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Assay Detail

CHEMBL929976

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

Functional
Antagonist activity at human recombinant P2Y2 receptor in 1321N1 cells assessed as inhibition of UTP-induced calcium mobilization
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Combinatorial synthesis of anilinoanthraquinone derivatives and evaluation as non-nucleotide-derived P2Y2 receptor antagonists.
Weyler S, Baqi Y, Hillmann P, Kaulich M, Hunder AM, Müller IA, Müller CE.
Bioorg Med Chem Lett (2008) 18 : 223 -227
PubMed 18006312 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 5.09 5.73

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223344 RB 2 1 5.73
CHEMBL445413 1 5.52
CHEMBL401859 1 5.41
CHEMBL271673 1 5.28
CHEMBL256688 1 5.26
CHEMBL256057 ACID BLUE 25 1 5.25
CHEMBL271688 1 5.24
CHEMBL404659 1 5.12
CHEMBL402239 1 5.10
CHEMBL402238 1 5.03
CHEMBL257495 1 5.01
CHEMBL401735 1 4.94
CHEMBL271881 1 4.94
CHEMBL403051 1 4.82
CHEMBL256864 1 4.79
CHEMBL404450 1 4.60
CHEMBL256689 1 4.52
CHEMBL271672 1 -
CHEMBL271689 1 -
CHEMBL270415 BROMAMINIC ACID 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223344 RB 2 IC50 = 1850.0 nM 5.73
CHEMBL445413 IC50 = 3040.0 nM 5.52
CHEMBL401859 IC50 = 3930.0 nM 5.41
CHEMBL271673 IC50 = 5310.0 nM 5.28
CHEMBL256688 IC50 = 5430.0 nM 5.26
CHEMBL256057 ACID BLUE 25 IC50 = 5610.0 nM 5.25
CHEMBL271688 IC50 = 5810.0 nM 5.24
CHEMBL404659 IC50 = 7520.0 nM 5.12
CHEMBL402239 IC50 = 7950.0 nM 5.10
CHEMBL402238 IC50 = 9260.0 nM 5.03
CHEMBL257495 IC50 = 9820.0 nM 5.01
CHEMBL401735 IC50 = 11500.0 nM 4.94
CHEMBL271881 IC50 = 11500.0 nM 4.94
CHEMBL403051 IC50 = 15000.0 nM 4.82
CHEMBL256864 IC50 = 16200.0 nM 4.79
CHEMBL404450 IC50 = 24900.0 nM 4.60
CHEMBL256689 IC50 = 30300.0 nM 4.52
CHEMBL271672 IC50 > 30000.0 nM -
CHEMBL271689 IC50 - -
CHEMBL270415 BROMAMINIC ACID IC50 - -