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Assay Detail

CHEMBL1065680

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Functional
Antagonist activity at human P2Y2 receptor expressed in astrocytoma cells assessed as inhibition of intracellular calcium mobilization
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Development of potent and selective inhibitors of ecto-5'-nucleotidase based on an anthraquinone scaffold.
Baqi Y, Lee SY, Iqbal J, Ripphausen P, Lehr A, Scheiff AB, Zimmermann H, Bajorath J, Müller CE.
J Med Chem (2010) 53 : 2076 -2086
PubMed 20146483 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.12 5.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223344 RB 2 1 5.73
CHEMBL496030 1 5.33
CHEMBL498423 1 5.18
CHEMBL608559 1 5.00
CHEMBL256057 ACID BLUE 25 1 4.96
CHEMBL590956 1 4.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223344 RB 2 IC50 = 1850.0 nM 5.73
CHEMBL496030 IC50 = 4630.0 nM 5.33
CHEMBL498423 IC50 = 6670.0 nM 5.18
CHEMBL608559 IC50 = 10000.0 nM 5.00
CHEMBL256057 ACID BLUE 25 IC50 = 11000.0 nM 4.96
CHEMBL590956 IC50 = 29900.0 nM 4.52