Assay Detail
Binding
CHEMBL4880045
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GPCRScan assay: inhibition of GABAA
170
Total Activities
164
Compounds Tested
2
Activity Types
12
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus |
| Confidence | 5 — Multiple protein complex / RNA |
| Curated By | Autocuration |
Target
GABA-A receptor; anion channel (CHEMBL1907607) ↗| Type | PROTEIN COMPLEX GROUP |
| Organism | Rattus norvegicus |
Publication
SGC PDSP GPCRScan assays
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 164 | - | - |
| Ki | 6 | 5.62 | 5.81 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | brain tissue |
| PMID | PMID | - | — | 2548571/8997506 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 9.50 – 25.0 |
| Radioligand Kd | Radioligand Kd | 7.7 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-Muscimol |
| Radioligand pKd | Radioligand pKd | 8.11 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.06 | — | — |
| Reference ligand | Reference ligand | - | — | GABA |
| Reference ligand Ki | Reference ligand Ki | 137.5 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 6.86 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.08 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4639128 | GSK778 | — | 3 | 5.81 |
| CHEMBL5027912 | — | — | 3 | 5.74 |
| CHEMBL3480577 | UCSF924 | — | 3 | 5.00 |
| CHEMBL3617968 | BAY-678 | — | 1 | - |
| CHEMBL4084419 | — | — | 1 | - |
| CHEMBL4096813 | — | — | 1 | - |
| CHEMBL4526351 | BAY-309 | — | 1 | - |
| CHEMBL3907057 | BAY-826 | — | 1 | - |
| CHEMBL4630643 | BAY-448 | — | 1 | - |
| CHEMBL4630644 | BAY-386 | — | 1 | - |
| CHEMBL4455582 | BAY-693 | — | 1 | - |
| CHEMBL4445670 | BAY-885 | — | 1 | - |
| CHEMBL4552180 | BAY-588 | — | 1 | - |
| CHEMBL4448899 | BAY-876 | — | 1 | - |
| CHEMBL4564312 | BAY-786 | — | 1 | - |
| 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 | - |
| 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 |
|---|---|---|---|---|---|---|
| CHEMBL4639128 | GSK778 | Ki | = | 1548.82 | nM | 5.81 |
| CHEMBL4639128 | GSK778 | Ki | = | 1595.89 | nM | 5.80 |
| CHEMBL5027912 | — | Ki | = | 1819.7 | nM | 5.74 |
| CHEMBL5027912 | — | Ki | = | 1822.22 | nM | 5.74 |
| CHEMBL3480577 | UCSF924 | Ki | = | 10000.0 | nM | 5.00 |
| CHEMBL4514203 | BAY-390 | Inhibition | = | 19.69 | % | - |
| CHEMBL4802042 | JNJ-54119936 | Inhibition | = | -28.84 | % | - |
| CHEMBL4555711 | BAY-9897 | Inhibition | = | -15.08 | % | - |
| CHEMBL4648362 | GSK789 | Inhibition | = | 14.77 | % | - |
| CHEMBL4635540 | GSK791 | Inhibition | = | 14.94 | % | - |
| CHEMBL4636881 | GSK046 | Inhibition | = | 15.28 | % | - |
| CHEMBL4635134 | GSK620 | Inhibition | = | 8.55 | % | - |
| CHEMBL4638406 | BAY-3153 | Inhibition | = | 18.57 | % | - |
| CHEMBL4647642 | BAY-173 | Inhibition | = | 20.02 | % | - |
| CHEMBL4075278 | — | Inhibition | = | 12.7 | % | - |
| CHEMBL4063249 | TP-021n | Inhibition | = | 15.54 | % | - |
| CHEMBL4516611 | BTZO-1 | Inhibition | = | 6.232 | % | - |
| CHEMBL4561806 | BTZO-4 | Inhibition | = | -11.46 | % | - |
| CHEMBL4282264 | A-485 | Inhibition | = | 8.97 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | 9.54 | % | - |
| CHEMBL4798829 | — | Inhibition | = | 7.9 | % | - |
| CHEMBL4545807 | BAY-070 | Inhibition | = | -11.95 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | 52.72 | % | - |
| CHEMBL4802046 | MSC-0516 | Inhibition | = | 19.36 | % | - |
| CHEMBL4748908 | TP-040n | Inhibition | = | 34.64 | % | - |
| CHEMBL4802043 | MSC-4381 | Inhibition | = | -15.68 | % | - |
| CHEMBL4778870 | TP-040 | Inhibition | = | 2.33 | % | - |
| CHEMBL4537673 | BAY-985 | Inhibition | = | 5.57 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | 4.07 | % | - |
| CHEMBL4543737 | Al11 | Inhibition | = | -14.29 | % | - |
| CHEMBL3480577 | UCSF924 | Inhibition | = | 1.68 | % | - |
| CHEMBL3480577 | UCSF924 | Ki | = | 1000000000.0 | nM | - |
| CHEMBL4228713 | A-1211212 | Inhibition | = | 18.99 | % | - |
| CHEMBL4551344 | A-1210227 | Inhibition | = | 14.49 | % | - |
| CHEMBL3342332 | A-1155463 | Inhibition | = | 11.34 | % | - |
| CHEMBL3589752 | IPP/CNRS-A017 | Inhibition | = | 17.28 | % | - |
| CHEMBL3590047 | IPP/CNRS-A019 | Inhibition | = | -19.69 | % | - |
| CHEMBL4458424 | BAY-899 | Inhibition | = | 19.37 | % | - |
| CHEMBL4592872 | BAY-897 | Inhibition | = | 26.88 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 8.16 | % | - |
| CHEMBL4538591 | BAY-440 | Inhibition | = | 13.96 | % | - |
| CHEMBL4580220 | BAY-3827 | Inhibition | = | -7.98 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | -0.8 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | 11.66 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 37.31 | % | - |
| CHEMBL4534980 | (S)-ZINC-3573 | Inhibition | = | -12.49 | % | - |
| CHEMBL4460070 | ZINC32547799 | Inhibition | = | -14.93 | % | - |
| CHEMBL4088216 | TP-030-1 | Inhibition | = | 10.49 | % | - |
| CHEMBL4549667 | TP-030-2 | Inhibition | = | 8.81 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | 11.27 | % | - |