Assay Detail
Binding
CHEMBL888114
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Displacement of [125I]SRIF14 from rat sst2 receptor from rat brain cortex membrane
55
Total Activities
55
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus norvegicus |
| Confidence | 9 — Direct single protein target |
| Curated By | Intermediate |
Publication
SAR of the arylpiperazine moiety of obeline somatostatin sst1 receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Kd | 55 | 5.12 | 9.13 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL250304 | — | — | 1 | 9.13 |
| CHEMBL251111 | — | — | 1 | 5.69 |
| CHEMBL250724 | — | — | 1 | 5.68 |
| CHEMBL250914 | — | — | 1 | 5.63 |
| CHEMBL251110 | — | — | 1 | 5.62 |
| CHEMBL250912 | — | — | 1 | 5.60 |
| CHEMBL250922 | — | — | 1 | 5.46 |
| CHEMBL250921 | — | — | 1 | 5.44 |
| CHEMBL400099 | — | — | 1 | 5.37 |
| CHEMBL250305 | — | — | 1 | 5.36 |
| CHEMBL428583 | — | — | 1 | 5.31 |
| CHEMBL250703 | — | — | 1 | 5.29 |
| CHEMBL250522 | — | — | 1 | 5.28 |
| CHEMBL400137 | — | — | 1 | 5.28 |
| CHEMBL250723 | — | — | 1 | 5.28 |
| CHEMBL440962 | — | — | 1 | 5.26 |
| CHEMBL250521 | — | — | 1 | 5.26 |
| CHEMBL248715 | — | — | 1 | 5.24 |
| CHEMBL251300 | — | — | 1 | 5.21 |
| CHEMBL251116 | — | — | 1 | 5.18 |
| CHEMBL250498 | — | — | 1 | 5.17 |
| CHEMBL250920 | — | — | 1 | 5.15 |
| CHEMBL249930 | — | — | 1 | 5.13 |
| CHEMBL251541 | OBELIN | — | 1 | 5.11 |
| CHEMBL250705 | — | — | 1 | 5.06 |
| CHEMBL250098 | — | — | 1 | 5.06 |
| CHEMBL400386 | — | — | 1 | 5.04 |
| CHEMBL398319 | — | — | 1 | 5.04 |
| CHEMBL249932 | — | — | 1 | 5.00 |
| CHEMBL251120 | — | — | 1 | 5.00 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL250304 | — | Kd | = | 0.7413 | nM | 9.13 |
| CHEMBL251111 | — | Kd | = | 2041.74 | nM | 5.69 |
| CHEMBL250724 | — | Kd | = | 2089.3 | nM | 5.68 |
| CHEMBL250914 | — | Kd | = | 2344.23 | nM | 5.63 |
| CHEMBL251110 | — | Kd | = | 2398.83 | nM | 5.62 |
| CHEMBL250912 | — | Kd | = | 2511.89 | nM | 5.60 |
| CHEMBL250922 | — | Kd | = | 3467.37 | nM | 5.46 |
| CHEMBL250921 | — | Kd | = | 3630.78 | nM | 5.44 |
| CHEMBL400099 | — | Kd | = | 4265.8 | nM | 5.37 |
| CHEMBL250305 | — | Kd | = | 4365.16 | nM | 5.36 |
| CHEMBL428583 | — | Kd | = | 4897.79 | nM | 5.31 |
| CHEMBL250703 | — | Kd | = | 5128.61 | nM | 5.29 |
| CHEMBL400137 | — | Kd | = | 5248.07 | nM | 5.28 |
| CHEMBL250723 | — | Kd | = | 5248.07 | nM | 5.28 |
| CHEMBL250522 | — | Kd | = | 5248.07 | nM | 5.28 |
| CHEMBL440962 | — | Kd | = | 5495.41 | nM | 5.26 |
| CHEMBL250521 | — | Kd | = | 5495.41 | nM | 5.26 |
| CHEMBL248715 | — | Kd | = | 5754.4 | nM | 5.24 |
| CHEMBL251300 | — | Kd | = | 6165.95 | nM | 5.21 |
| CHEMBL251116 | — | Kd | = | 6606.93 | nM | 5.18 |
| CHEMBL250498 | — | Kd | = | 6760.83 | nM | 5.17 |
| CHEMBL250920 | — | Kd | = | 7079.46 | nM | 5.15 |
| CHEMBL249930 | — | Kd | = | 7413.1 | nM | 5.13 |
| CHEMBL251541 | OBELIN | Kd | = | 7762.47 | nM | 5.11 |
| CHEMBL250098 | — | Kd | = | 8709.64 | nM | 5.06 |
| CHEMBL250705 | — | Kd | = | 8709.64 | nM | 5.06 |
| CHEMBL400386 | — | Kd | = | 9120.11 | nM | 5.04 |
| CHEMBL398319 | — | Kd | = | 9120.11 | nM | 5.04 |
| CHEMBL249932 | — | Kd | = | 10000.0 | nM | 5.00 |
| CHEMBL251120 | — | Kd | = | 10000.0 | nM | 5.00 |
| CHEMBL251334 | — | Kd | = | 10232.93 | nM | 4.99 |
| CHEMBL440233 | — | Kd | = | 10232.93 | nM | 4.99 |
| CHEMBL250314 | — | Kd | = | 10471.29 | nM | 4.98 |
| CHEMBL398681 | — | Kd | = | 10964.78 | nM | 4.96 |
| CHEMBL440235 | — | Kd | = | 10964.78 | nM | 4.96 |
| CHEMBL398655 | — | Kd | = | 11748.98 | nM | 4.93 |
| CHEMBL400709 | — | Kd | = | 13182.57 | nM | 4.88 |
| CHEMBL398656 | — | Kd | = | 14125.38 | nM | 4.85 |
| CHEMBL250900 | — | Kd | = | 14791.08 | nM | 4.83 |
| CHEMBL249892 | — | Kd | = | 16595.87 | nM | 4.78 |
| CHEMBL400136 | — | Kd | = | 16595.87 | nM | 4.78 |
| CHEMBL250111 | — | Kd | = | 17782.79 | nM | 4.75 |
| CHEMBL251311 | — | Kd | = | 18620.87 | nM | 4.73 |
| CHEMBL249893 | — | Kd | = | 19952.62 | nM | 4.70 |
| CHEMBL250313 | — | Kd | = | 19952.62 | nM | 4.70 |
| CHEMBL251121 | — | Kd | = | 20892.96 | nM | 4.68 |
| CHEMBL249723 | — | Kd | = | 21379.62 | nM | 4.67 |
| CHEMBL250715 | — | Kd | = | 22387.21 | nM | 4.65 |
| CHEMBL250704 | — | Kd | = | 24547.09 | nM | 4.61 |
| CHEMBL5483015 | ARSENIC TRIOXIDE | Kd | = | 25118.86 | nM | 4.60 |