Assay Detail
Functional
CHEMBL1008005
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Agonist activity at human recombinant motilin receptor expressed in CHO cells assessed as increase in intracellular calcium by FLIPR assay
13
Total Activities
13
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 | Autocuration |
Publication
Discovery of N-(3-fluorophenyl)-1-[(4-([(3S)-3-methyl-1-piperazinyl]methyl)phenyl)acetyl]-4-piperidinamine (GSK962040), the first small molecule motilin receptor agonist clinical candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| EC50 | 13 | 7.89 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL525634 | — | — | 1 | 10.40 |
| CHEMBL473921 | — | — | 1 | 8.40 |
| CHEMBL489480 | — | — | 1 | 8.40 |
| CHEMBL489094 | — | — | 1 | 8.00 |
| CHEMBL489095 | CAMICINAL | 3.0 | 1 | 7.90 |
| CHEMBL523933 | — | — | 1 | 7.70 |
| CHEMBL474130 | — | — | 1 | 7.60 |
| CHEMBL489297 | — | — | 1 | 7.50 |
| CHEMBL489479 | — | — | 1 | 7.50 |
| CHEMBL474934 | — | — | 1 | 7.40 |
| CHEMBL514475 | — | — | 1 | 7.30 |
| CHEMBL532 | ERYTHROMYCIN | 4.0 | 1 | 7.30 |
| CHEMBL474129 | — | — | 1 | 7.20 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL525634 | — | EC50 | = | 0.03981 | nM | 10.40 |
| CHEMBL473921 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL489480 | — | EC50 | = | 3.981 | nM | 8.40 |
| CHEMBL489094 | — | EC50 | = | 10.0 | nM | 8.00 |
| CHEMBL489095 | CAMICINAL | EC50 | = | 12.59 | nM | 7.90 |
| CHEMBL523933 | — | EC50 | = | 19.95 | nM | 7.70 |
| CHEMBL474130 | — | EC50 | = | 25.12 | nM | 7.60 |
| CHEMBL489297 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL489479 | — | EC50 | = | 31.62 | nM | 7.50 |
| CHEMBL474934 | — | EC50 | = | 39.81 | nM | 7.40 |
| CHEMBL514475 | — | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL532 | ERYTHROMYCIN | EC50 | = | 50.12 | nM | 7.30 |
| CHEMBL474129 | — | EC50 | = | 63.1 | nM | 7.20 |