Assay Detail
Binding
CHEMBL747298
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity towards Neurokinin -1(NK-1) receptor of human by using [125I]- Tyr8 substance P as a radioligand in CHO cells
16
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | CHO |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
1,2,3-Trisubstituted cyclohexyl substance P antagonists: significance of the ring nitrogen in piperidine-based NK-1 receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.08 | 9.30 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL441225 | CP-99994 | — | 1 | 9.30 |
| CHEMBL28055 | — | — | 1 | 9.07 |
| CHEMBL27003 | — | — | 1 | 9.00 |
| CHEMBL27006 | — | — | 1 | 9.00 |
| CHEMBL283872 | — | — | 2 | 8.82 |
| CHEMBL26086 | — | — | 1 | 8.43 |
| CHEMBL281717 | — | — | 1 | 8.17 |
| CHEMBL26251 | — | — | 1 | 8.15 |
| CHEMBL281940 | — | — | 1 | 7.97 |
| CHEMBL432279 | — | — | 1 | 7.85 |
| CHEMBL28003 | — | — | 1 | 7.77 |
| CHEMBL286747 | — | — | 1 | 7.47 |
| CHEMBL26193 | — | — | 1 | 6.05 |
| CHEMBL27026 | — | — | 1 | 5.58 |
| CHEMBL26593 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL441225 | CP-99994 | IC50 | = | 0.5 | nM | 9.30 |
| CHEMBL28055 | — | IC50 | = | 0.85 | nM | 9.07 |
| CHEMBL27003 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL27006 | — | IC50 | = | 1.0 | nM | 9.00 |
| CHEMBL283872 | — | IC50 | = | 1.5 | nM | 8.82 |
| CHEMBL283872 | — | IC50 | = | 3.0 | nM | 8.52 |
| CHEMBL26086 | — | IC50 | = | 3.7 | nM | 8.43 |
| CHEMBL281717 | — | IC50 | = | 6.7 | nM | 8.17 |
| CHEMBL26251 | — | IC50 | = | 7.0 | nM | 8.15 |
| CHEMBL281940 | — | IC50 | = | 10.7 | nM | 7.97 |
| CHEMBL432279 | — | IC50 | = | 14.0 | nM | 7.85 |
| CHEMBL28003 | — | IC50 | = | 17.0 | nM | 7.77 |
| CHEMBL286747 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL26193 | — | IC50 | = | 881.0 | nM | 6.05 |
| CHEMBL27026 | — | IC50 | = | 2632.0 | nM | 5.58 |
| CHEMBL26593 | — | IC50 | >= | 157.0 | nM | - |