Assay Detail
Binding
CHEMBL4121228
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of (E)-2-((5-(7-Chloro-2-((3-((2-(6-(3-(5,5-difluoro-7,9-dimethyl-5H-5-lambda4,6-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamido)ethyl)amino)-3-oxopropyl)amino)-4Hbenzo[5,6]cyclohepta[1,2-d]thiazol-4-yl)-2-oxo-4-thioxo-3,4-dihydropyrimidin-1(2H)-yl)methyl)-N-(1H-tetrazol-5-yl)thiazole-4-carboxamide from human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
18
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 9 | 6.41 | 7.38 |
| Inhibition | 9 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4082045 | — | — | 2 | 7.38 |
| CHEMBL4086462 | — | — | 2 | 7.08 |
| CHEMBL4128126 | — | — | 2 | 6.89 |
| CHEMBL4128024 | — | — | 2 | 6.84 |
| CHEMBL4128208 | — | — | 2 | 6.56 |
| CHEMBL4128318 | — | — | 2 | 6.40 |
| CHEMBL4127983 | — | — | 2 | 5.81 |
| CHEMBL220200 | — | — | 2 | 5.46 |
| CHEMBL4128059 | — | — | 2 | 5.28 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4082045 | — | Ki | = | 41.69 | nM | 7.38 |
| CHEMBL4086462 | — | Ki | = | 83.18 | nM | 7.08 |
| CHEMBL4128126 | — | Ki | = | 128.82 | nM | 6.89 |
| CHEMBL4128024 | — | Ki | = | 144.54 | nM | 6.84 |
| CHEMBL4128208 | — | Ki | = | 275.42 | nM | 6.56 |
| CHEMBL4128318 | — | Ki | = | 398.11 | nM | 6.40 |
| CHEMBL4127983 | — | Ki | = | 1548.82 | nM | 5.81 |
| CHEMBL220200 | — | Ki | = | 3467.37 | nM | 5.46 |
| CHEMBL4128059 | — | Ki | = | 5248.07 | nM | 5.28 |
| CHEMBL4082045 | — | Inhibition | - | % | - | |
| CHEMBL4128126 | — | Inhibition | - | % | - | |
| CHEMBL4127983 | — | Inhibition | - | % | - | |
| CHEMBL4128059 | — | Inhibition | - | % | - | |
| CHEMBL4128208 | — | Inhibition | - | % | - | |
| CHEMBL4128318 | — | Inhibition | - | % | - | |
| CHEMBL220200 | — | Inhibition | - | % | - | |
| CHEMBL4128024 | — | Inhibition | - | % | - | |
| CHEMBL4086462 | — | Inhibition | - | % | - |