Assay Detail
Functional
CHEMBL890161
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Agonist activity at GPR54 expressed in CHO cells assessed as intracellular calcium mobilization
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
SAR and QSAR studies on the N-terminally acylated pentapeptide agonists for GPR54.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 30 | 8.72 | 9.16 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL388586 | — | — | 1 | 9.16 |
| CHEMBL268579 | — | — | 1 | 9.10 |
| CHEMBL388146 | — | — | 1 | 9.00 |
| CHEMBL226757 | — | — | 1 | 9.00 |
| CHEMBL440431 | — | — | 1 | 9.00 |
| CHEMBL223390 | — | — | 1 | 8.92 |
| CHEMBL226566 | — | — | 1 | 8.92 |
| CHEMBL388585 | — | — | 1 | 8.89 |
| CHEMBL229621 | — | — | 1 | 8.85 |
| CHEMBL226633 | — | — | 1 | 8.80 |
| CHEMBL268660 | — | — | 1 | 8.77 |
| CHEMBL227165 | — | — | 1 | 8.77 |
| CHEMBL268659 | — | — | 1 | 8.77 |
| CHEMBL226635 | — | — | 1 | 8.70 |
| CHEMBL389708 | — | — | 1 | 8.68 |
| CHEMBL229656 | — | — | 1 | 8.57 |
| CHEMBL389493 | — | — | 1 | 8.52 |
| CHEMBL387875 | — | — | 1 | 8.52 |
| CHEMBL415004 | — | — | 1 | 8.52 |
| CHEMBL226634 | — | — | 1 | 8.51 |
| CHEMBL374398 | — | — | 1 | 8.51 |
| CHEMBL387648 | — | — | 1 | 8.48 |
| CHEMBL229655 | — | — | 1 | 8.48 |
| CHEMBL387923 | — | — | 1 | 8.33 |
| CHEMBL268661 | — | — | 1 | 8.30 |
| CHEMBL274960 | — | — | 1 | - |
| CHEMBL389262 | — | — | 1 | - |
| CHEMBL226537 | — | — | 1 | - |
| CHEMBL229103 | — | — | 1 | - |
| CHEMBL415221 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL388586 | — | EC50 | = | 0.69 | nM | 9.16 |
| CHEMBL268579 | — | EC50 | = | 0.8 | nM | 9.10 |
| CHEMBL388146 | — | EC50 | = | 1.0 | nM | 9.00 |
| CHEMBL226757 | — | EC50 | = | 0.99 | nM | 9.00 |
| CHEMBL440431 | — | EC50 | = | 0.99 | nM | 9.00 |
| CHEMBL223390 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL226566 | — | EC50 | = | 1.2 | nM | 8.92 |
| CHEMBL388585 | — | EC50 | = | 1.3 | nM | 8.89 |
| CHEMBL229621 | — | EC50 | = | 1.4 | nM | 8.85 |
| CHEMBL226633 | — | EC50 | = | 1.6 | nM | 8.80 |
| CHEMBL268660 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL227165 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL268659 | — | EC50 | = | 1.7 | nM | 8.77 |
| CHEMBL226635 | — | EC50 | = | 2.0 | nM | 8.70 |
| CHEMBL389708 | — | EC50 | = | 2.1 | nM | 8.68 |
| CHEMBL229656 | — | EC50 | = | 2.7 | nM | 8.57 |
| CHEMBL389493 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL387875 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL415004 | — | EC50 | = | 3.0 | nM | 8.52 |
| CHEMBL226634 | — | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL374398 | — | EC50 | = | 3.1 | nM | 8.51 |
| CHEMBL387648 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL229655 | — | EC50 | = | 3.3 | nM | 8.48 |
| CHEMBL387923 | — | EC50 | = | 4.7 | nM | 8.33 |
| CHEMBL268661 | — | EC50 | = | 5.0 | nM | 8.30 |
| CHEMBL274960 | — | EC50 | - | — | - | |
| CHEMBL389262 | — | EC50 | - | — | - | |
| CHEMBL226537 | — | EC50 | > | 100.0 | nM | - |
| CHEMBL229103 | — | EC50 | - | — | - | |
| CHEMBL415221 | — | EC50 | > | 100.0 | nM | - |