Assay Detail
Binding
CHEMBL5586080
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Displacement of 2-((5-(7-chloro-2-((3-((2-(5-(3-(5,5-difluoro-7,9-dimethyl-5H-4lambda4,5lambda4-dipyrrolo[1,2-c:2',1'-f][1,3,2]diazaborinin-3-yl)propanamido)pentanamido)ethyl)amino)-3-oxopropyl)amino)-4H-benzo[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 NLuc fused P2Y2R (unknown origin) extracted from 1321N1 cell membrane incubated for 1 hr by NanoBRET assay
11
Total Activities
10
Compounds Tested
2
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | 1321N1 |
| Subcellular | Membrane |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Design, Synthesis, and Evaluation of a New Chemotype Fluorescent Ligand for the P2Y<sub>2</sub> Receptor.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| Ki | 10 | 5.30 | 7.49 |
| Activity | 1 | - | - |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4082045 | — | — | 1 | 7.49 |
| CHEMBL5597711 | — | — | 1 | 5.61 |
| CHEMBL5596071 | — | — | 2 | 5.48 |
| CHEMBL5596941 | — | — | 1 | 5.17 |
| CHEMBL5596524 | — | — | 1 | 5.04 |
| CHEMBL5591024 | — | — | 1 | 4.87 |
| CHEMBL5598495 | — | — | 1 | 4.84 |
| CHEMBL5597487 | — | — | 1 | 4.71 |
| CHEMBL5596778 | — | — | 1 | 4.49 |
| CHEMBL5597798 | — | — | 1 | - |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4082045 | — | Ki | = | 32.36 | nM | 7.49 |
| CHEMBL5597711 | — | Ki | = | 2454.71 | nM | 5.61 |
| CHEMBL5596071 | — | Ki | = | 3311.31 | nM | 5.48 |
| CHEMBL5596941 | — | Ki | = | 6760.83 | nM | 5.17 |
| CHEMBL5596524 | — | Ki | = | 9120.11 | nM | 5.04 |
| CHEMBL5591024 | — | Ki | = | 13489.63 | nM | 4.87 |
| CHEMBL5598495 | — | Ki | = | 14454.4 | nM | 4.84 |
| CHEMBL5597487 | — | Ki | = | 19498.45 | nM | 4.71 |
| CHEMBL5596778 | — | Ki | = | 32359.37 | nM | 4.49 |
| CHEMBL5597798 | — | Ki | ~ | 1000000.0 | nM | - |
| CHEMBL5596071 | — | Activity | - | — | - |