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Assay Detail

CHEMBL4041379

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Binding
Inhibition of Plasmodium falciparum HGPRT using PRib-PP as the substrate by spectrophotometric method
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 8 5.83 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4086362 1 7.16
CHEMBL2325754 1 6.30
CHEMBL4064903 1 6.05
CHEMBL4078513 1 5.70
CHEMBL4102796 1 5.52
CHEMBL4067618 1 5.40
CHEMBL2325753 1 5.30
CHEMBL4066772 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4086362 Ki = 70.0 nM 7.16
CHEMBL2325754 Ki = 500.0 nM 6.30
CHEMBL4064903 Ki = 900.0 nM 6.05
CHEMBL4078513 Ki = 2000.0 nM 5.70
CHEMBL4102796 Ki = 3000.0 nM 5.52
CHEMBL4067618 Ki = 4000.0 nM 5.40
CHEMBL2325753 Ki = 5000.0 nM 5.30
CHEMBL4066772 Ki = 6000.0 nM 5.22