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Assay Detail

CHEMBL4622294

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

Binding
Inhibition of MRS4174 binding to mouse P2Y14R expressed in HEK293 cells pre-incubated for 30 mins before MRS4174 addition and further incubated for 30 mins by flow cytomtery based competitive fluorescence assay
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

P2Y purinoceptor 14 (CHEMBL1770046)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Exploration of Alternative Scaffolds for P2Y<sub>14</sub> Receptor Antagonists Containing a Biaryl Core.
Jung YH, Yu J, Wen Z, Salmaso V, Karcz TP, Phung NB, Chen Z, Duca S, Bennett JM, Dudas S, Salvemini D, Gao ZG, Cook DN, Jacobson KA.
J Med Chem (2020) 63 : 9563 -9589
PubMed 32787142 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 6.73 7.67

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4645216 1 7.67
CHEMBL1800685 PPTN 1 7.67
CHEMBL4642592 1 7.53
CHEMBL4640370 1 7.25
CHEMBL4212441 1 6.89
CHEMBL4454538 1 6.85
CHEMBL4633982 1 6.61
CHEMBL4212721 1 6.42
CHEMBL4649194 1 6.31
CHEMBL4645987 1 6.30
CHEMBL4646514 1 6.07
CHEMBL4299805 1 6.04
CHEMBL4637158 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4645216 IC50 = 21.4 nM 7.67
CHEMBL1800685 PPTN IC50 = 21.6 nM 7.67
CHEMBL4642592 IC50 = 29.7 nM 7.53
CHEMBL4640370 IC50 = 56.3 nM 7.25
CHEMBL4212441 IC50 = 130.0 nM 6.89
CHEMBL4454538 IC50 = 142.0 nM 6.85
CHEMBL4633982 IC50 = 246.0 nM 6.61
CHEMBL4212721 IC50 = 384.0 nM 6.42
CHEMBL4649194 IC50 = 487.0 nM 6.31
CHEMBL4645987 IC50 = 499.0 nM 6.30
CHEMBL4646514 IC50 = 845.0 nM 6.07
CHEMBL4299805 IC50 = 902.0 nM 6.04
CHEMBL4637158 IC50 = 1160.0 nM 5.94