Assay Detail
Binding
CHEMBL4880032
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GPCRScan assay: inhibition of 5-HT6
203
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 | 22 | 5.79 | 6.22 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | stable HEK |
| PMID | PMID | - | — | 9284367.0 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 2.0 – 4.0 |
| Radioligand Kd | Radioligand Kd | 4.27 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-LSD |
| Radioligand pKd | Radioligand pKd | 8.37 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.04 | — | — |
| Reference ligand | Reference ligand | - | — | Clozapine |
| Reference ligand Ki | Reference ligand Ki | 5.27 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 8.28 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.02 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4748908 | TP-040n | — | 3 | 6.22 |
| CHEMBL4522773 | BAY-827 | — | 3 | 6.20 |
| CHEMBL4520293 | (R)-ZINC-3573 | — | 3 | 6.13 |
| CHEMBL4534980 | (S)-ZINC-3573 | — | 3 | 5.96 |
| CHEMBL4802046 | MSC-0516 | — | 3 | 5.84 |
| CHEMBL3582461 | MSD-CYP11B2-Negative-control | — | 3 | 5.51 |
| CHEMBL4798829 | — | — | 3 | 5.28 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.20 |
| CHEMBL4539943 | BAY-694 | — | 1 | - |
| CHEMBL4630643 | BAY-448 | — | 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 | - |
| CHEMBL4585243 | BAY-7598 | — | 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 |
|---|---|---|---|---|---|---|
| CHEMBL4748908 | TP-040n | Ki | = | 602.56 | nM | 6.22 |
| CHEMBL4748908 | TP-040n | Ki | = | 606.4 | nM | 6.22 |
| CHEMBL4522773 | BAY-827 | Ki | = | 630.96 | nM | 6.20 |
| CHEMBL4522773 | BAY-827 | Ki | = | 674.0 | nM | 6.17 |
| CHEMBL4520293 | (R)-ZINC-3573 | Ki | = | 748.23 | nM | 6.13 |
| CHEMBL4520293 | (R)-ZINC-3573 | Ki | = | 741.31 | nM | 6.13 |
| CHEMBL4534980 | (S)-ZINC-3573 | Ki | = | 1092.22 | nM | 5.96 |
| CHEMBL4534980 | (S)-ZINC-3573 | Ki | = | 1083.93 | nM | 5.96 |
| CHEMBL4802046 | MSC-0516 | Ki | = | 1445.44 | nM | 5.84 |
| CHEMBL4802046 | MSC-0516 | Ki | = | 1523.62 | nM | 5.82 |
| CHEMBL3582461 | MSD-CYP11B2-Negative-control | Ki | = | 3060.55 | nM | 5.51 |
| CHEMBL3582461 | MSD-CYP11B2-Negative-control | Ki | = | 3090.3 | nM | 5.51 |
| CHEMBL4798829 | — | Ki | = | 5239.62 | nM | 5.28 |
| CHEMBL4798829 | — | Ki | = | 5248.07 | nM | 5.28 |
| CHEMBL3480577 | UCSF924 | Ki | = | 6309.57 | nM | 5.20 |
| CHEMBL3480577 | UCSF924 | Ki | = | 6681.0 | nM | 5.17 |
| CHEMBL4630642 | BAY-974 | Inhibition | = | 2.21 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | -20.19 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 58.85 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | 69.1 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | 26.66 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | -3.95 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | 8.15 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | 13.0 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 6.59 | % | - |
| CHEMBL4514203 | BAY-390 | Inhibition | = | -26.38 | % | - |
| CHEMBL4555711 | BAY-9897 | Inhibition | = | -4.02 | % | - |
| CHEMBL4561806 | BTZO-4 | Inhibition | = | -15.88 | % | - |
| CHEMBL4063249 | TP-021n | Inhibition | = | -1.18 | % | - |
| CHEMBL4436748 | SR-318 | Inhibition | = | 26.83 | % | - |
| CHEMBL4075278 | — | Inhibition | = | -2.48 | % | - |
| CHEMBL4282264 | A-485 | Inhibition | = | 32.62 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | 24.11 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | -2.64 | % | - |
| CHEMBL4516611 | BTZO-1 | Inhibition | = | -1.328 | % | - |
| CHEMBL4445645 | — | Inhibition | = | 3.94 | % | - |
| CHEMBL4584981 | NVS-MALT1-C | Inhibition | = | -10.22 | % | - |
| CHEMBL4568735 | NVS-MALT1 | Inhibition | = | -23.54 | % | - |
| CHEMBL4518706 | PF-00911705 | Inhibition | = | 11.07 | % | - |
| CHEMBL3137331 | DEFACTINIB | Inhibition | = | -8.99 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | 16.11 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | 6.67 | % | - |
| CHEMBL4648362 | GSK789 | Inhibition | = | -37.35 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | -6.47 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | 2.79 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -20.04 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | -1.21 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | 16.77 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | -9.08 | % | - |
| CHEMBL4545807 | BAY-070 | Inhibition | = | 31.36 | % | - |