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Assay Detail

CHEMBL5586086

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of (E)-N6-(5-(bis(4-chlorophenyl)methyl)thiazol-2-yl)-N2-(6-(2-(4-(2-(5,5-difluoro-7-(thiophen-2-yl)-5H-4lambda4,5lambda4-dipyrrolo[1,2-c:2',1'-f][1,3,2]diazaborinin-3-yl)vinyl)phenoxy)acetamido)hexanoyl)-L-lysine from NLuc fused P2Y2R (unknown origin) extracted from 1321N1 cell membrane incubated for 1 hr by NanoBRET assay
4
Total Activities
4
Compounds Tested
1
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

Target

P2Y purinoceptor 2 (CHEMBL4398)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, Synthesis, and Evaluation of a New Chemotype Fluorescent Ligand for the P2Y<sub>2</sub> Receptor.
Knight R, Kilpatrick LE, Hill SJ, Stocks MJ.
ACS Med Chem Lett (2024) 15 : 1127 -1135
PubMed 39015271 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 4.68 5.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4128059 1 5.04
CHEMBL5596941 1 4.86
CHEMBL4082045 1 4.14
CHEMBL5597711 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4128059 Ki = 9120.11 nM 5.04
CHEMBL5596941 Ki = 13803.84 nM 4.86
CHEMBL4082045 Ki = 72443.6 nM 4.14
CHEMBL5597711 Ki = 120226.44 nM -