Assay Detail
Binding
CHEMBL750068
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Displacement of [125I][MePhe]-NKB from human NK3 receptor expressed in CHO cells
14
Total Activities
14
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 | Expert |
Publication
The rational development of small molecule tachykinin NK3 receptor selective antagonists - the utilisation of a dipeptide chemical library in drug design
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 14 | 6.76 | 8.00 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL437797 | NEUROKININ B | — | 1 | 8.00 |
| CHEMBL444832 | — | — | 1 | 7.80 |
| CHEMBL106124 | SENKTIDE | — | 1 | 7.68 |
| CHEMBL298477 | — | — | 1 | 7.55 |
| CHEMBL295301 | — | — | 1 | 7.41 |
| CHEMBL297327 | — | — | 1 | 7.40 |
| CHEMBL295982 | — | — | 1 | 7.04 |
| CHEMBL47929 | — | — | 1 | 6.99 |
| CHEMBL46290 | — | — | 1 | 6.64 |
| CHEMBL430952 | — | — | 1 | 6.37 |
| CHEMBL46113 | — | — | 1 | 5.82 |
| CHEMBL298252 | — | — | 1 | 5.77 |
| CHEMBL416641 | — | — | 1 | 5.23 |
| CHEMBL295041 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL437797 | NEUROKININ B | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL444832 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL106124 | SENKTIDE | IC50 | = | 21.0 | nM | 7.68 |
| CHEMBL298477 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL295301 | — | IC50 | = | 39.0 | nM | 7.41 |
| CHEMBL297327 | — | IC50 | = | 40.0 | nM | 7.40 |
| CHEMBL295982 | — | IC50 | = | 92.0 | nM | 7.04 |
| CHEMBL47929 | — | IC50 | = | 102.0 | nM | 6.99 |
| CHEMBL46290 | — | IC50 | = | 229.0 | nM | 6.64 |
| CHEMBL430952 | — | IC50 | = | 425.0 | nM | 6.37 |
| CHEMBL46113 | — | IC50 | = | 1520.0 | nM | 5.82 |
| CHEMBL298252 | — | IC50 | = | 1690.0 | nM | 5.77 |
| CHEMBL416641 | — | IC50 | = | 5890.0 | nM | 5.23 |
| CHEMBL295041 | — | IC50 | = | 10000.0 | nM | 5.00 |