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Assay Detail

CHEMBL4121224

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

Binding
Displacement of N-(2-(3-((7-Chloro-4-(1-methyl-2-oxo-4-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)-4H-benzo[5,6]cyclohepta[1,2-d]thiazol-2-yl)-amino)propanamido)ethyl)-6-(3-(5,5-difluoro-7,9-dimethyl-5H-4-lamba4,5-lambda4-dipyrrolo[1,2-c:2,1-f ][1,3,2]diazaborinin-3-yl)-propanamido)hexanamide from recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr by furimazine-based NanoBRET assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and Evaluation of the First Fluorescent Antagonists of the Human P2Y2 Receptor Based on AR-C118925.
Conroy S, Kindon ND, Glenn J, Stoddart LA, Lewis RJ, Hill SJ, Kellam B, Stocks MJ.
J Med Chem (2018) 61 : 3089 -3113
PubMed 29558126 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 7.45 7.45

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4082045 1 7.45

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4082045 Ki = 35.48 nM 7.45