Assay Detail
Functional
CHEMBL1055017
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Agonist activity at mu opioid receptor in Hartley guinea pig longitudinal muscle myenteric plexus assessed as inhibition of electrically evoked contraction
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Cavia porcellus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
Influence of the side chain next to C-terminal benzimidazole in opioid pseudopeptides containing the Dmt-Tic pharmacophore.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 18 | 7.31 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL553221 | — | — | 1 | 8.85 |
| CHEMBL563304 | — | — | 1 | 8.16 |
| CHEMBL557346 | — | — | 1 | 8.11 |
| CHEMBL538699 | — | — | 1 | 8.07 |
| CHEMBL554838 | — | — | 1 | 7.99 |
| CHEMBL539386 | — | — | 1 | 7.63 |
| CHEMBL556230 | — | — | 1 | 7.57 |
| CHEMBL553461 | — | — | 1 | 7.46 |
| CHEMBL538384 | — | — | 1 | 7.45 |
| CHEMBL538456 | — | — | 1 | 7.40 |
| CHEMBL538457 | — | — | 1 | 7.27 |
| CHEMBL551937 | — | — | 1 | 7.14 |
| CHEMBL564083 | — | — | 1 | 6.97 |
| CHEMBL556063 | — | — | 1 | 6.56 |
| CHEMBL559088 | — | — | 1 | 6.43 |
| CHEMBL554625 | — | — | 1 | 6.40 |
| CHEMBL540724 | — | — | 1 | 6.31 |
| CHEMBL540972 | — | — | 1 | 5.76 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL553221 | — | IC50 | = | 1.41 | nM | 8.85 |
| CHEMBL563304 | — | IC50 | = | 6.9 | nM | 8.16 |
| CHEMBL557346 | — | IC50 | = | 7.84 | nM | 8.11 |
| CHEMBL538699 | — | IC50 | = | 8.5 | nM | 8.07 |
| CHEMBL554838 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL539386 | — | IC50 | = | 23.4 | nM | 7.63 |
| CHEMBL556230 | — | IC50 | = | 26.92 | nM | 7.57 |
| CHEMBL553461 | — | IC50 | = | 34.9 | nM | 7.46 |
| CHEMBL538384 | — | IC50 | = | 35.4 | nM | 7.45 |
| CHEMBL538456 | — | IC50 | = | 39.7 | nM | 7.40 |
| CHEMBL538457 | — | IC50 | = | 53.9 | nM | 7.27 |
| CHEMBL551937 | — | IC50 | = | 71.7 | nM | 7.14 |
| CHEMBL564083 | — | IC50 | = | 106.0 | nM | 6.97 |
| CHEMBL556063 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL559088 | — | IC50 | = | 375.0 | nM | 6.43 |
| CHEMBL554625 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL540724 | — | IC50 | = | 494.0 | nM | 6.31 |
| CHEMBL540972 | — | IC50 | = | 1724.0 | nM | 5.76 |