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Assay Detail

CHEMBL823109

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

Binding
Displacement of 5-(SAENTA)-X8-fluorescein from K562 cell nucleoside transporter
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type K562
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Novel halogenated nitrobenzylthioinosine analogs as es nucleoside transporter inhibitors.
Gupte A, Buolamwini JK.
Bioorg Med Chem Lett (2004) 14 : 2257 -2260
PubMed 15081020 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.87 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE 1 9.15
CHEMBL512162 1 8.41
CHEMBL932 DIPYRIDAMOLE 4.0 1 8.06
CHEMBL418496 1 8.04
CHEMBL430946 1 8.00
CHEMBL517945 1 7.95
CHEMBL473492 1 7.86
CHEMBL61387 1 7.85
CHEMBL464810 1 7.80
CHEMBL516202 1 7.79
CHEMBL60735 1 7.70
CHEMBL475104 1 7.69
CHEMBL292374 1 7.00
CHEMBL475103 1 6.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE Ki = 0.7 nM 9.15
CHEMBL512162 Ki = 3.88 nM 8.41
CHEMBL932 DIPYRIDAMOLE Ki = 8.79 nM 8.06
CHEMBL418496 Ki = 9.02 nM 8.04
CHEMBL430946 Ki = 9.98 nM 8.00
CHEMBL517945 Ki = 11.21 nM 7.95
CHEMBL473492 Ki = 13.79 nM 7.86
CHEMBL61387 Ki = 14.23 nM 7.85
CHEMBL464810 Ki = 15.96 nM 7.80
CHEMBL516202 Ki = 16.13 nM 7.79
CHEMBL60735 Ki = 19.87 nM 7.70
CHEMBL475104 Ki = 20.54 nM 7.69
CHEMBL292374 Ki = 99.49 nM 7.00
CHEMBL475103 Ki = 134.23 nM 6.87