Assay Detail
Binding
CHEMBL4880036
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GPCRScan assay: inhibition of D3
209
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 | 28 | 5.88 | 6.59 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | HEKT |
| PMID | PMID | - | — | 1977888/26685100 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 0.5 – 1.8 |
| Radioligand Kd | Radioligand Kd | 0.36 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-N-methylspiperone |
| Radioligand pKd | Radioligand pKd | 9.44 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.09 | — | — |
| Reference ligand | Reference ligand | - | — | Chlorpromazine |
| Reference ligand Ki | Reference ligand Ki | 10.3 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 7.99 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.02 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4637208 | GSK973 | — | 3 | 6.59 |
| CHEMBL4522930 | BI-605906 | — | 3 | 6.54 |
| CHEMBL4639128 | GSK778 | — | 3 | 6.39 |
| CHEMBL4558518 | GSI-NC | — | 3 | 6.15 |
| CHEMBL4520788 | BAY-294 | — | 3 | 6.06 |
| CHEMBL1800685 | PPTN | — | 3 | 6.05 |
| CHEMBL4535474 | BAY-293 | — | 3 | 6.03 |
| CHEMBL2048623 | — | — | 3 | 6.03 |
| CHEMBL4536197 | A-486 | — | 3 | 5.96 |
| CHEMBL4576555 | T3-CLK-N | — | 3 | 5.72 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.50 |
| CHEMBL5092747 | — | — | 3 | 5.44 |
| CHEMBL5087167 | — | — | 3 | 5.06 |
| CHEMBL4551344 | A-1210227 | — | 3 | 5.00 |
| CHEMBL4537788 | BAY-784 | — | 1 | - |
| CHEMBL4516843 | BAY-207 | — | 1 | - |
| CHEMBL4521594 | BAY-1797 | — | 1 | - |
| CHEMBL4539943 | BAY-694 | — | 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 |
|---|---|---|---|---|---|---|
| CHEMBL4637208 | GSK973 | Ki | = | 257.47 | nM | 6.59 |
| CHEMBL4637208 | GSK973 | Ki | = | 257.04 | nM | 6.59 |
| CHEMBL4522930 | BI-605906 | Ki | = | 288.4 | nM | 6.54 |
| CHEMBL4639128 | GSK778 | Ki | = | 407.38 | nM | 6.39 |
| CHEMBL4522930 | BI-605906 | Ki | = | 428.07 | nM | 6.37 |
| CHEMBL4639128 | GSK778 | Ki | = | 485.92 | nM | 6.31 |
| CHEMBL4558518 | GSI-NC | Ki | = | 707.95 | nM | 6.15 |
| CHEMBL4558518 | GSI-NC | Ki | = | 710.0 | nM | 6.15 |
| CHEMBL4520788 | BAY-294 | Ki | = | 870.96 | nM | 6.06 |
| CHEMBL4520788 | BAY-294 | Ki | = | 868.61 | nM | 6.06 |
| CHEMBL1800685 | PPTN | Ki | = | 884.3 | nM | 6.05 |
| CHEMBL1800685 | PPTN | Ki | = | 891.25 | nM | 6.05 |
| CHEMBL2048623 | — | Ki | = | 924.7 | nM | 6.03 |
| CHEMBL4535474 | BAY-293 | Ki | = | 936.32 | nM | 6.03 |
| CHEMBL4535474 | BAY-293 | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL2048623 | — | Ki | = | 933.25 | nM | 6.03 |
| CHEMBL4536197 | A-486 | Ki | = | 1096.48 | nM | 5.96 |
| CHEMBL4536197 | A-486 | Ki | = | 1136.58 | nM | 5.94 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 1905.46 | nM | 5.72 |
| CHEMBL4576555 | T3-CLK-N | Ki | = | 2249.15 | nM | 5.65 |
| CHEMBL3480577 | UCSF924 | Ki | = | 3162.28 | nM | 5.50 |
| CHEMBL3480577 | UCSF924 | Ki | = | 3193.33 | nM | 5.50 |
| CHEMBL5092747 | — | Ki | = | 3630.78 | nM | 5.44 |
| CHEMBL5092747 | — | Ki | = | 3603.3 | nM | 5.44 |
| CHEMBL5087167 | — | Ki | = | 8709.64 | nM | 5.06 |
| CHEMBL5087167 | — | Ki | = | 8625.81 | nM | 5.06 |
| CHEMBL4551344 | A-1210227 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4551344 | A-1210227 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4647642 | BAY-173 | Inhibition | = | 2.75 | % | - |
| CHEMBL4063249 | TP-021n | Inhibition | = | 3.81 | % | - |
| CHEMBL4075278 | — | Inhibition | = | 35.44 | % | - |
| CHEMBL4648362 | GSK789 | Inhibition | = | 9.01 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | 3.31 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | 81.79 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | -4.81 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | 8.38 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | 4.11 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | 39.01 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 28.15 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | 4.97 | % | - |
| CHEMBL3589752 | IPP/CNRS-A017 | Inhibition | = | -7.08 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | -7.39 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | -12.76 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | 32.96 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | 3.89 | % | - |
| CHEMBL4530740 | BI 1950 | Inhibition | = | -3.54 | % | - |
| CHEMBL4577237 | BI 9446 | Inhibition | = | 9.55 | % | - |
| CHEMBL3137331 | DEFACTINIB | Inhibition | = | 11.35 | % | - |
| CHEMBL4635540 | GSK791 | Inhibition | = | 15.52 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | 2.48 | % | - |