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Assay Detail

CHEMBL4818709

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Binding
Inhibition of Plasmodium falciparum HGXPRT using PRib-PP as substrate by Hanes-plot based method
12
Total Activities
12
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

Nucleotide analogues containing a pyrrolidine, piperidine or piperazine ring: Synthesis and evaluation of inhibition of plasmodial and human 6-oxopurine phosphoribosyltransferases and in vitro antimalarial activity.
Frydrych J, Keough DT, Chavchich M, Travis J, Dračínský M, Edstein MD, Guddat LW, Hocková D, Janeba Z.
Eur J Med Chem (2021) 219 : 113416 -113416
PubMed 33887682 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.49 6.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3394316 1 6.72
CHEMBL3394313 1 6.70
CHEMBL2420976 1 6.40
CHEMBL4845693 1 5.70
CHEMBL4846343 1 5.70
CHEMBL4857499 1 5.52
CHEMBL4878296 1 5.33
CHEMBL4864826 1 5.30
CHEMBL4871215 1 4.82
CHEMBL4873456 1 4.77
CHEMBL4865439 1 4.52
CHEMBL4864370 1 4.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3394316 Ki = 190.0 nM 6.72
CHEMBL3394313 Ki = 200.0 nM 6.70
CHEMBL2420976 Ki = 400.0 nM 6.40
CHEMBL4845693 Ki = 2000.0 nM 5.70
CHEMBL4846343 Ki = 2000.0 nM 5.70
CHEMBL4857499 Ki = 3000.0 nM 5.52
CHEMBL4878296 Ki = 4700.0 nM 5.33
CHEMBL4864826 Ki = 5000.0 nM 5.30
CHEMBL4871215 Ki = 15000.0 nM 4.82
CHEMBL4873456 Ki = 17000.0 nM 4.77
CHEMBL4865439 Ki = 30000.0 nM 4.52
CHEMBL4864370 Ki = 44000.0 nM 4.36