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Assay Detail

CHEMBL4041378

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Binding
Inhibition of human HGPRT using PRib-PP as the substrate by spectrophotometric method
10
Total Activities
10
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

Synthesis and Evaluation of Asymmetric Acyclic Nucleoside Bisphosphonates as Inhibitors of Plasmodium falciparum and Human Hypoxanthine-Guanine-(Xanthine) Phosphoribosyltransferase.
Špaček P, Keough DT, Chavchich M, Dračínský M, Janeba Z, Naesens L, Edstein MD, Guddat LW, Hocková D.
J Med Chem (2017) 60 : 7539 -7554
PubMed 28813147 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.37 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086362 1 8.22
CHEMBL4067618 1 7.00
CHEMBL4078513 1 7.00
CHEMBL4064903 1 6.40
CHEMBL2325754 1 6.22
CHEMBL3578109 1 6.16
CHEMBL2325753 1 6.00
CHEMBL4102796 1 5.75
CHEMBL4083808 1 5.60
CHEMBL4066772 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086362 Ki = 6.0 nM 8.22
CHEMBL4067618 Ki = 100.0 nM 7.00
CHEMBL4078513 Ki = 100.0 nM 7.00
CHEMBL4064903 Ki = 400.0 nM 6.40
CHEMBL2325754 Ki = 600.0 nM 6.22
CHEMBL3578109 Ki = 700.0 nM 6.16
CHEMBL2325753 Ki = 1000.0 nM 6.00
CHEMBL4102796 Ki = 1800.0 nM 5.75
CHEMBL4083808 Ki = 2500.0 nM 5.60
CHEMBL4066772 Ki = 4600.0 nM 5.34