Assay Detail
Binding
CHEMBL1000259
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Displacement of [125I]substance P human recombinant NK1 receptor expressed in CHO cells in absence of human serum albumin
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | CHO |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Potent, brain-penetrant, hydroisoindoline-based human neurokinin-1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 8 | 9.85 | 10.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL447955 | SERLOPITANT | 3.0 | 1 | 10.22 |
| CHEMBL490869 | — | — | 1 | 10.05 |
| CHEMBL445686 | — | — | 1 | 10.00 |
| CHEMBL484134 | — | — | 1 | 9.96 |
| CHEMBL499004 | — | — | 1 | 9.89 |
| CHEMBL473680 | — | — | 1 | 9.82 |
| CHEMBL484133 | — | — | 1 | 9.59 |
| CHEMBL445239 | — | — | 1 | 9.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL447955 | SERLOPITANT | IC50 | = | 0.06 | nM | 10.22 |
| CHEMBL490869 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL445686 | — | IC50 | = | 0.1 | nM | 10.00 |
| CHEMBL484134 | — | IC50 | = | 0.11 | nM | 9.96 |
| CHEMBL499004 | — | IC50 | = | 0.13 | nM | 9.89 |
| CHEMBL473680 | — | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL484133 | — | IC50 | = | 0.255 | nM | 9.59 |
| CHEMBL445239 | — | IC50 | = | 0.525 | nM | 9.28 |