Assay Detail
Binding
CHEMBL4880050
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GPCRScan assay: inhibition of Alpha1A
195
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 | 14 | 5.92 | 6.37 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | stable HEK |
| PMID | PMID | - | — | 7780636/1687370 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 0.2 - 1.0 |
| Radioligand Kd | Radioligand Kd | 0.43 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-Prazosin |
| Radioligand pKd | Radioligand pKd | 9.36 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.07 | — | — |
| Reference ligand | Reference ligand | - | — | Prazosin |
| Reference ligand Ki | Reference ligand Ki | 0.7 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 9.16 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.03 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4535474 | BAY-293 | — | 3 | 6.37 |
| CHEMBL4520788 | BAY-294 | — | 3 | 6.36 |
| CHEMBL3797887 | (S)-9s | — | 3 | 5.97 |
| CHEMBL4576555 | T3-CLK-N | — | 3 | 5.87 |
| CHEMBL4752561 | — | — | 3 | 5.86 |
| CHEMBL4795065 | Borussertib | — | 3 | 5.58 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.00 |
| 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 | - |
| 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 |
|---|---|---|---|---|---|---|
| CHEMBL4535474 | BAY-293 | Ki | = | 428.25 | nM | 6.37 |
| CHEMBL4535474 | BAY-293 | Ki | = | 426.58 | nM | 6.37 |
| CHEMBL4520788 | BAY-294 | Ki | = | 436.52 | nM | 6.36 |
| CHEMBL4520788 | BAY-294 | Ki | = | 453.53 | nM | 6.34 |
| CHEMBL3797887 | (S)-9s | Ki | = | 1071.52 | nM | 5.97 |
| CHEMBL3797887 | (S)-9s | Ki | = | 1065.37 | nM | 5.97 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 1348.96 | nM | 5.87 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 1394.62 | nM | 5.86 |
| CHEMBL4752561 | — | Ki | = | 1394.44 | nM | 5.86 |
| CHEMBL4752561 | — | Ki | = | 1380.38 | nM | 5.86 |
| CHEMBL4795065 | Borussertib | Ki | = | 2655.83 | nM | 5.58 |
| CHEMBL4795065 | Borussertib | Ki | = | 2630.27 | nM | 5.58 |
| CHEMBL3480577 | UCSF924 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL3590047 | IPP/CNRS-A019 | Inhibition | = | -2.65 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 1.72 | % | - |
| CHEMBL4458424 | BAY-899 | Inhibition | = | -3.5 | % | - |
| CHEMBL4592872 | BAY-897 | Inhibition | = | 16.25 | % | - |
| CHEMBL4537673 | BAY-985 | Inhibition | = | 11.94 | % | - |
| CHEMBL4538591 | BAY-440 | Inhibition | = | 12.84 | % | - |
| CHEMBL4580220 | BAY-3827 | Inhibition | = | 6.85 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | 1.96 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | 9.59 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 21.8 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | 34.22 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | 5.91 | % | - |
| CHEMBL4648362 | GSK789 | Inhibition | = | 25.24 | % | - |
| CHEMBL4647642 | BAY-173 | Inhibition | = | 7.02 | % | - |
| CHEMBL3623630 | — | Inhibition | = | 6.7 | % | - |
| CHEMBL4635134 | GSK620 | Inhibition | = | -0.64 | % | - |
| CHEMBL4636881 | GSK046 | Inhibition | = | -12.8 | % | - |
| CHEMBL4635540 | GSK791 | Inhibition | = | 10.06 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | -4.55 | % | - |
| CHEMBL4638406 | BAY-3153 | Inhibition | = | 16.97 | % | - |
| CHEMBL3137331 | DEFACTINIB | Inhibition | = | -4.42 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | -1.65 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | -8.89 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | -4.09 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | 2.52 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | -26.36 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -33.2 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | 7.39 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | -0.5 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | 0.31 | % | - |
| CHEMBL4545807 | BAY-070 | Inhibition | = | 6.33 | % | - |
| CHEMBL4798829 | — | Inhibition | = | 15.53 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | 0.04 | % | - |
| CHEMBL4282264 | A-485 | Inhibition | = | -11.26 | % | - |
| CHEMBL4561806 | BTZO-4 | Inhibition | = | -9.971 | % | - |
| CHEMBL4516611 | BTZO-1 | Inhibition | = | -12.51 | % | - |
| CHEMBL4063249 | TP-021n | Inhibition | = | -23.18 | % | - |