Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL752093

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

Binding
Binding affinity of compound towards Nucleoside transporter es-type by facile competitive binding flow cytometric assay using the human K562 chronic melogenous leukemia cell line
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type K562
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Synthesis and flow cytometric evaluation of novel 1,2,3,4-tetrahydroisoquinoline conformationally constrained analogues of nitrobenzylmercaptopurine riboside (NBMPR) designed for probing its conformation when bound to the es nucleoside transporter.
Zhu Z, Furr J, Buolamwini JK.
J Med Chem (2003) 46 : 831 -837
PubMed 12593662 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.71 9.35

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL260570 1 9.35
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE 1 9.15
CHEMBL261227 1 7.82
CHEMBL429511 1 6.82
CHEMBL408670 1 6.60
CHEMBL261226 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL260570 Ki = 0.45 nM 9.35
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE Ki = 0.7 nM 9.15
CHEMBL261227 Ki = 15.0 nM 7.82
CHEMBL429511 Ki = 150.0 nM 6.82
CHEMBL408670 Ki = 250.0 nM 6.60
CHEMBL261226 Ki = 300.0 nM 6.52