — | EC50 | = | 380.0 | nM | 6.42 |
| CHEMBL5192321 | — | EC50 | = | 416.87 | nM | 6.38 |
| CHEMBL1200490 | CETRORELIX | EC50 | = | 616.6 | nM | 6.21 |
| CHEMBL5665379 | — | EC50 | = | 645.65 | nM | 6.19 |
| CHEMBL5665379 | — | EC50 | = | 740.0 | nM | 6.13 |
| CHEMBL4520293 | (R)-ZINC-3573 | EC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL405618 | ANALOG OF DYNORPHIN A | EC50 | = | 1047.13 | nM | 5.98 |
| CHEMBL235363 | SUBSTANCE P | EC50 | = | 1071.52 | nM | 5.97 |
| CHEMBL405618 | ANALOG OF DYNORPHIN A | EC50 | = | 1100.0 | nM | 5.96 |
| CHEMBL5665430 | — | EC50 | = | 1621.81 | nM | 5.79 |
| CHEMBL2028997 | — | EC50 | = | 2290.87 | nM | 5.64 |
| CHEMBL2028997 | — | EC50 | = | 2450.0 | nM | 5.61 |
| CHEMBL1254766 | DEXTRORPHAN | EC50 | = | 3890.45 | nM | 5.41 |
| CHEMBL248095 | SINOMENINE | EC50 | = | 3981.07 | nM | 5.40 |
| CHEMBL5665408 | — | EC50 | = | 4265.8 | nM | 5.37 |
| CHEMBL5665374 | — | EC50 | = | 5011.87 | nM | 5.30 |
| CHEMBL52440 | DEXTROMETHORPHAN | EC50 | = | 5888.44 | nM | 5.23 |
| CHEMBL1254766 | DEXTRORPHAN | EC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL500830 | DYNORPHIN B | EC50 | = | 6456.54 | nM | 5.19 |
| CHEMBL70 | MORPHINE | EC50 | = | 6606.93 | nM | 5.18 |
| CHEMBL70 | MORPHINE | EC50 | = | 7000.0 | nM | 5.16 |
| CHEMBL500830 | DYNORPHIN B | EC50 | = | 8340.0 | nM | 5.08 |
| CHEMBL3343989 | — | EC50 | = | 8912.51 | nM | 5.05 |
| CHEMBL3307199 | — | EC50 | = | 9332.54 | nM | 5.03 |
| CHEMBL485 | CODEINE | EC50 | = | 10000.0 | nM | 5.00 |
| CHEMBL407832 | — | EC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL1457 | HYDROCODONE | EC50 | = | 10964.78 | nM | 4.96 |
| CHEMBL5665421 | — | EC50 | = | 11500.0 | nM | 4.94 |
| CHEMBL5665421 | — | EC50 | = | 11481.54 | nM | 4.94 |
| CHEMBL2370408 | — | EC50 | = | 11748.98 | nM | 4.93 |
| CHEMBL592 | LEVORPHANOL | EC50 | = | 12589.25 | nM | 4.90 |
| CHEMBL5665367 | — | EC50 | = | 13489.63 | nM | 4.87 |
| CHEMBL5665410 | — | EC50 | = | 13803.84 | nM | 4.86 |
| CHEMBL592 | LEVORPHANOL | EC50 | = | 14000.0 | nM | 4.85 |
| CHEMBL323503 | — | EC50 | = | 15135.61 | nM | 4.82 |
| CHEMBL407832 | — | EC50 | = | 15488.17 | nM | 4.81 |
| CHEMBL1644379 | COMPLANADINE A | EC50 | = | 18000.0 | nM | 4.75 |
| CHEMBL1644379 | COMPLANADINE A | EC50 | = | 17782.79 | nM | 4.75 |
| CHEMBL5665375 | — | EC50 | = | 20892.96 | nM | 4.68 |
| CHEMBL5665368 | — | EC50 | = | 25118.86 | nM | 4.60 |
| CHEMBL2028850 | ICATIBANT | EC50 | = | 28183.83 | nM | 4.55 |
| CHEMBL1738990 | LEVOPROPOXYPHENE | EC50 | = | 31622.78 | nM | 4.50 |
| CHEMBL5665437 | — | EC50 | = | 39600.0 | nM | 4.40 |
| CHEMBL217379 | — | EC50 | = | 58000.0 | nM | 4.24 |
| CHEMBL5665378 | — | EC50 | = | 70794.58 | nM | 4.15 |
| CHEMBL1201244 | ROCURONIUM | EC50 | > | 31622.78 | nM | - |
| CHEMBL100116 | PENTAZOCINE | pEC50 | - | — | - |