Assay Detail
Binding
CHEMBL829162
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Inhibition of human Neurokinin 2 receptor
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Publication
Structure-activity relationships of 1-alkyl-5-(3,4-dichlorophenyl)-5-{2-[3-(substituted)-1-azetidinyl]-ethyl}-2-piperidones. Part 2: Improving oral absorption.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 15 | 8.39 | 9.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL182600 | — | — | 1 | 9.40 |
| CHEMBL185572 | — | — | 1 | 9.10 |
| CHEMBL434142 | — | — | 1 | 9.00 |
| CHEMBL434548 | — | — | 1 | 8.90 |
| CHEMBL185182 | — | — | 1 | 8.90 |
| CHEMBL185133 | — | — | 1 | 8.60 |
| CHEMBL367815 | — | — | 1 | 8.50 |
| CHEMBL365613 | — | — | 1 | 8.40 |
| CHEMBL367348 | — | — | 1 | 8.20 |
| CHEMBL185452 | — | — | 1 | 8.10 |
| CHEMBL359655 | — | — | 1 | 8.10 |
| CHEMBL359903 | — | — | 1 | 8.00 |
| CHEMBL185007 | — | — | 1 | 7.80 |
| CHEMBL180049 | — | — | 1 | 7.80 |
| CHEMBL360721 | — | — | 1 | 7.10 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL182600 | — | IC50 | = | 0.3981 | nM | 9.40 |
| CHEMBL185572 | — | IC50 | = | 0.7943 | nM | 9.10 |
| CHEMBL434142 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL434548 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL185182 | — | IC50 | = | 1.259 | nM | 8.90 |
| CHEMBL185133 | — | IC50 | = | 2.512 | nM | 8.60 |
| CHEMBL367815 | — | IC50 | = | 3.162 | nM | 8.50 |
| CHEMBL365613 | — | IC50 | = | 3.981 | nM | 8.40 |
| CHEMBL367348 | — | IC50 | = | 6.31 | nM | 8.20 |
| CHEMBL185452 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL359655 | — | IC50 | = | 7.943 | nM | 8.10 |
| CHEMBL359903 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL185007 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL180049 | — | IC50 | = | 15.85 | nM | 7.80 |
| CHEMBL360721 | — | IC50 | = | 79.43 | nM | 7.10 |