Assay Detail
Functional
CHEMBL4818330
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2Y6 receptor expressed in human 1321N1 cells assessed as inhibition of UDP-induced intracellular calcium mobilization by fluorescence based analysis
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | 1321N1 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Structure activity relationship of 3-nitro-2-(trifluoromethyl)-2H-chromene derivatives as P2Y<sub>6</sub> receptor antagonists.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 26 | 5.29 | 6.22 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4877977 | — | — | 1 | 6.22 |
| CHEMBL4851349 | — | — | 1 | 6.11 |
| CHEMBL4857492 | — | — | 1 | 5.96 |
| CHEMBL4856060 | — | — | 1 | 5.92 |
| CHEMBL4871107 | — | — | 1 | 5.88 |
| CHEMBL4876210 | — | — | 1 | 5.54 |
| CHEMBL4854398 | — | — | 1 | 5.46 |
| CHEMBL4875858 | — | — | 1 | 5.40 |
| CHEMBL4845850 | — | — | 1 | 5.33 |
| CHEMBL4864185 | — | — | 1 | 5.31 |
| CHEMBL4858554 | — | — | 1 | 5.28 |
| CHEMBL4854854 | — | — | 1 | 5.27 |
| CHEMBL4852231 | — | — | 1 | 5.23 |
| CHEMBL4878016 | — | — | 1 | 5.20 |
| CHEMBL4872572 | — | — | 1 | 5.18 |
| CHEMBL4873868 | — | — | 1 | 5.17 |
| CHEMBL4870366 | — | — | 1 | 5.15 |
| CHEMBL4852131 | — | — | 1 | 5.14 |
| CHEMBL4848838 | — | — | 1 | 5.12 |
| CHEMBL4873092 | — | — | 1 | 4.97 |
| CHEMBL4862488 | — | — | 1 | 4.46 |
| CHEMBL4861225 | — | — | 1 | 4.16 |
| CHEMBL4878817 | — | — | 1 | 4.11 |
| CHEMBL4875249 | — | — | 1 | - |
| CHEMBL4866371 | — | — | 1 | - |
| CHEMBL4859169 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4877977 | — | IC50 | = | 604.0 | nM | 6.22 |
| CHEMBL4851349 | — | IC50 | = | 785.0 | nM | 6.11 |
| CHEMBL4857492 | — | IC50 | = | 1090.0 | nM | 5.96 |
| CHEMBL4856060 | — | IC50 | = | 1200.0 | nM | 5.92 |
| CHEMBL4871107 | — | IC50 | = | 1330.0 | nM | 5.88 |
| CHEMBL4876210 | — | IC50 | = | 2910.0 | nM | 5.54 |
| CHEMBL4854398 | — | IC50 | = | 3490.0 | nM | 5.46 |
| CHEMBL4875858 | — | IC50 | = | 4000.0 | nM | 5.40 |
| CHEMBL4845850 | — | IC50 | = | 4650.0 | nM | 5.33 |
| CHEMBL4864185 | — | IC50 | = | 4870.0 | nM | 5.31 |
| CHEMBL4858554 | — | IC50 | = | 5230.0 | nM | 5.28 |
| CHEMBL4854854 | — | IC50 | = | 5330.0 | nM | 5.27 |
| CHEMBL4852231 | — | IC50 | = | 5900.0 | nM | 5.23 |
| CHEMBL4878016 | — | IC50 | = | 6330.0 | nM | 5.20 |
| CHEMBL4872572 | — | IC50 | = | 6590.0 | nM | 5.18 |
| CHEMBL4873868 | — | IC50 | = | 6840.0 | nM | 5.17 |
| CHEMBL4870366 | — | IC50 | = | 7130.0 | nM | 5.15 |
| CHEMBL4852131 | — | IC50 | = | 7310.0 | nM | 5.14 |
| CHEMBL4848838 | — | IC50 | = | 7670.0 | nM | 5.12 |
| CHEMBL4873092 | — | IC50 | = | 10600.0 | nM | 4.97 |
| CHEMBL4862488 | — | IC50 | = | 34600.0 | nM | 4.46 |
| CHEMBL4861225 | — | IC50 | = | 69100.0 | nM | 4.16 |
| CHEMBL4878817 | — | IC50 | = | 77900.0 | nM | 4.11 |
| CHEMBL4875249 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4866371 | — | IC50 | > | 100000.0 | nM | - |
| CHEMBL4859169 | — | IC50 | = | 121000.0 | nM | - |