Assay Detail
Binding
CHEMBL5737006
Review assay metadata, readout intent, target linkage, and publication context from the same page.
SSTR4 I-125 Somatostatin Competition Binding Assay: This membrane-based assay measures the ability of compounds to competitively inhibit binding of I-125 labeled somatostatin to SSTR4 in membranes from CHO-K1 that overexpress SSTR4. Membranes from CHO-K1 cells overexpressing SSTR4 are purchased from Perkin Elmer (catalog number ES-524-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 0.2 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 1 μg of SSTR4 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 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 | 7.02 | 8.80 |
| kon | 114 | - | - |
| k_off | 114 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5745719 | — | — | 3 | 8.80 |
| CHEMBL6064025 | — | — | 3 | 8.40 |
| CHEMBL5790086 | — | — | 3 | 8.30 |
| CHEMBL6062387 | — | — | 3 | 8.10 |
| CHEMBL6048061 | — | — | 3 | 8.00 |
| CHEMBL5862026 | — | — | 3 | 8.00 |
| CHEMBL5801992 | — | — | 3 | 7.80 |
| CHEMBL5939370 | — | — | 3 | 7.80 |
| CHEMBL6027712 | — | — | 3 | 7.80 |
| CHEMBL5933642 | — | — | 3 | 7.70 |
| CHEMBL5977345 | — | — | 3 | 7.70 |
| CHEMBL6000561 | — | — | 3 | 7.70 |
| CHEMBL5802392 | — | — | 3 | 7.70 |
| CHEMBL5886715 | — | — | 3 | 7.70 |
| CHEMBL5982226 | — | — | 3 | 7.60 |
| CHEMBL5815326 | — | — | 3 | 7.60 |
| CHEMBL5980093 | — | — | 3 | 7.60 |
| CHEMBL6040848 | — | — | 3 | 7.60 |
| CHEMBL5858085 | — | — | 3 | 7.60 |
| CHEMBL6005000 | — | — | 3 | 7.60 |
| CHEMBL6052010 | — | — | 3 | 7.60 |
| CHEMBL6055274 | — | — | 3 | 7.60 |
| CHEMBL5920986 | — | — | 6 | 7.50 |
| CHEMBL5829751 | — | — | 3 | 7.50 |
| CHEMBL5901530 | — | — | 3 | 7.50 |
| CHEMBL5875145 | — | — | 3 | 7.40 |
| CHEMBL5894549 | — | — | 3 | 7.40 |
| CHEMBL5773674 | — | — | 3 | 7.40 |
| CHEMBL5999769 | — | — | 3 | 7.40 |
| CHEMBL5934843 | — | — | 3 | 7.40 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5745719 | — | IC50 | = | 1.58 | nM | 8.80 |
| CHEMBL6064025 | — | IC50 | = | 3.98 | nM | 8.40 |
| CHEMBL5790086 | — | IC50 | = | 5.01 | nM | 8.30 |
| CHEMBL6062387 | — | IC50 | = | 7.94 | nM | 8.10 |
| CHEMBL5862026 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6048061 | — | IC50 | = | 10.0 | nM | 8.00 |
| CHEMBL6027712 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL5939370 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL5801992 | — | IC50 | = | 15.8 | nM | 7.80 |
| CHEMBL5802392 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5933642 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL6000561 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5886715 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5977345 | — | IC50 | = | 20.0 | nM | 7.70 |
| CHEMBL5815326 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL5980093 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL6040848 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL5858085 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL6055274 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL5982226 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL6005000 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL6052010 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL5829751 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL5920986 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL5901530 | — | IC50 | = | 31.6 | nM | 7.50 |
| CHEMBL5999769 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL5748655 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL5875145 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL5894549 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL5800615 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL5934843 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL5773674 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL5899589 | — | IC50 | = | 39.8 | nM | 7.40 |
| CHEMBL5869711 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL6038753 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL5785607 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL5851110 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL5949740 | — | IC50 | = | 50.1 | nM | 7.30 |
| CHEMBL5933378 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5957831 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5818753 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5836617 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5807083 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5954140 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5801275 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5999051 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5841698 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL5814161 | — | IC50 | = | 63.1 | nM | 7.20 |
| CHEMBL6027274 | — | IC50 | = | 79.4 | nM | 7.10 |
| CHEMBL5934849 | — | IC50 | = | 79.4 | nM | 7.10 |