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Assay Detail

CHEMBL2329985

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

Binding
Inhibition of human N-terminal hexahistidine-tagged HGPRT
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Hypoxanthine-guanine phosphoribosyltransferase (CHEMBL2360)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Acyclic nucleoside phosphonates containing a second phosphonate group are potent inhibitors of 6-oxopurine phosphoribosyltransferases and have antimalarial activity.
Keough DT, Špaček P, Hocková D, Tichý T, Vrbková S, Slavětínská L, Janeba Z, Naesens L, Edstein MD, Chavchich M, Wang TH, de Jersey J, Guddat LW.
J Med Chem (2013) 56 : 2513 -2526
PubMed 23448281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 6.04 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2325752 1 7.52
CHEMBL2325754 1 6.22
CHEMBL2325753 1 6.00
CHEMBL2325755 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2325752 Ki = 30.0 nM 7.52
CHEMBL2325754 Ki = 600.0 nM 6.22
CHEMBL2325753 Ki = 1000.0 nM 6.00
CHEMBL2325755 Ki = 37000.0 nM 4.43