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Assay Detail

CHEMBL1037264

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

Binding
Displacement of SAENTA-fluorescein from human ENT1 in HL60 cells by flow cytometry
4
Total Activities
2
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HL-60
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Equilibrative nucleoside transporter 1 (CHEMBL1997)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Towards to hENT1-nucleoside transporter selective imaging agents. Synthesis and in vitro evaluation of the radiolabeled SAENTA analogues.
Zlatopolskiy BD, Morgenroth A, Urusova EA, Dinger C, Kull T, Pape M, Glatting G, Reske SN.
Bioorg Med Chem Lett (2009) 19 : 5151 -5154
PubMed 19632836 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 8.57 8.85
Ki 2 10.47 10.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL571939 2 10.74
CHEMBL569223 2 10.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL571939 Ki = 0.018 nM 10.74
CHEMBL569223 Ki = 0.064 nM 10.19
CHEMBL571939 IC50 = 1.4 nM 8.85
CHEMBL569223 IC50 = 5.1 nM 8.29