Assay Detail
Binding
CHEMBL4880063
Review assay metadata, readout intent, target linkage, and publication context from the same page.
GPCRScan assay: inhibition of GABAA/BZP
205
Total Activities
181
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 | 181 | - | - |
| Ki | 24 | 5.84 | 6.72 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | brain tissue |
| PMID | PMID | - | — | 25191/6134627 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 0.6 – 4.0 |
| Radioligand Kd | Radioligand Kd | 1.64 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-Flunitrazepam |
| Radioligand pKd | Radioligand pKd | 8.79 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.14 | — | — |
| Reference ligand | Reference ligand | - | — | Clonazepam |
| Reference ligand Ki | Reference ligand Ki | 1.03 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 8.99 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.03 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4084419 | — | — | 3 | 6.72 |
| CHEMBL4638939 | GSK943 | — | 3 | 6.33 |
| CHEMBL4778870 | TP-040 | — | 3 | 6.30 |
| CHEMBL4516611 | BTZO-1 | — | 3 | 6.03 |
| CHEMBL4096813 | — | — | 3 | 5.82 |
| CHEMBL4578164 | MRL-CB1-NC | — | 3 | 5.78 |
| CHEMBL4639128 | GSK778 | — | 3 | 5.75 |
| CHEMBL4520293 | (R)-ZINC-3573 | — | 3 | 5.73 |
| CHEMBL4635540 | GSK791 | — | 3 | 5.60 |
| CHEMBL4543737 | Al11 | — | 3 | 5.56 |
| CHEMBL3799512 | TP-004 | — | 3 | 5.34 |
| CHEMBL4802045 | BAY-091 | — | 3 | 5.17 |
| 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 | - |
| 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 |
|---|---|---|---|---|---|---|
| CHEMBL4084419 | — | Ki | = | 190.55 | nM | 6.72 |
| CHEMBL4084419 | — | Ki | = | 224.22 | nM | 6.65 |
| CHEMBL4638939 | GSK943 | Ki | = | 473.15 | nM | 6.33 |
| CHEMBL4638939 | GSK943 | Ki | = | 473.91 | nM | 6.32 |
| CHEMBL4778870 | TP-040 | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4778870 | TP-040 | Ki | = | 511.7 | nM | 6.29 |
| CHEMBL4516611 | BTZO-1 | Ki | = | 934.0 | nM | 6.03 |
| CHEMBL4516611 | BTZO-1 | Ki | = | 1000.0 | nM | 6.00 |
| CHEMBL4096813 | — | Ki | = | 1527.0 | nM | 5.82 |
| CHEMBL4096813 | — | Ki | = | 1584.89 | nM | 5.80 |
| CHEMBL4578164 | MRL-CB1-NC | Ki | = | 1660.0 | nM | 5.78 |
| CHEMBL4578164 | MRL-CB1-NC | Ki | = | 1659.59 | nM | 5.78 |
| CHEMBL4639128 | GSK778 | Ki | = | 1778.28 | nM | 5.75 |
| CHEMBL4520293 | (R)-ZINC-3573 | Ki | = | 1862.09 | nM | 5.73 |
| CHEMBL4639128 | GSK778 | Ki | = | 1970.29 | nM | 5.71 |
| CHEMBL4520293 | (R)-ZINC-3573 | Ki | = | 1937.43 | nM | 5.71 |
| CHEMBL4635540 | GSK791 | Ki | = | 2511.89 | nM | 5.60 |
| CHEMBL4635540 | GSK791 | Ki | = | 2539.22 | nM | 5.59 |
| CHEMBL4543737 | Al11 | Ki | = | 2754.23 | nM | 5.56 |
| CHEMBL4543737 | Al11 | Ki | = | 2746.0 | nM | 5.56 |
| CHEMBL3799512 | TP-004 | Ki | = | 4538.0 | nM | 5.34 |
| CHEMBL3799512 | TP-004 | Ki | = | 4570.88 | nM | 5.34 |
| CHEMBL4802045 | BAY-091 | Ki | = | 6760.83 | nM | 5.17 |
| CHEMBL4802045 | BAY-091 | Ki | = | 6834.39 | nM | 5.17 |
| CHEMBL4545807 | BAY-070 | Inhibition | = | -6.05 | % | - |
| CHEMBL4798829 | — | Inhibition | = | 48.34 | % | - |
| CHEMBL4536197 | A-486 | Inhibition | = | 15.55 | % | - |
| CHEMBL4282264 | A-485 | Inhibition | = | 19.71 | % | - |
| CHEMBL4514203 | BAY-390 | Inhibition | = | 4.57 | % | - |
| CHEMBL4638406 | BAY-3153 | Inhibition | = | -6.17 | % | - |
| CHEMBL4551635 | BAY-069 | Inhibition | = | 16.34 | % | - |
| CHEMBL4643852 | BAY-6672 | Inhibition | = | 5.06 | % | - |
| CHEMBL4635134 | GSK620 | Inhibition | = | 28.16 | % | - |
| CHEMBL4636881 | GSK046 | Inhibition | = | 0.61 | % | - |
| CHEMBL4648362 | GSK789 | Inhibition | = | 24.74 | % | - |
| CHEMBL4647642 | BAY-173 | Inhibition | = | 0.65 | % | - |
| CHEMBL4555711 | BAY-9897 | Inhibition | = | 5.42 | % | - |
| CHEMBL4639128 | GSK778 | Inhibition | = | 91.62 | % | - |
| CHEMBL4520293 | (R)-ZINC-3573 | Inhibition | = | 54.94 | % | - |
| CHEMBL4456585 | WM-1119 | Inhibition | = | 75.65 | % | - |
| CHEMBL4637208 | GSK973 | Inhibition | = | 30.17 | % | - |
| CHEMBL4638939 | GSK943 | Inhibition | = | 74.23 | % | - |
| CHEMBL4630642 | BAY-974 | Inhibition | = | -1.23 | % | - |
| CHEMBL3589752 | IPP/CNRS-A017 | Inhibition | = | 8.426 | % | - |
| CHEMBL1800285 | MSD-M1PAM | Inhibition | = | 8.92 | % | - |
| CHEMBL2204283 | MSD-M1PAM-NC | Inhibition | = | 21.76 | % | - |
| CHEMBL3286797 | PF-04418948 | Inhibition | = | 18.7 | % | - |
| CHEMBL4580220 | BAY-3827 | Inhibition | = | -16.29 | % | - |
| CHEMBL4552554 | PF-04475866 | Inhibition | = | -5.33 | % | - |
| CHEMBL4561806 | BTZO-4 | Inhibition | = | 6.344 | % | - |