Assay Detail
Binding
CHEMBL745024
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Binding affinity for NK2 receptor in HSKR-1 cells was determined by using [125 I ]-Iodohistidyl NKA.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Cell Type | HSKR-1 |
| Confidence | 8 — Homologous single protein target |
| Curated By | Expert |
Publication
Synthesis and structure-activity relationships for a series of substituted pyrrolidine NK1/NK2 receptor antagonists
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 21 | 7.75 | 8.69 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL540553 | — | — | 1 | 8.69 |
| CHEMBL553617 | — | — | 1 | 8.66 |
| CHEMBL315814 | — | — | 1 | 8.50 |
| CHEMBL313931 | — | — | 1 | 8.44 |
| CHEMBL553451 | — | — | 1 | 8.35 |
| CHEMBL554092 | — | — | 1 | 8.11 |
| CHEMBL539021 | — | — | 1 | 8.08 |
| CHEMBL84055 | — | — | 1 | 8.03 |
| CHEMBL553554 | — | — | 1 | 7.99 |
| CHEMBL432183 | — | — | 1 | 7.93 |
| CHEMBL313546 | — | — | 1 | 7.92 |
| CHEMBL314119 | — | — | 1 | 7.79 |
| CHEMBL315923 | — | — | 1 | 7.79 |
| CHEMBL315982 | — | — | 1 | 7.77 |
| CHEMBL82386 | — | — | 1 | 7.68 |
| CHEMBL312173 | — | — | 1 | 7.24 |
| CHEMBL310173 | — | — | 1 | 7.13 |
| CHEMBL83585 | — | — | 1 | 6.72 |
| CHEMBL315322 | — | — | 1 | 6.63 |
| CHEMBL85499 | — | — | 1 | 5.56 |
| CHEMBL83885 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL540553 | — | IC50 | = | 2.05 | nM | 8.69 |
| CHEMBL553617 | — | IC50 | = | 2.19 | nM | 8.66 |
| CHEMBL315814 | — | IC50 | = | 3.13 | nM | 8.50 |
| CHEMBL313931 | — | IC50 | = | 3.64 | nM | 8.44 |
| CHEMBL553451 | — | IC50 | = | 4.51 | nM | 8.35 |
| CHEMBL554092 | — | IC50 | = | 7.77 | nM | 8.11 |
| CHEMBL539021 | — | IC50 | = | 8.4 | nM | 8.08 |
| CHEMBL84055 | — | IC50 | = | 9.39 | nM | 8.03 |
| CHEMBL553554 | — | IC50 | = | 10.2 | nM | 7.99 |
| CHEMBL432183 | — | IC50 | = | 11.8 | nM | 7.93 |
| CHEMBL313546 | — | IC50 | = | 12.0 | nM | 7.92 |
| CHEMBL314119 | — | IC50 | = | 16.2 | nM | 7.79 |
| CHEMBL315923 | — | IC50 | = | 16.4 | nM | 7.79 |
| CHEMBL315982 | — | IC50 | = | 17.1 | nM | 7.77 |
| CHEMBL82386 | — | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL312173 | — | IC50 | = | 57.9 | nM | 7.24 |
| CHEMBL310173 | — | IC50 | = | 74.5 | nM | 7.13 |
| CHEMBL83585 | — | IC50 | = | 190.0 | nM | 6.72 |
| CHEMBL315322 | — | IC50 | = | 235.0 | nM | 6.63 |
| CHEMBL85499 | — | IC50 | = | 2770.0 | nM | 5.56 |
| CHEMBL83885 | — | IC50 | > | 10000.0 | nM | - |