Assay Detail
Binding
CHEMBL5737007
Review assay metadata, readout intent, target linkage, and publication context from the same page.
SSTR1 I-125 Somatostatin Competition Binding Assay for Selectivity Versus SSTR4: This membrane-based assay measures the ability of compounds to competitively inhibit binding of I-125 labeled somatostatin to SSTR1 in membranes from CHO-K1 that overexpress SSTR1. Membranes from CHO-K1 cells overexpressing SSTR1 are purchased from Perkin Elmer (catalog number ES-520-M400UA). Test compounds are suspended in DMSO and then diluted in assay buffer (25 mM HEPES pH 7.4, 10 mM MgCl2, 1 mM CaCl2), 0.5% BSA) plus 0.4 nM I-125 labeled somatostatin (Perkin Elmer catalog number NEX389). Fifty μL of compound/I-125 somatostatin in assay buffer are added per well to 96-well poly-propylene plate. Then 10 μg of SSTR1 membranes in 50 μL assay buffer are added per well. The plate is incubated for 60 minutes at room temperature. FilterMat A filters (Perkin Elmer catalog number 1450-421) are pre-soaked in 0.5% PEI (Sigma catalog number P3143). The contents of the assay plate are transferred to filters with a TomTech harvester and washed 5 times with 20 mM HEPES, 100 mM NaCl. The filters are dried in a microwave oven then transferred to sample bag containing a scintillator sheet (Perkin Elmer catalog number 1450-441). The scintillator sheets are melted to the filters using a heat block. The filters are then read in a MicroBeta scintillation counter. Binding Ki curves are generated using Activity Base for Screening Data Management and the results are reported as pIC50.
342
Total Activities
109
Compounds Tested
3
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Confidence | 8 — Homologous single protein target |
| Curated By | Autocuration |
Publication
Piperidinyl-3-(aryloxy)propanamides and propanoates
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 114 | 5.25 | 7.00 |
| kon | 114 | - | - |
| k_off | 114 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5745719 | — | — | 3 | 7.00 |
| CHEMBL6055274 | — | — | 3 | 6.90 |
| CHEMBL5801992 | — | — | 3 | 6.90 |
| CHEMBL5812815 | — | — | 3 | 6.90 |
| CHEMBL5933642 | — | — | 3 | 6.80 |
| CHEMBL5852788 | — | — | 3 | 6.60 |
| CHEMBL5802392 | — | — | 3 | 6.50 |
| CHEMBL5797414 | — | — | 3 | 6.40 |
| CHEMBL5875145 | — | — | 3 | 6.40 |
| CHEMBL5987384 | — | — | 3 | 6.40 |
| CHEMBL5934843 | — | — | 3 | 6.20 |
| CHEMBL5748582 | — | — | 3 | 6.10 |
| CHEMBL5949740 | — | — | 3 | 6.10 |
| CHEMBL5785607 | — | — | 3 | 6.10 |
| CHEMBL5954701 | — | — | 3 | 6.00 |
| CHEMBL5857117 | — | — | 3 | 5.80 |
| CHEMBL5999769 | — | — | 3 | 5.80 |
| CHEMBL5862026 | — | — | 3 | 5.80 |
| CHEMBL5790086 | — | — | 3 | 5.80 |
| CHEMBL6027712 | — | — | 3 | 5.70 |
| CHEMBL5954140 | — | — | 3 | 5.70 |
| CHEMBL5939370 | — | — | 3 | 5.60 |
| CHEMBL5851110 | — | — | 3 | 5.60 |
| CHEMBL6041440 | — | — | 3 | 5.50 |
| CHEMBL5814161 | — | — | 3 | 5.50 |
| CHEMBL5818753 | — | — | 3 | 5.50 |
| CHEMBL5815326 | — | — | 3 | 5.50 |
| CHEMBL5801275 | — | — | 3 | 5.50 |
| CHEMBL5967165 | — | — | 3 | 5.50 |
| CHEMBL5899589 | — | — | 3 | 5.50 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5745719 | — | IC50 | = | 100.0 | nM | 7.00 |
| CHEMBL5812815 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5801992 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL6055274 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5933642 | — | IC50 | = | 158.0 | nM | 6.80 |
| CHEMBL5852788 | — | IC50 | = | 251.0 | nM | 6.60 |
| CHEMBL5802392 | — | IC50 | = | 316.0 | nM | 6.50 |
| CHEMBL5875145 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL5797414 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL5987384 | — | IC50 | = | 398.0 | nM | 6.40 |
| CHEMBL5934843 | — | IC50 | = | 631.0 | nM | 6.20 |
| CHEMBL5949740 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL5748582 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL5785607 | — | IC50 | = | 794.0 | nM | 6.10 |
| CHEMBL5954701 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL5862026 | — | IC50 | = | 1585.0 | nM | 5.80 |
| CHEMBL5999769 | — | IC50 | = | 1585.0 | nM | 5.80 |
| CHEMBL5790086 | — | IC50 | = | 1585.0 | nM | 5.80 |
| CHEMBL5857117 | — | IC50 | = | 1585.0 | nM | 5.80 |
| CHEMBL6027712 | — | IC50 | = | 1995.0 | nM | 5.70 |
| CHEMBL5954140 | — | IC50 | = | 1995.0 | nM | 5.70 |
| CHEMBL5939370 | — | IC50 | = | 2512.0 | nM | 5.60 |
| CHEMBL5851110 | — | IC50 | = | 2512.0 | nM | 5.60 |
| CHEMBL5899589 | — | IC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL5801275 | — | IC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL5818753 | — | IC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL5814161 | — | IC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL5815326 | — | IC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL5967165 | — | IC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL6041440 | — | IC50 | = | 3162.0 | nM | 5.50 |
| CHEMBL5886715 | — | IC50 | = | 3981.0 | nM | 5.40 |
| CHEMBL6008758 | — | IC50 | = | 3981.0 | nM | 5.40 |
| CHEMBL5999051 | — | IC50 | = | 3981.0 | nM | 5.40 |
| CHEMBL5829751 | — | IC50 | = | 5012.0 | nM | 5.30 |
| CHEMBL6038753 | — | IC50 | = | 5012.0 | nM | 5.30 |
| CHEMBL6005000 | — | IC50 | = | 5012.0 | nM | 5.30 |
| CHEMBL6053521 | — | IC50 | = | 5012.0 | nM | 5.30 |
| CHEMBL5920986 | — | IC50 | = | 5012.0 | nM | 5.30 |
| CHEMBL5841698 | — | IC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL5924029 | — | IC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL5836617 | — | IC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL5807083 | — | IC50 | = | 6310.0 | nM | 5.20 |
| CHEMBL5894549 | — | IC50 | = | 7943.0 | nM | 5.10 |
| CHEMBL5972254 | — | IC50 | = | 7943.0 | nM | 5.10 |
| CHEMBL6017778 | — | IC50 | = | 7943.0 | nM | 5.10 |
| CHEMBL6017778 | — | IC50 | = | 7943.0 | nM | 5.10 |
| CHEMBL5747308 | — | IC50 | = | 7943.0 | nM | 5.10 |
| CHEMBL5939445 | — | IC50 | = | 7943.0 | nM | 5.10 |
| CHEMBL5773674 | — | IC50 | = | 7943.0 | nM | 5.10 |
| CHEMBL6038030 | — | IC50 | = | 7943.0 | nM | 5.10 |