Assay Detail
Binding
CHEMBL807903
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Binding affinity at human Tachykinin receptor 1 expressed in CHO cells by [125 I]Trp8-substance P displacement.
22
Total Activities
21
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
Tryptophan-derived NK1 antagonists: conformationally constrained heterocyclic bioisosteres of the ester linkage.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 22 | 6.59 | 8.60 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL22870 | L-732138 | — | 1 | 8.60 |
| CHEMBL173014 | — | — | 1 | 7.96 |
| CHEMBL367711 | — | — | 2 | 7.66 |
| CHEMBL173013 | — | — | 1 | 7.51 |
| CHEMBL425848 | — | — | 1 | 7.20 |
| CHEMBL173120 | — | — | 1 | 6.82 |
| CHEMBL369692 | — | — | 1 | 6.69 |
| CHEMBL355643 | — | — | 1 | 6.66 |
| CHEMBL176471 | — | — | 1 | 6.61 |
| CHEMBL172238 | — | — | 1 | 6.57 |
| CHEMBL176919 | — | — | 1 | 6.56 |
| CHEMBL427295 | — | — | 1 | 6.51 |
| CHEMBL369580 | — | — | 1 | 6.50 |
| CHEMBL368804 | — | — | 1 | 6.40 |
| CHEMBL176772 | — | — | 1 | 6.25 |
| CHEMBL174464 | — | — | 1 | 6.17 |
| CHEMBL367423 | — | — | 1 | 5.57 |
| CHEMBL444552 | — | — | 1 | 5.37 |
| CHEMBL172308 | — | — | 1 | 5.36 |
| CHEMBL174465 | — | — | 1 | 5.22 |
| CHEMBL366753 | — | — | 1 | 5.13 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL22870 | L-732138 | IC50 | = | 2.5 | nM | 8.60 |
| CHEMBL173014 | — | IC50 | = | 11.0 | nM | 7.96 |
| CHEMBL367711 | — | IC50 | = | 22.0 | nM | 7.66 |
| CHEMBL367711 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL173013 | — | IC50 | = | 31.0 | nM | 7.51 |
| CHEMBL425848 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL173120 | — | IC50 | = | 153.0 | nM | 6.82 |
| CHEMBL369692 | — | IC50 | = | 203.0 | nM | 6.69 |
| CHEMBL355643 | — | IC50 | = | 220.0 | nM | 6.66 |
| CHEMBL176471 | — | IC50 | = | 243.0 | nM | 6.61 |
| CHEMBL172238 | — | IC50 | = | 267.0 | nM | 6.57 |
| CHEMBL176919 | — | IC50 | = | 273.0 | nM | 6.56 |
| CHEMBL427295 | — | IC50 | = | 310.0 | nM | 6.51 |
| CHEMBL369580 | — | IC50 | = | 317.0 | nM | 6.50 |
| CHEMBL368804 | — | IC50 | = | 400.0 | nM | 6.40 |
| CHEMBL176772 | — | IC50 | = | 567.0 | nM | 6.25 |
| CHEMBL174464 | — | IC50 | = | 683.0 | nM | 6.17 |
| CHEMBL367423 | — | IC50 | = | 2666.0 | nM | 5.57 |
| CHEMBL444552 | — | IC50 | = | 4275.0 | nM | 5.37 |
| CHEMBL172308 | — | IC50 | = | 4333.0 | nM | 5.36 |
| CHEMBL174465 | — | IC50 | = | 6000.0 | nM | 5.22 |
| CHEMBL366753 | — | IC50 | = | 7366.0 | nM | 5.13 |