Assay Detail
Functional
CHEMBL750291
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Antagonism of NK1 receptor in rat liver microsomes.
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Rattus norvegicus |
| Tissue | Liver |
| Subcellular | Microsome |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
3-Benzyloxy-2-phenylpiperidine NK1 antagonists: the influence of alpha methyl substitution
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 8.55 | 10.05 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL100636 | — | — | 1 | 10.05 |
| CHEMBL102032 | — | — | 1 | 9.82 |
| CHEMBL101148 | — | — | 1 | 9.80 |
| CHEMBL98524 | — | — | 1 | 9.80 |
| CHEMBL99792 | — | — | 1 | 9.74 |
| CHEMBL27006 | — | — | 1 | 9.10 |
| CHEMBL102157 | — | — | 1 | 9.04 |
| CHEMBL317979 | — | — | 1 | 8.23 |
| CHEMBL418800 | — | — | 1 | 7.60 |
| CHEMBL319212 | — | — | 1 | 7.07 |
| CHEMBL103657 | — | — | 1 | 7.07 |
| CHEMBL316486 | — | — | 1 | 7.06 |
| CHEMBL100178 | — | — | 1 | 6.80 |
| CHEMBL2111607 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL100636 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL102032 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL101148 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL98524 | — | IC50 | = | 0.16 | nM | 9.80 |
| CHEMBL99792 | — | IC50 | = | 0.18 | nM | 9.74 |
| CHEMBL27006 | — | IC50 | = | 0.8 | nM | 9.10 |
| CHEMBL102157 | — | IC50 | = | 0.91 | nM | 9.04 |
| CHEMBL317979 | — | IC50 | = | 5.9 | nM | 8.23 |
| CHEMBL418800 | — | IC50 | = | 25.0 | nM | 7.60 |
| CHEMBL319212 | — | IC50 | = | 85.0 | nM | 7.07 |
| CHEMBL103657 | — | IC50 | = | 86.0 | nM | 7.07 |
| CHEMBL316486 | — | IC50 | = | 87.0 | nM | 7.06 |
| CHEMBL100178 | — | IC50 | = | 160.0 | nM | 6.80 |
| CHEMBL2111607 | — | IC50 | > | 10000.0 | nM | - |