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Assay Detail

CHEMBL5159176

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Binding
Inhibition of Plasmodium falciparum HGXPRT using PRib-PP as substrate by spectrophotometric assay
19
Total Activities
19
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

Stereo-Defined Acyclic Nucleoside Phosphonates are Selective and Potent Inhibitors of Parasite 6-Oxopurine Phosphoribosyltransferases.
Klejch T, Keough DT, King G, Doleželová E, Česnek M, Buděšínský M, Zíková A, Janeba Z, Guddat LW, Hocková D.
J Med Chem (2022) 65 : 4030 -4057
PubMed 35175749 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 6.60 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5184028 1 8.70
CHEMBL5178774 1 7.85
CHEMBL5185227 1 7.52
CHEMBL5208021 1 7.52
CHEMBL5171024 1 7.30
CHEMBL5198761 1 7.16
CHEMBL5207635 1 7.16
CHEMBL5187896 1 7.00
CHEMBL5180136 1 6.70
CHEMBL5186759 1 6.52
CHEMBL5179417 1 6.40
CHEMBL5197487 1 6.16
CHEMBL5180101 1 6.10
CHEMBL5205733 1 6.00
CHEMBL5170511 1 6.00
CHEMBL5176444 1 5.62
CHEMBL5185264 1 5.52
CHEMBL5180341 1 5.22
CHEMBL5193549 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5184028 Ki = 2.0 nM 8.70
CHEMBL5178774 Ki = 14.0 nM 7.85
CHEMBL5185227 Ki = 30.0 nM 7.52
CHEMBL5208021 Ki = 30.0 nM 7.52
CHEMBL5171024 Ki = 50.0 nM 7.30
CHEMBL5198761 Ki = 70.0 nM 7.16
CHEMBL5207635 Ki = 70.0 nM 7.16
CHEMBL5187896 Ki = 100.0 nM 7.00
CHEMBL5180136 Ki = 200.0 nM 6.70
CHEMBL5186759 Ki = 300.0 nM 6.52
CHEMBL5179417 Ki = 400.0 nM 6.40
CHEMBL5197487 Ki = 700.0 nM 6.16
CHEMBL5180101 Ki = 800.0 nM 6.10
CHEMBL5205733 Ki = 1000.0 nM 6.00
CHEMBL5170511 Ki = 1000.0 nM 6.00
CHEMBL5176444 Ki = 2400.0 nM 5.62
CHEMBL5185264 Ki = 3000.0 nM 5.52
CHEMBL5180341 Ki = 6000.0 nM 5.22
CHEMBL5193549 Ki = 13000.0 nM 4.89