Assay Detail
Functional
CHEMBL5385281
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Antagonist activity at human P2Y6R expressed in HEK293 cells assessed as inhibition of UDP-induced IP3 production preincubated for 0.5 hrs followed by UDP stimulation and measured after 12 hrs by ELISA analysis
37
Total Activities
37
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Homo sapiens |
| Cell Type | HEK293 |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Discovery of Selective P2Y<sub>6</sub>R Antagonists with High Affinity and <i>In Vivo</i> Efficacy for Inflammatory Disease Therapy.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 37 | 7.12 | 8.23 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL5431885 | — | — | 1 | 8.23 |
| CHEMBL5436258 | — | — | 1 | 7.90 |
| CHEMBL5439747 | — | — | 1 | 7.82 |
| CHEMBL1321988 | — | — | 1 | 7.56 |
| CHEMBL5417339 | — | — | 1 | 7.51 |
| CHEMBL5418022 | — | — | 1 | 7.37 |
| CHEMBL5406215 | — | — | 1 | 7.34 |
| CHEMBL5437857 | — | — | 1 | 7.31 |
| CHEMBL5407949 | — | — | 1 | 7.19 |
| CHEMBL5410330 | — | — | 1 | 7.14 |
| CHEMBL5410858 | — | — | 1 | 7.11 |
| CHEMBL5411070 | — | — | 1 | 7.06 |
| CHEMBL5414535 | — | — | 1 | 7.03 |
| CHEMBL5421135 | — | — | 1 | 7.03 |
| CHEMBL1443161 | — | — | 1 | 6.90 |
| CHEMBL5395633 | — | — | 1 | 6.89 |
| CHEMBL5400464 | — | — | 1 | 6.80 |
| CHEMBL5425616 | — | — | 1 | 6.76 |
| CHEMBL5409374 | — | — | 1 | 6.69 |
| CHEMBL5439739 | — | — | 1 | 6.67 |
| CHEMBL5394242 | — | — | 1 | 6.59 |
| CHEMBL5432130 | — | — | 1 | 6.50 |
| CHEMBL5394118 | — | — | 1 | 6.34 |
| CHEMBL5411408 | — | — | 1 | - |
| CHEMBL5408737 | — | — | 1 | - |
| CHEMBL5430019 | — | — | 1 | - |
| CHEMBL5401590 | — | — | 1 | - |
| CHEMBL5420335 | — | — | 1 | - |
| CHEMBL5399277 | — | — | 1 | - |
| CHEMBL5425675 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL5431885 | — | IC50 | = | 5.914 | nM | 8.23 |
| CHEMBL5436258 | — | IC50 | = | 12.59 | nM | 7.90 |
| CHEMBL5439747 | — | IC50 | = | 15.24 | nM | 7.82 |
| CHEMBL1321988 | — | IC50 | = | 27.47 | nM | 7.56 |
| CHEMBL5417339 | — | IC50 | = | 30.81 | nM | 7.51 |
| CHEMBL5418022 | — | IC50 | = | 42.5 | nM | 7.37 |
| CHEMBL5406215 | — | IC50 | = | 45.72 | nM | 7.34 |
| CHEMBL5437857 | — | IC50 | = | 49.21 | nM | 7.31 |
| CHEMBL5407949 | — | IC50 | = | 64.13 | nM | 7.19 |
| CHEMBL5410330 | — | IC50 | = | 72.86 | nM | 7.14 |
| CHEMBL5410858 | — | IC50 | = | 77.85 | nM | 7.11 |
| CHEMBL5411070 | — | IC50 | = | 87.84 | nM | 7.06 |
| CHEMBL5414535 | — | IC50 | = | 94.21 | nM | 7.03 |
| CHEMBL5421135 | — | IC50 | = | 93.46 | nM | 7.03 |
| CHEMBL1443161 | — | IC50 | = | 126.0 | nM | 6.90 |
| CHEMBL5395633 | — | IC50 | = | 128.13 | nM | 6.89 |
| CHEMBL5400464 | — | IC50 | = | 159.24 | nM | 6.80 |
| CHEMBL5425616 | — | IC50 | = | 172.58 | nM | 6.76 |
| CHEMBL5409374 | — | IC50 | = | 202.22 | nM | 6.69 |
| CHEMBL5439739 | — | IC50 | = | 216.22 | nM | 6.67 |
| CHEMBL5394242 | — | IC50 | = | 256.24 | nM | 6.59 |
| CHEMBL5432130 | — | IC50 | = | 314.04 | nM | 6.50 |
| CHEMBL5394118 | — | IC50 | = | 456.73 | nM | 6.34 |
| CHEMBL5437881 | — | IC50 | - | — | - | |
| CHEMBL5421681 | — | IC50 | - | — | - | |
| CHEMBL5395495 | — | IC50 | - | — | - | |
| CHEMBL5404034 | — | IC50 | - | — | - | |
| CHEMBL5396901 | — | IC50 | - | — | - | |
| CHEMBL5429175 | — | IC50 | - | — | - | |
| CHEMBL5438702 | — | IC50 | - | — | - | |
| CHEMBL5425675 | — | IC50 | - | — | - | |
| CHEMBL5399277 | — | IC50 | - | — | - | |
| CHEMBL5420335 | — | IC50 | - | — | - | |
| CHEMBL5401590 | — | IC50 | - | — | - | |
| CHEMBL5430019 | — | IC50 | - | — | - | |
| CHEMBL5408737 | — | IC50 | - | — | - | |
| CHEMBL5411408 | — | IC50 | - | — | - |