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Assay Detail

CHEMBL4392271

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

Binding
Displacement of 6-Amino-9-(2-carboxy-4-((6-(4-(4-(4-(4-(3-carboxy-6-(4-(trifluoromethyl)phenyl)-naphthalen-1-yl)phenyl)piperidin-1-yl)butyl)-1H-1,2,3-triazol-1-yl)hexyl)carbamoyl)-phenyl)-3-iminio-5-sulfo-3H-xanthene-4-sulfonate from recombinant human P2Y14 receptor expressed in CHO cells preincubated for 30 mins followed by tracer addition and measured after 30 mins by flow cytometry
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Structure-Activity Relationship of Purine and Pyrimidine Nucleotides as Ecto-5'-Nucleotidase (CD73) Inhibitors.
Junker A, Renn C, Dobelmann C, Namasivayam V, Jain S, Losenkova K, Irjala H, Duca S, Balasubramanian R, Chakraborty S, Börgel F, Zimmermann H, Yegutkin GG, Müller CE, Jacobson KA.
J Med Chem (2019) 62 : 3677 -3695
PubMed 30895781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 5.81 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3606064 1 6.44
CHEMBL4483379 1 5.18
CHEMBL4443977 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3606064 IC50 = 362.0 nM 6.44
CHEMBL4483379 IC50 = 6660.0 nM 5.18
CHEMBL4443977 IC50 > 3000.0 nM -