Assay Detail
Binding
CHEMBL4880046
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCRScan assay: inhibition of H1
199
Total Activities
179
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 | 179 | - | - |
| Ki | 20 | 5.82 | 7.73 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | stable HEK |
| PMID | PMID | - | — | 9794809/7925364 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 0.6 – 2.0 |
| Radioligand Kd | Radioligand Kd | 0.97 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-Pyrilamine |
| Radioligand pKd | Radioligand pKd | 9.01 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.05 | — | — |
| Reference ligand | Reference ligand | - | — | Chlorpheniramine |
| Reference ligand Ki | Reference ligand Ki | 1.64 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 8.78 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.02 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL3337895 | T-26f | — | 3 | 7.73 |
| CHEMBL3337894 | T-26c | — | 3 | 7.01 |
| CHEMBL4576555 | T3-CLK-N | — | 3 | 5.88 |
| CHEMBL4520788 | BAY-294 | — | 3 | 5.87 |
| CHEMBL4531334 | T3-CLK | — | 3 | 5.67 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.34 |
| CHEMBL4586794 | ABT-100 | — | 3 | 5.00 |
| CHEMBL111612 | ABT-546 | — | 3 | 5.00 |
| CHEMBL4448899 | BAY-876 | — | 3 | 5.00 |
| CHEMBL4516843 | BAY-207 | — | 1 | - |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4564312 | BAY-786 | — | 1 | - |
| CHEMBL4552180 | BAY-588 | — | 1 | - |
| CHEMBL4445670 | BAY-885 | — | 1 | - |
| CHEMBL4455582 | BAY-693 | — | 1 | - |
| CHEMBL4630644 | BAY-386 | — | 1 | - |
| CHEMBL4630643 | BAY-448 | — | 1 | - |
| CHEMBL3907057 | BAY-826 | — | 1 | - |
| CHEMBL4096813 | — | — | 1 | - |
| CHEMBL4521594 | BAY-1797 | — | 1 | - |
| CHEMBL4539943 | BAY-694 | — | 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 | - |
| CHEMBL4526341 | A-108 | — | 1 | - |
| CHEMBL3701197 | A-226 | — | 1 | - |
| CHEMBL3697701 | A-079 | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL3337895 | T-26f | Ki | = | 18.62 | nM | 7.73 |
| CHEMBL3337895 | T-26f | Ki | = | 19.0 | nM | 7.72 |
| CHEMBL3337894 | T-26c | Ki | = | 98.0 | nM | 7.01 |
| CHEMBL3337894 | T-26c | Ki | = | 100.0 | nM | 7.00 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 1318.26 | nM | 5.88 |
| CHEMBL4520788 | BAY-294 | Ki | = | 1365.75 | nM | 5.87 |
| CHEMBL4520788 | BAY-294 | Ki | = | 1348.96 | nM | 5.87 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 1901.2 | nM | 5.72 |
| CHEMBL4531334 | T3-CLK | Ki | = | 2137.96 | nM | 5.67 |
| CHEMBL4531334 | T3-CLK | Ki | = | 2154.79 | nM | 5.67 |
| CHEMBL3480577 | UCSF924 | Ki | = | 4553.0 | nM | 5.34 |
| CHEMBL3480577 | UCSF924 | Ki | = | 4677.35 | nM | 5.33 |
| CHEMBL4448899 | BAY-876 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4448899 | BAY-876 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL111612 | ABT-546 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4586794 | ABT-100 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL111612 | ABT-546 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4586794 | ABT-100 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4516611 | BTZO-1 | Inhibition | = | -14.85 | % | - |
| CHEMBL4063249 | TP-021n | Inhibition | = | 14.73 | % | - |
| CHEMBL4075278 | — | Inhibition | = | 16.99 | % | - |
| CHEMBL4647642 | BAY-173 | Inhibition | = | 14.28 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | 20.53 | % | - |
| CHEMBL4458424 | BAY-899 | Inhibition | = | 5.89 | % | - |
| CHEMBL4592872 | BAY-897 | Inhibition | = | 15.89 | % | - |
| CHEMBL4537673 | BAY-985 | Inhibition | = | 35.0 | % | - |
| CHEMBL4538591 | BAY-440 | Inhibition | = | 26.36 | % | - |
| CHEMBL4580220 | BAY-3827 | Inhibition | = | 6.23 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | 0.94 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | -8.33 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 39.34 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | 16.43 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | -5.64 | % | - |
| CHEMBL4636881 | GSK046 | Inhibition | = | -10.65 | % | - |
| CHEMBL4561806 | BTZO-4 | Inhibition | = | 49.86 | % | - |
| CHEMBL4282264 | A-485 | Inhibition | = | 1.99 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | -7.68 | % | - |
| CHEMBL4798829 | — | Inhibition | = | 37.38 | % | - |
| CHEMBL4545807 | BAY-070 | Inhibition | = | 0.44 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | 0.33 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | -26.88 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | -1.58 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 28.43 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | 9.7 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | -11.53 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | -4.38 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | 3.2 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | 10.26 | % | - |
| CHEMBL4544690 | BI 2049 | Inhibition | = | 3.07 | % | - |
| CHEMBL3137331 | DEFACTINIB | Inhibition | = | -3.38 | % | - |