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Assay Detail

CHEMBL957102

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

Binding
Binding affinity to human recombinant CNT3 expressed in pig PK15NTD cells assessed as [3H]uridine uptake by beta-scintillation counter
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type PK15NTD
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Solute carrier family 28 member 3 (CHEMBL5707)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of phloridzin analogs as human concentrative nucleoside transporter 3 (hCNT3) inhibitors.
Gupte A, Buolamwini JK.
Bioorg Med Chem Lett (2009) 19 : 917 -921
PubMed 19097778 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 4.64 5.54

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL482331 1 5.54
CHEMBL516204 1 4.91
CHEMBL516247 1 4.91
CHEMBL245067 PHLORIZIN 1 4.80
CHEMBL474611 1 4.52
CHEMBL482066 1 4.51
CHEMBL45068 PHLORETIN 1 4.49
CHEMBL480372 1 4.38
CHEMBL482065 1 4.27
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE 1 4.05
CHEMBL514177 1 -
CHEMBL452477 2,4,6-TRIHYDROXYACETOPHENONE 1 -
CHEMBL482068 1 -
CHEMBL482067 1 -
CHEMBL480393 1 -
CHEMBL490143 DIHYDROCHALCONE 1 -
CHEMBL482332 1 -
CHEMBL454739 1 -
CHEMBL507042 1 -
CHEMBL243374 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL482331 Ki = 2880.0 nM 5.54
CHEMBL516204 Ki = 12400.0 nM 4.91
CHEMBL516247 Ki = 12350.0 nM 4.91
CHEMBL245067 PHLORIZIN Ki = 16000.0 nM 4.80
CHEMBL474611 Ki = 30020.0 nM 4.52
CHEMBL482066 Ki = 30770.0 nM 4.51
CHEMBL45068 PHLORETIN Ki = 32280.0 nM 4.49
CHEMBL480372 Ki = 42120.0 nM 4.38
CHEMBL482065 Ki = 53860.0 nM 4.27
CHEMBL418509 NITROBENZYLMERCAPTOPURINE RIBONUCLEOSIDE Ki = 88050.0 nM 4.05
CHEMBL514177 Ki > 100000.0 nM -
CHEMBL452477 2,4,6-TRIHYDROXYACETOPHENONE Ki > 100000.0 nM -
CHEMBL482068 Ki > 100000.0 nM -
CHEMBL482067 Ki > 100000.0 nM -
CHEMBL480393 Ki > 100000.0 nM -
CHEMBL490143 DIHYDROCHALCONE Ki > 100000.0 nM -
CHEMBL482332 Ki > 100000.0 nM -
CHEMBL454739 Ki > 100000.0 nM -
CHEMBL507042 Ki > 100000.0 nM -
CHEMBL243374 Ki > 100000.0 nM -