Assay Detail
Functional
CHEMBL1001501
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Antagonist activity at MTL receptor in rabbit duodenum homogenate
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| 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 |
|---|---|---|---|
| Kd | 10 | 7.63 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL496190 | — | — | 1 | 8.60 |
| CHEMBL496191 | — | — | 1 | 8.40 |
| CHEMBL496391 | — | — | 1 | 7.90 |
| CHEMBL497004 | — | — | 1 | 7.80 |
| CHEMBL526496 | — | — | 1 | 7.40 |
| CHEMBL496390 | — | — | 1 | 7.30 |
| CHEMBL502792 | — | — | 1 | 7.20 |
| CHEMBL495994 | — | — | 1 | 7.20 |
| CHEMBL496389 | — | — | 1 | 6.90 |
| CHEMBL524083 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL496190 | — | Kd | = | 2.512 | nM | 8.60 |
| CHEMBL496191 | — | Kd | = | 3.981 | nM | 8.40 |
| CHEMBL496391 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL497004 | — | Kd | = | 15.85 | nM | 7.80 |
| CHEMBL526496 | — | Kd | = | 39.81 | nM | 7.40 |
| CHEMBL496390 | — | Kd | = | 50.12 | nM | 7.30 |
| CHEMBL502792 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL495994 | — | Kd | = | 63.1 | nM | 7.20 |
| CHEMBL496389 | — | Kd | = | 125.89 | nM | 6.90 |
| CHEMBL524083 | — | Kd | > | 1000.0 | nM | - |