Assay Detail
Binding
CHEMBL2447076
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Antagonist activity at NK1 receptor (unknown origin)
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 10 | 9.60 | 10.40 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL555572 | — | — | 1 | 10.40 |
| CHEMBL1471 | APREPITANT | 4.0 | 1 | 10.05 |
| CHEMBL425956 | — | — | 1 | 10.05 |
| CHEMBL2441368 | — | — | 1 | 9.77 |
| CHEMBL22194 | L-709210 | — | 1 | 9.70 |
| CHEMBL522987 | VESTIPITANT | 2.0 | 1 | 9.60 |
| CHEMBL2441369 | — | — | 1 | 9.21 |
| CHEMBL16192 | CP-96345 | — | 1 | 9.18 |
| CHEMBL206253 | NETUPITANT | 4.0 | 1 | 9.02 |
| CHEMBL27006 | — | — | 1 | 9.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL555572 | — | IC50 | = | 0.04 | nM | 10.40 |
| CHEMBL1471 | APREPITANT | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL425956 | — | IC50 | = | 0.09 | nM | 10.05 |
| CHEMBL2441368 | — | IC50 | = | 0.17 | nM | 9.77 |
| CHEMBL22194 | L-709210 | IC50 | = | 0.2 | nM | 9.70 |
| CHEMBL522987 | VESTIPITANT | IC50 | = | 0.25 | nM | 9.60 |
| CHEMBL2441369 | — | IC50 | = | 0.61 | nM | 9.21 |
| CHEMBL16192 | CP-96345 | IC50 | = | 0.66 | nM | 9.18 |
| CHEMBL206253 | NETUPITANT | IC50 | = | 0.95 | nM | 9.02 |
| CHEMBL27006 | — | IC50 | = | 1.0 | nM | 9.00 |