Assay Detail
Binding
CHEMBL4880044
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GPCRScan assay: inhibition of KOR
221
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 | 183 | - | - |
| Ki | 38 | 5.83 | 6.95 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | stable HEK |
| PMID | PMID | - | — | 8234341/2986999 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 0.6 – 1.2 |
| Radioligand Kd | Radioligand Kd | 0.83 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-U69593 |
| Radioligand pKd | Radioligand pKd | 9.08 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.04 | — | — |
| Reference ligand | Reference ligand | - | — | Salvinorin A |
| Reference ligand Ki | Reference ligand Ki | 2.98 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 8.53 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.02 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3907057 | BAY-826 | — | 3 | 6.95 |
| CHEMBL1971943 | BAY-549 | — | 3 | 6.73 |
| CHEMBL5092747 | — | — | 3 | 6.70 |
| CHEMBL4546802 | BAY-4900 | — | 3 | 6.41 |
| CHEMBL4802039 | JNJ-65355394 | — | 3 | 6.13 |
| CHEMBL4520788 | BAY-294 | — | 3 | 6.08 |
| CHEMBL4576555 | T3-CLK-N | — | 3 | 6.01 |
| CHEMBL5094181 | — | — | 3 | 5.93 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.66 |
| CHEMBL4513786 | A-545 | — | 3 | 5.55 |
| CHEMBL4638406 | BAY-3153 | — | 3 | 5.52 |
| CHEMBL4592872 | BAY-897 | — | 3 | 5.50 |
| CHEMBL4558518 | GSI-NC | — | 9 | 5.48 |
| CHEMBL3640116 | BI-1942 | — | 3 | 5.32 |
| CHEMBL4458424 | BAY-899 | — | 3 | 5.12 |
| CHEMBL4526351 | BAY-309 | — | 3 | 5.00 |
| CHEMBL3697701 | A-079 | — | 1 | - |
| CHEMBL3701197 | A-226 | — | 1 | - |
| CHEMBL4586794 | ABT-100 | — | 1 | - |
| CHEMBL4526341 | A-108 | — | 1 | - |
| CHEMBL111612 | ABT-546 | — | 1 | - |
| CHEMBL332794 | A-192621 | — | 1 | - |
| CHEMBL4093612 | A-1596586 | — | 1 | - |
| CHEMBL4066040 | A-1596584 | — | 1 | - |
| CHEMBL4593677 | BAY-474 | — | 1 | - |
| CHEMBL4522773 | BAY-827 | — | 1 | - |
| CHEMBL4585243 | BAY-7598 | — | 1 | - |
| CHEMBL4539943 | BAY-694 | — | 1 | - |
| CHEMBL4521594 | BAY-1797 | — | 1 | - |
| CHEMBL4516843 | BAY-207 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3907057 | BAY-826 | Ki | = | 112.2 | nM | 6.95 |
| CHEMBL3907057 | BAY-826 | Ki | = | 124.61 | nM | 6.90 |
| CHEMBL1971943 | BAY-549 | Ki | = | 186.21 | nM | 6.73 |
| CHEMBL1971943 | BAY-549 | Ki | = | 187.33 | nM | 6.73 |
| CHEMBL5092747 | — | Ki | = | 199.53 | nM | 6.70 |
| CHEMBL5092747 | — | Ki | = | 197.79 | nM | 6.70 |
| CHEMBL4546802 | BAY-4900 | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL4546802 | BAY-4900 | Ki | = | 390.57 | nM | 6.41 |
| CHEMBL4802039 | JNJ-65355394 | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL4802039 | JNJ-65355394 | Ki | = | 773.3 | nM | 6.11 |
| CHEMBL4520788 | BAY-294 | Ki | = | 841.37 | nM | 6.08 |
| CHEMBL4520788 | BAY-294 | Ki | = | 822.24 | nM | 6.08 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 977.24 | nM | 6.01 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 990.27 | nM | 6.00 |
| CHEMBL5094181 | — | Ki | = | 1174.9 | nM | 5.93 |
| CHEMBL5094181 | — | Ki | = | 1168.96 | nM | 5.93 |
| CHEMBL3480577 | UCSF924 | Ki | = | 2187.76 | nM | 5.66 |
| CHEMBL3480577 | UCSF924 | Ki | = | 2307.75 | nM | 5.64 |
| CHEMBL4513786 | A-545 | Ki | = | 2784.5 | nM | 5.55 |
| CHEMBL4513786 | A-545 | Ki | = | 2818.38 | nM | 5.55 |
| CHEMBL4638406 | BAY-3153 | Ki | = | 3019.95 | nM | 5.52 |
| CHEMBL4638406 | BAY-3153 | Ki | = | 3005.38 | nM | 5.52 |
| CHEMBL4592872 | BAY-897 | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL4592872 | BAY-897 | Ki | = | 3134.73 | nM | 5.50 |
| CHEMBL4558518 | GSI-NC | Ki | = | 3311.31 | nM | 5.48 |
| CHEMBL4558518 | GSI-NC | Ki | = | 3305.0 | nM | 5.48 |
| CHEMBL4558518 | GSI-NC | Ki | = | 3305.0 | nM | 5.48 |
| CHEMBL4558518 | GSI-NC | Ki | = | 3311.31 | nM | 5.48 |
| CHEMBL4558518 | GSI-NC | Ki | = | 3311.31 | nM | 5.48 |
| CHEMBL4558518 | GSI-NC | Ki | = | 3305.0 | nM | 5.48 |
| CHEMBL3640116 | BI-1942 | Ki | = | 4786.3 | nM | 5.32 |
| CHEMBL3640116 | BI-1942 | Ki | = | 4948.48 | nM | 5.31 |
| CHEMBL4458424 | BAY-899 | Ki | = | 7585.78 | nM | 5.12 |
| CHEMBL4458424 | BAY-899 | Ki | = | 7634.84 | nM | 5.12 |
| CHEMBL4526351 | BAY-309 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4526351 | BAY-309 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4568735 | NVS-MALT1 | Inhibition | = | 31.9 | % | - |
| CHEMBL4558518 | GSI-NC | Inhibition | = | 69.81 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | 37.52 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | 16.52 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | 14.71 | % | - |
| CHEMBL4584981 | NVS-MALT1-C | Inhibition | = | 29.45 | % | - |
| CHEMBL3137331 | DEFACTINIB | Inhibition | = | 10.82 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | 12.55 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | 9.67 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | -9.45 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | 16.41 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | 46.83 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 47.32 | % | - |
| CHEMBL4555711 | BAY-9897 | Inhibition | = | 10.47 | % | - |