Assay Detail
Binding
CHEMBL1925646
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of [125I-His9]-ghrelin from human GRLN receptor by radioligand binding assay
53
Total Activities
52
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Target
Growth hormone secretagogue receptor type 1 (CHEMBL4616) ↗| Type | SINGLE PROTEIN |
| Organism | Homo sapiens |
Publication
Optimization of the potency and pharmacokinetic properties of a macrocyclic ghrelin receptor agonist (Part I): Development of ulimorelin (TZP-101) from hit to clinic.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 53 | 7.40 | 9.46 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1923617 | — | — | 1 | 9.46 |
| CHEMBL1923629 | — | — | 1 | 9.42 |
| CHEMBL1923640 | — | — | 1 | 9.05 |
| CHEMBL1923642 | — | — | 1 | 8.59 |
| CHEMBL1923610 | — | — | 1 | 8.36 |
| CHEMBL1923628 | — | — | 2 | 8.32 |
| CHEMBL1923627 | — | — | 1 | 8.30 |
| CHEMBL1923623 | — | — | 1 | 8.21 |
| CHEMBL1923609 | — | — | 1 | 8.19 |
| CHEMBL1923626 | — | — | 1 | 8.15 |
| CHEMBL1923625 | — | — | 1 | 8.14 |
| CHEMBL1923637 | — | — | 1 | 8.05 |
| CHEMBL1923639 | — | — | 1 | 7.92 |
| CHEMBL1923621 | — | — | 1 | 7.82 |
| CHEMBL1923611 | — | — | 1 | 7.80 |
| CHEMBL1923502 | ULIMORELIN HYDROCHLORIDE | 3.0 | 1 | 7.80 |
| CHEMBL1923641 | — | — | 1 | 7.72 |
| CHEMBL1923624 | — | — | 1 | 7.68 |
| CHEMBL1923608 | — | — | 1 | 7.60 |
| CHEMBL1923620 | — | — | 1 | 7.50 |
| CHEMBL1923622 | — | — | 1 | 7.47 |
| CHEMBL1923618 | — | — | 1 | 7.47 |
| CHEMBL1923614 | — | — | 1 | 7.46 |
| CHEMBL1923616 | — | — | 1 | 7.37 |
| CHEMBL1923638 | — | — | 1 | 7.25 |
| CHEMBL1923643 | — | — | 1 | 7.24 |
| CHEMBL1923644 | — | — | 1 | 7.21 |
| CHEMBL1923504 | — | — | 1 | 7.17 |
| CHEMBL1923636 | — | — | 1 | 7.11 |
| CHEMBL1923635 | — | — | 1 | 7.09 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1923617 | — | Ki | = | 0.35 | nM | 9.46 |
| CHEMBL1923629 | — | Ki | = | 0.38 | nM | 9.42 |
| CHEMBL1923640 | — | Ki | = | 0.9 | nM | 9.05 |
| CHEMBL1923642 | — | Ki | = | 2.6 | nM | 8.59 |
| CHEMBL1923610 | — | Ki | = | 4.4 | nM | 8.36 |
| CHEMBL1923628 | — | Ki | = | 4.8 | nM | 8.32 |
| CHEMBL1923627 | — | Ki | = | 5.0 | nM | 8.30 |
| CHEMBL1923623 | — | Ki | = | 6.2 | nM | 8.21 |
| CHEMBL1923609 | — | Ki | = | 6.4 | nM | 8.19 |
| CHEMBL1923626 | — | Ki | = | 7.0 | nM | 8.15 |
| CHEMBL1923625 | — | Ki | = | 7.3 | nM | 8.14 |
| CHEMBL1923637 | — | Ki | = | 9.0 | nM | 8.05 |
| CHEMBL1923639 | — | Ki | = | 12.0 | nM | 7.92 |
| CHEMBL1923621 | — | Ki | = | 15.0 | nM | 7.82 |
| CHEMBL1923502 | ULIMORELIN HYDROCHLORIDE | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1923611 | — | Ki | = | 16.0 | nM | 7.80 |
| CHEMBL1923641 | — | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL1923624 | — | Ki | = | 21.0 | nM | 7.68 |
| CHEMBL1923608 | — | Ki | = | 25.0 | nM | 7.60 |
| CHEMBL1923620 | — | Ki | = | 32.0 | nM | 7.50 |
| CHEMBL1923622 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL1923618 | — | Ki | = | 34.0 | nM | 7.47 |
| CHEMBL1923614 | — | Ki | = | 35.0 | nM | 7.46 |
| CHEMBL1923616 | — | Ki | = | 43.0 | nM | 7.37 |
| CHEMBL1923638 | — | Ki | = | 56.0 | nM | 7.25 |
| CHEMBL1923643 | — | Ki | = | 58.0 | nM | 7.24 |
| CHEMBL1923644 | — | Ki | = | 61.0 | nM | 7.21 |
| CHEMBL1923504 | — | Ki | = | 68.0 | nM | 7.17 |
| CHEMBL1923628 | — | Ki | = | 75.0 | nM | 7.12 |
| CHEMBL1923636 | — | Ki | = | 78.0 | nM | 7.11 |
| CHEMBL1923635 | — | Ki | = | 81.0 | nM | 7.09 |
| CHEMBL1923501 | — | Ki | = | 86.0 | nM | 7.07 |
| CHEMBL1923619 | — | Ki | = | 104.0 | nM | 6.98 |
| CHEMBL1923512 | — | Ki | = | 120.0 | nM | 6.92 |
| CHEMBL1923632 | — | Ki | = | 160.0 | nM | 6.80 |
| CHEMBL1923634 | — | Ki | = | 210.0 | nM | 6.68 |
| CHEMBL1923615 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL1923506 | — | Ki | = | 380.0 | nM | 6.42 |
| CHEMBL1923511 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL1923633 | — | Ki | = | 400.0 | nM | 6.40 |
| CHEMBL1923613 | — | Ki | = | 500.0 | nM | 6.30 |
| CHEMBL1923612 | — | Ki | = | 580.0 | nM | 6.24 |
| CHEMBL1923510 | — | Ki | = | 670.0 | nM | 6.17 |
| CHEMBL1923508 | — | Ki | = | 1100.0 | nM | 5.96 |
| CHEMBL1923505 | — | Ki | = | 1200.0 | nM | 5.92 |
| CHEMBL1923631 | — | Ki | = | 1500.0 | nM | 5.82 |
| CHEMBL1923514 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1923607 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1923509 | — | Ki | > | 10000.0 | nM | - |
| CHEMBL1923507 | — | Ki | > | 10000.0 | nM | - |