Assay Detail
Binding
CHEMBL4880035
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GPCRScan assay: inhibition of D2
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 | 5.83 | 6.48 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | stable fibroblast |
| PMID | PMID | - | — | 1977888/26685100 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 0.4 – 1.0 |
| Radioligand Kd | Radioligand Kd | 0.47 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-N-methylspiperone |
| Radioligand pKd | Radioligand pKd | 9.33 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.06 | — | — |
| Reference ligand | Reference ligand | - | — | Haloperidol |
| Reference ligand Ki | Reference ligand Ki | 7.15 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 8.15 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.02 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4522930 | BI-605906 | — | 3 | 6.48 |
| CHEMBL4520293 | (R)-ZINC-3573 | — | 3 | 6.45 |
| CHEMBL4456585 | WM-1119 | — | 3 | 6.41 |
| CHEMBL4637208 | GSK973 | — | 3 | 6.09 |
| CHEMBL4558518 | GSI-NC | — | 3 | 5.91 |
| CHEMBL4520788 | BAY-294 | — | 3 | 5.70 |
| CHEMBL4576555 | T3-CLK-N | — | 3 | 5.63 |
| CHEMBL561132 | MK-7246 | 1.0 | 3 | 5.43 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.40 |
| CHEMBL4526351 | BAY-309 | — | 3 | 5.00 |
| CHEMBL4522773 | BAY-827 | — | 1 | - |
| CHEMBL4585243 | BAY-7598 | — | 1 | - |
| CHEMBL4539943 | BAY-694 | — | 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 | - |
| 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 |
|---|---|---|---|---|---|---|
| CHEMBL4522930 | BI-605906 | Ki | = | 331.13 | nM | 6.48 |
| CHEMBL4522930 | BI-605906 | Ki | = | 341.44 | nM | 6.47 |
| CHEMBL4520293 | (R)-ZINC-3573 | Ki | = | 354.81 | nM | 6.45 |
| CHEMBL4520293 | (R)-ZINC-3573 | Ki | = | 369.37 | nM | 6.43 |
| CHEMBL4456585 | WM-1119 | Ki | = | 389.05 | nM | 6.41 |
| CHEMBL4456585 | WM-1119 | Ki | = | 397.52 | nM | 6.40 |
| CHEMBL4637208 | GSK973 | Ki | = | 812.83 | nM | 6.09 |
| CHEMBL4637208 | GSK973 | Ki | = | 967.0 | nM | 6.01 |
| CHEMBL4558518 | GSI-NC | Ki | = | 1219.0 | nM | 5.91 |
| CHEMBL4558518 | GSI-NC | Ki | = | 1258.93 | nM | 5.90 |
| CHEMBL4520788 | BAY-294 | Ki | = | 1995.26 | nM | 5.70 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 2344.23 | nM | 5.63 |
| CHEMBL4520788 | BAY-294 | Ki | = | 2333.64 | nM | 5.63 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 2752.36 | nM | 5.56 |
| CHEMBL561132 | MK-7246 | Ki | = | 3746.0 | nM | 5.43 |
| CHEMBL3480577 | UCSF924 | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL561132 | MK-7246 | Ki | = | 3981.07 | nM | 5.40 |
| CHEMBL3480577 | UCSF924 | Ki | = | 4328.0 | nM | 5.36 |
| CHEMBL4526351 | BAY-309 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4526351 | BAY-309 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4538591 | BAY-440 | Inhibition | = | 10.62 | % | - |
| CHEMBL4580220 | BAY-3827 | Inhibition | = | -10.36 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | -13.67 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | 79.62 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 69.78 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | 2.85 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | -7.4 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | -5.46 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | -5.95 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | -12.15 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 9.71 | % | - |
| CHEMBL3623630 | — | Inhibition | = | 50.0 | % | - |
| CHEMBL4647642 | BAY-173 | Inhibition | = | -16.5 | % | - |
| CHEMBL4075278 | — | Inhibition | = | 2.86 | % | - |
| CHEMBL4638406 | BAY-3153 | Inhibition | = | 7.26 | % | - |
| CHEMBL4514203 | BAY-390 | Inhibition | = | -22.13 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | -8.75 | % | - |
| CHEMBL4798829 | — | Inhibition | = | 5.5 | % | - |
| CHEMBL4545807 | BAY-070 | Inhibition | = | 44.65 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | 27.74 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | 60.9 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | -10.18 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -16.84 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | -5.66 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | -23.45 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | -29.44 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | 7.62 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | 16.44 | % | - |
| CHEMBL3137331 | DEFACTINIB | Inhibition | = | -33.27 | % | - |
| CHEMBL4063249 | TP-021n | Inhibition | = | -18.93 | % | - |