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Assay Detail

CHEMBL1932722

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Binding
Inhibition of Plasmodium falciparum HGXPRT
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

Synthesis of 9-phosphonoalkyl and 9-phosphonoalkoxyalkyl purines: evaluation of their ability to act as inhibitors of Plasmodium falciparum, Plasmodium vivax and human hypoxanthine-guanine-(xanthine) phosphoribosyltransferases.
Česnek M, Hocková D, Holý A, Dračínský M, Baszczyňski O, Jersey Jd, Keough DT, Guddat LW.
Bioorg Med Chem (2012) 20 : 1076 -1089
PubMed 22178188 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 4.96 5.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL267803 1 5.70
CHEMBL1928778 1 5.66
CHEMBL20283 1 5.30
CHEMBL1928783 1 5.17
CHEMBL172844 1 5.00
CHEMBL13130 1 4.68
CHEMBL1928782 1 4.60
CHEMBL1928930 1 4.54
CHEMBL1928785 1 4.01
CHEMBL1928777 1 -
CHEMBL1928775 1 -
CHEMBL1928779 1 -
CHEMBL1928780 1 -
CHEMBL19784 1 -
CHEMBL1928781 1 -
CHEMBL1928784 1 -
CHEMBL177948 1 -
CHEMBL1928776 1 -
CHEMBL1928931 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL267803 Ki = 2000.0 nM 5.70
CHEMBL1928778 Ki = 2200.0 nM 5.66
CHEMBL20283 Ki = 5000.0 nM 5.30
CHEMBL1928783 Ki = 6700.0 nM 5.17
CHEMBL172844 Ki = 10000.0 nM 5.00
CHEMBL13130 Ki = 21000.0 nM 4.68
CHEMBL1928782 Ki = 25000.0 nM 4.60
CHEMBL1928930 Ki = 29000.0 nM 4.54
CHEMBL1928785 Ki = 97000.0 nM 4.01
CHEMBL1928777 Ki > 100000.0 nM -
CHEMBL1928775 Ki > 100000.0 nM -
CHEMBL1928779 Ki > 100000.0 nM -
CHEMBL1928780 Ki > 100000.0 nM -
CHEMBL19784 Ki > 100000.0 nM -
CHEMBL1928781 Ki > 100000.0 nM -
CHEMBL1928784 Ki > 100000.0 nM -
CHEMBL177948 Ki = 200000.0 nM -
CHEMBL1928776 Ki > 100000.0 nM -
CHEMBL1928931 Ki > 100000.0 nM -