Assay Detail
Binding
CHEMBL1001500
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Displacement of [125I]motilin from MTL receptor in rabbit duodenum homogenate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Oryctolagus cuniculus |
| Tissue | Duodenum |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel motilin antagonists: Conversion of tetrapeptide leads to orally available peptidomimetics.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 7.94 | 8.96 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL496391 | — | — | 1 | 8.96 |
| CHEMBL496191 | — | — | 1 | 8.72 |
| CHEMBL496190 | — | — | 1 | 8.37 |
| CHEMBL502792 | — | — | 1 | 8.22 |
| CHEMBL497004 | — | — | 1 | 7.92 |
| CHEMBL526496 | — | — | 1 | 7.92 |
| CHEMBL495994 | — | — | 1 | 7.62 |
| CHEMBL496390 | — | — | 1 | 7.57 |
| CHEMBL496389 | — | — | 1 | 7.34 |
| CHEMBL524083 | — | — | 1 | 6.73 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL496391 | — | IC50 | = | 1.1 | nM | 8.96 |
| CHEMBL496191 | — | IC50 | = | 1.9 | nM | 8.72 |
| CHEMBL496190 | — | IC50 | = | 4.3 | nM | 8.37 |
| CHEMBL502792 | — | IC50 | = | 6.0 | nM | 8.22 |
| CHEMBL497004 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL526496 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL495994 | — | IC50 | = | 24.0 | nM | 7.62 |
| CHEMBL496390 | — | IC50 | = | 27.0 | nM | 7.57 |
| CHEMBL496389 | — | IC50 | = | 46.0 | nM | 7.34 |
| CHEMBL524083 | — | IC50 | = | 185.0 | nM | 6.73 |