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Assay Detail

CHEMBL4121223

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

Binding
Binding affinity to recombinant human N-terminal NLuc-tagged P2Y2R expressed in human 1321N1 cells incubated for 1 hr in presence of AR-C118925 by furimazine-based NanoBRET assay
13
Total Activities
13
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
Kd 13 5.97 7.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4127889 1 7.05
CHEMBL4128532 1 6.89
CHEMBL4128024 1 6.53
CHEMBL4126655 1 6.32
CHEMBL4125853 1 6.12
CHEMBL4125987 1 6.07
CHEMBL4125833 1 6.05
CHEMBL4127230 1 5.78
CHEMBL4128318 1 5.67
CHEMBL4126826 1 5.56
CHEMBL4129129 1 5.38
CHEMBL4129299 1 5.29
CHEMBL4129692 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4127889 Kd = 89.13 nM 7.05
CHEMBL4128532 Kd = 128.82 nM 6.89
CHEMBL4128024 Kd = 295.12 nM 6.53
CHEMBL4126655 Kd = 478.63 nM 6.32
CHEMBL4125853 Kd = 758.58 nM 6.12
CHEMBL4125987 Kd = 851.14 nM 6.07
CHEMBL4125833 Kd = 891.25 nM 6.05
CHEMBL4127230 Kd = 1659.59 nM 5.78
CHEMBL4128318 Kd = 2137.96 nM 5.67
CHEMBL4126826 Kd = 2754.23 nM 5.56
CHEMBL4129129 Kd = 4168.69 nM 5.38
CHEMBL4129299 Kd = 5128.61 nM 5.29
CHEMBL4129692 Kd = 12302.69 nM 4.91