Assay Detail
Binding
CHEMBL5058651
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GPCRScan assay: inhibition of A1
3
Total Activities
1
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 |
|---|---|---|---|
| Ki | 2 | 5.88 | 5.96 |
| Inhibition | 1 | - | - |
Assay Parameters
| Parameter | Type | Value | Units | Text |
|---|---|---|---|---|
| Parental cells | Parental cells | - | — | HEKT |
| PMID | PMID | - | — | 9827575/8300561 |
| Protein length | Protein length | - | — | full-length |
| Radioligand conc. used [nM] | Radioligand conc. used [nM] | - | — | 5.0 |
| Radioligand Kd | Radioligand Kd | 4.95 | nM | — |
| Radioligand name | Radioligand name | - | — | [3H] DPCPX |
| Radioligand pKd | Radioligand pKd | 8.31 | — | — |
| Radioligand pKd ± SEM | Radioligand pKd ± SEM | 0.16 | — | — |
| Reference ligand | Reference ligand | - | — | CGS15943 |
| Reference ligand Ki | Reference ligand Ki | 13.3 | nM | — |
| Reference ligand pKi | Reference ligand pKi | 7.88 | — | — |
| Reference ligand pKi ± SEM | Reference ligand pKi ± SEM | 0.26 | — | — |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4445645 | — | — | 3 | 5.96 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4445645 | — | Ki | = | 1096.48 | nM | 5.96 |
| CHEMBL4445645 | — | Ki | = | 1630.55 | nM | 5.79 |
| CHEMBL4445645 | — | Inhibition | = | 93.08 | % | - |