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Assay Detail

CHEMBL4815974

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

Functional
Antagonist activity at P2Y14 (unknown origin) expressed in HEK293 cells assessed as reduction in cAMP production incubated for 30 mins by ADP-glo assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2Y purinoceptor 14 (CHEMBL4518)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis and evaluation of 3-amide-5-aryl benzoic acid derivatives as novel P2Y<sub>14</sub>R antagonists with potential high efficiency against acute gouty arthritis.
Lu R, Wang Y, Liu C, Zhang Z, Li B, Meng Z, Jiang C, Hu Q.
Eur J Med Chem (2021) 216 : 113313 -113313
PubMed 33667846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 8.51 8.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4436879 1 8.75
CHEMBL1800685 PPTN 1 8.70
CHEMBL4854775 1 8.66
CHEMBL4858280 1 8.58
CHEMBL4875670 1 8.53
CHEMBL4857372 1 8.31
CHEMBL4871413 1 8.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4436879 IC50 = 1.77 nM 8.75
CHEMBL1800685 PPTN IC50 = 1.98 nM 8.70
CHEMBL4854775 IC50 = 2.18 nM 8.66
CHEMBL4858280 IC50 = 2.63 nM 8.58
CHEMBL4875670 IC50 = 2.95 nM 8.53
CHEMBL4857372 IC50 = 4.85 nM 8.31
CHEMBL4871413 IC50 = 9.74 nM 8.01