Assay Detail
Functional
CHEMBL1107400
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Antagonist activity at human GPR17 R255I mutant expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321-N1 |
| Confidence | 0 — Uncurated / Unknown |
| Curated By | Autocuration |
Publication
Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 2 | 8.23 | 9.82 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL1097279 | CANGRELOR TETRASODIUM | 4.0 | 1 | 9.82 |
| CHEMBL1096400 | — | — | 1 | 6.64 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL1097279 | CANGRELOR TETRASODIUM | IC50 | = | 0.15 | nM | 9.82 |
| CHEMBL1096400 | — | IC50 | = | 227.0 | nM | 6.64 |