Assay Detail
Binding
CHEMBL4880043
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GPCRScan assay: inhibition of DOR
193
Total Activities
181
Compounds Tested
2
Activity Types
12
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
SGC PDSP GPCRScan assays
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 181 | - | - |
| Ki | 12 | 6.06 | 7.35 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | stable HEK |
| PMID | PMID | - | — | 6316063/2986120 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 1.0 – 2.0 |
| Radioligand Kd | Radioligand Kd | 2.69 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-DADLE |
| Radioligand pKd | Radioligand pKd | 8.57 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.05 | — | — |
| Reference ligand | Reference ligand | - | — | Naltrindole |
| Reference ligand Ki | Reference ligand Ki | 0.5 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 9.3 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.02 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3086284 | KISS1-305 | — | 3 | 7.35 |
| CHEMBL4802046 | MSC-0516 | — | 3 | 6.23 |
| CHEMBL4578164 | MRL-CB1-NC | — | 3 | 5.85 |
| CHEMBL4526351 | BAY-309 | — | 3 | 5.76 |
| CHEMBL3342332 | A-1155463 | — | 3 | 5.67 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.00 |
| CHEMBL4539943 | BAY-694 | — | 1 | - |
| CHEMBL3907057 | BAY-826 | — | 1 | - |
| CHEMBL4521594 | BAY-1797 | — | 1 | - |
| CHEMBL4516843 | BAY-207 | — | 1 | - |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4564312 | BAY-786 | — | 1 | - |
| CHEMBL4448899 | BAY-876 | — | 1 | - |
| CHEMBL4552180 | BAY-588 | — | 1 | - |
| CHEMBL4445670 | BAY-885 | — | 1 | - |
| CHEMBL4455582 | BAY-693 | — | 1 | - |
| CHEMBL4630644 | BAY-386 | — | 1 | - |
| CHEMBL4630643 | BAY-448 | — | 1 | - |
| CHEMBL4585243 | BAY-7598 | — | 1 | - |
| CHEMBL4522773 | BAY-827 | — | 1 | - |
| CHEMBL4593677 | BAY-474 | — | 1 | - |
| CHEMBL4066040 | A-1596584 | — | 1 | - |
| CHEMBL4093612 | A-1596586 | — | 1 | - |
| CHEMBL332794 | A-192621 | — | 1 | - |
| CHEMBL4513786 | A-545 | — | 1 | - |
| CHEMBL111612 | ABT-546 | — | 1 | - |
| CHEMBL4526341 | A-108 | — | 1 | - |
| CHEMBL4586794 | ABT-100 | — | 1 | - |
| CHEMBL3701197 | A-226 | — | 1 | - |
| CHEMBL3697701 | A-079 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3086284 | KISS1-305 | Ki | = | 44.67 | nM | 7.35 |
| CHEMBL3086284 | KISS1-305 | Ki | = | 47.5 | nM | 7.32 |
| CHEMBL4802046 | MSC-0516 | Ki | = | 588.84 | nM | 6.23 |
| CHEMBL4802046 | MSC-0516 | Ki | = | 597.96 | nM | 6.22 |
| CHEMBL4578164 | MRL-CB1-NC | Ki | = | 1415.0 | nM | 5.85 |
| CHEMBL4578164 | MRL-CB1-NC | Ki | = | 1412.54 | nM | 5.85 |
| CHEMBL4526351 | BAY-309 | Ki | = | 1737.8 | nM | 5.76 |
| CHEMBL4526351 | BAY-309 | Ki | = | 1733.0 | nM | 5.76 |
| CHEMBL3342332 | A-1155463 | Ki | = | 2118.36 | nM | 5.67 |
| CHEMBL3342332 | A-1155463 | Ki | = | 2137.96 | nM | 5.67 |
| CHEMBL3480577 | UCSF924 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4638406 | BAY-3153 | Inhibition | = | 10.33 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 15.43 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | 14.51 | % | - |
| CHEMBL4580220 | BAY-3827 | Inhibition | = | 20.48 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | 17.66 | % | - |
| CHEMBL4537673 | BAY-985 | Inhibition | = | 29.03 | % | - |
| CHEMBL4592872 | BAY-897 | Inhibition | = | 32.71 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | 20.56 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 34.28 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | 2.89 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | 9.2 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | 28.83 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | 30.08 | % | - |
| CHEMBL4458424 | BAY-899 | Inhibition | = | -10.33 | % | - |
| CHEMBL3589752 | IPP/CNRS-A017 | Inhibition | = | 2.124 | % | - |
| CHEMBL3590047 | IPP/CNRS-A019 | Inhibition | = | 1.01 | % | - |
| CHEMBL4636881 | GSK046 | Inhibition | = | 27.07 | % | - |
| CHEMBL4635540 | GSK791 | Inhibition | = | 21.99 | % | - |
| CHEMBL4555711 | BAY-9897 | Inhibition | = | 14.42 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | 2.46 | % | - |
| CHEMBL4635134 | GSK620 | Inhibition | = | -2.78 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | 8.3 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | -0.33 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | -5.22 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | 5.07 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | -0.84 | % | - |
| CHEMBL4568735 | NVS-MALT1 | Inhibition | = | -26.4 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -20.87 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | 17.07 | % | - |
| CHEMBL4647642 | BAY-173 | Inhibition | = | -14.99 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | 38.45 | % | - |
| CHEMBL4545807 | BAY-070 | Inhibition | = | 3.76 | % | - |
| CHEMBL4798829 | — | Inhibition | = | 21.98 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | -10.62 | % | - |
| CHEMBL4282264 | A-485 | Inhibition | = | -2.53 | % | - |
| CHEMBL4561806 | BTZO-4 | Inhibition | = | -0.6239 | % | - |
| CHEMBL4516611 | BTZO-1 | Inhibition | = | 4.807 | % | - |
| CHEMBL4063249 | TP-021n | Inhibition | = | -0.28 | % | - |
| CHEMBL4075278 | — | Inhibition | = | 3.32 | % | - |