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Assay Detail

CHEMBL896616

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

Binding
Inhibition of human PNP in presence of 1 mM phosphate
7
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Purine nucleoside phosphorylase (CHEMBL4338)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of 9-deazaguanine derivatives connected by a linker to difluoromethylene phosphonic acid as multi-substrate analogue inhibitors of PNP.
Hikishima S, Hashimoto M, Magnowska L, Bzowska A, Yokomatsu T.
Bioorg Med Chem Lett (2007) 17 : 4173 -4177
PubMed 17544667 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 7.54 8.02
Ki 3 8.11 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL236711 2 8.28
CHEMBL236709 2 8.09
CHEMBL236708 2 7.97
CHEMBL236710 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL236711 Ki = 5.3 nM 8.28
CHEMBL236709 Ki = 8.1 nM 8.09
CHEMBL236711 IC50 = 9.5 nM 8.02
CHEMBL236708 Ki = 10.8 nM 7.97
CHEMBL236708 IC50 = 20.2 nM 7.70
CHEMBL236709 IC50 = 20.4 nM 7.69
CHEMBL236710 IC50 = 173.0 nM 6.76