Assay Detail
Binding
CHEMBL4880064
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GPCRScan assay: inhibition of GABA/PBR
253
Total Activities
181
Compounds Tested
2
Activity Types
11
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Rattus sp. |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
SGC PDSP GPCRScan assays
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Inhibition | 181 | - | - |
| Ki | 72 | 6.28 | 8.03 |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | brain tissue |
| PMID | PMID | - | — | 1317581/6087829 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 0.3 – 2.0 |
| Radioligand Kd | Radioligand Kd | 1.0 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H]-PK11195 |
| Radioligand pKd | Radioligand pKd | 9.0 | — | — |
| Reference ligand | Reference ligand | - | — | Ro5-4864 |
| Reference ligand Ki | Reference ligand Ki | 14.97 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 7.82 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.02 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4526351 | BAY-309 | — | 3 | 8.03 |
| CHEMBL4093612 | A-1596586 | — | 3 | 7.71 |
| CHEMBL4630642 | BAY-974 | — | 3 | 7.69 |
| CHEMBL4795065 | Borussertib | — | 3 | 7.24 |
| CHEMBL4551635 | BAY-069 | — | 3 | 7.13 |
| CHEMBL204232 | NAPHTHYRIDINONE | — | 3 | 7.09 |
| CHEMBL3907057 | BAY-826 | — | 3 | 6.68 |
| CHEMBL4066040 | A-1596584 | — | 3 | 6.66 |
| CHEMBL4580220 | BAY-3827 | — | 3 | 6.66 |
| CHEMBL4516843 | BAY-207 | — | 3 | 6.62 |
| CHEMBL5092747 | — | — | 3 | 6.51 |
| CHEMBL5092058 | — | — | 5 | 6.47 |
| CHEMBL4549667 | TP-030-2 | — | 3 | 6.46 |
| CHEMBL4088216 | TP-030-1 | — | 3 | 6.43 |
| CHEMBL5094181 | — | — | 3 | 6.30 |
| CHEMBL4802046 | MSC-0516 | — | 3 | 6.14 |
| CHEMBL4530401 | MRL-SYKi-NC | — | 3 | 6.11 |
| CHEMBL3342332 | A-1155463 | — | 3 | 6.10 |
| CHEMBL4445645 | — | — | 3 | 6.01 |
| CHEMBL3577885 | PF-05105679 | 1.0 | 3 | 5.99 |
| CHEMBL4282264 | A-485 | — | 3 | 5.96 |
| CHEMBL561132 | MK-7246 | 1.0 | 3 | 5.95 |
| CHEMBL1651534 | REDAFAMDASTAT | 2.0 | 3 | 5.94 |
| CHEMBL4518706 | PF-00911705 | — | 3 | 5.83 |
| CHEMBL5306285 | — | — | 3 | 5.81 |
| CHEMBL4638406 | BAY-3153 | — | 3 | 5.74 |
| CHEMBL4522773 | BAY-827 | — | 3 | 5.67 |
| CHEMBL4165749 | BI 2545 | — | 3 | 5.62 |
| CHEMBL4536197 | A-486 | — | 3 | 5.60 |
| CHEMBL4522930 | BI-605906 | — | 3 | 5.59 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4526351 | BAY-309 | Ki | = | 9.333 | nM | 8.03 |
| CHEMBL4526351 | BAY-309 | Ki | = | 10.9 | nM | 7.96 |
| CHEMBL4093612 | A-1596586 | Ki | = | 19.59 | nM | 7.71 |
| CHEMBL4093612 | A-1596586 | Ki | = | 19.5 | nM | 7.71 |
| CHEMBL4630642 | BAY-974 | Ki | = | 20.42 | nM | 7.69 |
| CHEMBL4630642 | BAY-974 | Ki | = | 20.99 | nM | 7.68 |
| CHEMBL4795065 | Borussertib | Ki | = | 57.32 | nM | 7.24 |
| CHEMBL4795065 | Borussertib | Ki | = | 57.54 | nM | 7.24 |
| CHEMBL4551635 | BAY-069 | Ki | = | 73.28 | nM | 7.13 |
| CHEMBL4551635 | BAY-069 | Ki | = | 74.19 | nM | 7.13 |
| CHEMBL204232 | NAPHTHYRIDINONE | Ki | = | 82.0 | nM | 7.09 |
| CHEMBL204232 | NAPHTHYRIDINONE | Ki | = | 81.28 | nM | 7.09 |
| CHEMBL3907057 | BAY-826 | Ki | = | 208.93 | nM | 6.68 |
| CHEMBL4066040 | A-1596584 | Ki | = | 217.72 | nM | 6.66 |
| CHEMBL4066040 | A-1596584 | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL4580220 | BAY-3827 | Ki | = | 218.78 | nM | 6.66 |
| CHEMBL3907057 | BAY-826 | Ki | = | 217.26 | nM | 6.66 |
| CHEMBL4580220 | BAY-3827 | Ki | = | 222.4 | nM | 6.65 |
| CHEMBL4516843 | BAY-207 | Ki | = | 239.88 | nM | 6.62 |
| CHEMBL4516843 | BAY-207 | Ki | = | 250.13 | nM | 6.60 |
| CHEMBL5092747 | — | Ki | = | 309.03 | nM | 6.51 |
| CHEMBL5092747 | — | Ki | = | 306.41 | nM | 6.51 |
| CHEMBL5092058 | — | Ki | = | 338.84 | nM | 6.47 |
| CHEMBL5092058 | — | Ki | = | 336.05 | nM | 6.47 |
| CHEMBL5092058 | — | Ki | = | 338.84 | nM | 6.47 |
| CHEMBL5092058 | — | Ki | = | 336.05 | nM | 6.47 |
| CHEMBL4549667 | TP-030-2 | Ki | = | 342.77 | nM | 6.46 |
| CHEMBL4549667 | TP-030-2 | Ki | = | 346.58 | nM | 6.46 |
| CHEMBL4088216 | TP-030-1 | Ki | = | 374.92 | nM | 6.43 |
| CHEMBL4088216 | TP-030-1 | Ki | = | 375.84 | nM | 6.42 |
| CHEMBL5094181 | — | Ki | = | 497.62 | nM | 6.30 |
| CHEMBL5094181 | — | Ki | = | 501.19 | nM | 6.30 |
| CHEMBL4802046 | MSC-0516 | Ki | = | 724.44 | nM | 6.14 |
| CHEMBL4802046 | MSC-0516 | Ki | = | 733.68 | nM | 6.13 |
| CHEMBL4530401 | MRL-SYKi-NC | Ki | = | 776.25 | nM | 6.11 |
| CHEMBL4530401 | MRL-SYKi-NC | Ki | = | 774.0 | nM | 6.11 |
| CHEMBL3342332 | A-1155463 | Ki | = | 794.33 | nM | 6.10 |
| CHEMBL3342332 | A-1155463 | Ki | = | 793.96 | nM | 6.10 |
| CHEMBL4445645 | — | Ki | = | 977.24 | nM | 6.01 |
| CHEMBL3577885 | PF-05105679 | Ki | = | 1023.29 | nM | 5.99 |
| CHEMBL3577885 | PF-05105679 | Ki | = | 1022.12 | nM | 5.99 |
| CHEMBL4282264 | A-485 | Ki | = | 1096.48 | nM | 5.96 |
| CHEMBL4282264 | A-485 | Ki | = | 1107.62 | nM | 5.96 |
| CHEMBL4445645 | — | Ki | = | 1113.88 | nM | 5.95 |
| CHEMBL561132 | MK-7246 | Ki | = | 1122.02 | nM | 5.95 |
| CHEMBL561132 | MK-7246 | Ki | = | 1115.0 | nM | 5.95 |
| CHEMBL1651534 | REDAFAMDASTAT | Ki | = | 1148.15 | nM | 5.94 |
| CHEMBL1651534 | REDAFAMDASTAT | Ki | = | 1140.08 | nM | 5.94 |
| CHEMBL4518706 | PF-00911705 | Ki | = | 1479.11 | nM | 5.83 |
| CHEMBL4518706 | PF-00911705 | Ki | = | 1479.11 | nM | 5.83 |