Assay Detail
Binding
CHEMBL964158
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Binding affinity to rat sst1 receptor
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of novel non-peptidic beta-alanine piperazine amide derivatives and their optimization to achiral, easily accessible, potent and selective somatostatin sst1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 34 | 8.20 | 9.49 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL540705 | — | — | 1 | 9.49 |
| CHEMBL473763 | — | — | 1 | 9.24 |
| CHEMBL461988 | — | — | 1 | 9.15 |
| CHEMBL523814 | — | — | 1 | 9.13 |
| CHEMBL460542 | — | — | 1 | 9.11 |
| CHEMBL462336 | — | — | 1 | 9.05 |
| CHEMBL515907 | — | — | 1 | 9.02 |
| CHEMBL491497 | — | — | 1 | 8.96 |
| CHEMBL515113 | — | — | 1 | 8.77 |
| CHEMBL472751 | — | — | 1 | 8.72 |
| CHEMBL491507 | — | — | 1 | 8.71 |
| CHEMBL491144 | — | — | 1 | 8.67 |
| CHEMBL473762 | — | — | 1 | 8.48 |
| CHEMBL472752 | — | — | 1 | 8.44 |
| CHEMBL491508 | — | — | 1 | 8.34 |
| CHEMBL491498 | — | — | 1 | 8.34 |
| CHEMBL514027 | — | — | 1 | 8.33 |
| CHEMBL491145 | — | — | 1 | 8.18 |
| CHEMBL474345 | — | — | 1 | 8.15 |
| CHEMBL517921 | — | — | 1 | 7.94 |
| CHEMBL462335 | — | — | 1 | 7.90 |
| CHEMBL474752 | — | — | 1 | 7.86 |
| CHEMBL474745 | — | — | 1 | 7.75 |
| CHEMBL516837 | — | — | 1 | 7.74 |
| CHEMBL522135 | — | — | 1 | 7.67 |
| CHEMBL472750 | — | — | 1 | 7.62 |
| CHEMBL462159 | — | — | 1 | 7.53 |
| CHEMBL470500 | — | — | 1 | 7.50 |
| CHEMBL470331 | — | — | 1 | 7.34 |
| CHEMBL495264 | — | — | 1 | 7.21 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL540705 | — | Kd | = | 0.3236 | nM | 9.49 |
| CHEMBL473763 | — | Kd | = | 0.5754 | nM | 9.24 |
| CHEMBL461988 | — | Kd | = | 0.7079 | nM | 9.15 |
| CHEMBL523814 | — | Kd | = | 0.7413 | nM | 9.13 |
| CHEMBL460542 | — | Kd | = | 0.7762 | nM | 9.11 |
| CHEMBL462336 | — | Kd | = | 0.8913 | nM | 9.05 |
| CHEMBL515907 | — | Kd | = | 0.955 | nM | 9.02 |
| CHEMBL491497 | — | Kd | = | 1.096 | nM | 8.96 |
| CHEMBL515113 | — | Kd | = | 1.698 | nM | 8.77 |
| CHEMBL472751 | — | Kd | = | 1.905 | nM | 8.72 |
| CHEMBL491507 | — | Kd | = | 1.95 | nM | 8.71 |
| CHEMBL491144 | — | Kd | = | 2.138 | nM | 8.67 |
| CHEMBL473762 | — | Kd | = | 3.311 | nM | 8.48 |
| CHEMBL472752 | — | Kd | = | 3.631 | nM | 8.44 |
| CHEMBL491498 | — | Kd | = | 4.571 | nM | 8.34 |
| CHEMBL491508 | — | Kd | = | 4.571 | nM | 8.34 |
| CHEMBL514027 | — | Kd | = | 4.677 | nM | 8.33 |
| CHEMBL491145 | — | Kd | = | 6.607 | nM | 8.18 |
| CHEMBL474345 | — | Kd | = | 7.079 | nM | 8.15 |
| CHEMBL517921 | — | Kd | = | 11.48 | nM | 7.94 |
| CHEMBL462335 | — | Kd | = | 12.59 | nM | 7.90 |
| CHEMBL474752 | — | Kd | = | 13.8 | nM | 7.86 |
| CHEMBL474745 | — | Kd | = | 17.78 | nM | 7.75 |
| CHEMBL516837 | — | Kd | = | 18.2 | nM | 7.74 |
| CHEMBL522135 | — | Kd | = | 21.38 | nM | 7.67 |
| CHEMBL472750 | — | Kd | = | 23.99 | nM | 7.62 |
| CHEMBL462159 | — | Kd | = | 29.51 | nM | 7.53 |
| CHEMBL470500 | — | Kd | = | 31.62 | nM | 7.50 |
| CHEMBL470331 | — | Kd | = | 45.71 | nM | 7.34 |
| CHEMBL495264 | — | Kd | = | 61.66 | nM | 7.21 |
| CHEMBL462158 | — | Kd | = | 77.62 | nM | 7.11 |
| CHEMBL460934 | — | Kd | = | 275.42 | nM | 6.56 |
| CHEMBL462157 | — | Kd | = | 331.13 | nM | 6.48 |
| CHEMBL491143 | — | Kd | > | 1000.0 | nM | - |