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Assay Detail

CHEMBL1287512

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Binding
Inhibition of Plasmodium falciparum PNP expressed in Escherichia coli BL21(DE3) cells by spectrophotometry
20
Total Activities
12
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Plasmodium falciparum
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Purine nucleoside phosphorylase (CHEMBL5648)
Type SINGLE PROTEIN
Organism Plasmodium falciparum

Publication

Exploring new inhibitors of Plasmodium falciparum purine nucleoside phosphorylase.
Cui H, Ruda GF, Carrero-Lérida J, Ruiz-Pérez LM, Gilbert IH, González-Pacanowska D.
Eur J Med Chem (2010) 45 : 5140 -5149
PubMed 20817362 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 6.39 9.07
IC50 10 4.38 4.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL218291 FORODESINE 4.0 1 9.07
CHEMBL1277898 2 8.96
CHEMBL1275659 1 8.57
CHEMBL1275720 2 5.22
CHEMBL1275699 2 4.57
CHEMBL1275700 2 4.23
CHEMBL1275721 2 4.12
CHEMBL37519 1 -
CHEMBL1275661 1 -
CHEMBL1275701 2 -
CHEMBL1275702 2 -
CHEMBL1275719 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL218291 FORODESINE Ki = 0.86 nM 9.07
CHEMBL1277898 Ki = 1.1 nM 8.96
CHEMBL1275659 Ki = 2.7 nM 8.57
CHEMBL1275720 Ki = 6000.0 nM 5.22
CHEMBL1275699 Ki = 27000.0 nM 4.57
CHEMBL1275720 IC50 = 42000.0 nM 4.38
CHEMBL1275700 Ki = 59000.0 nM 4.23
CHEMBL1275721 Ki = 75000.0 nM 4.12
CHEMBL37519 IC50 > 1000000.0 nM -
CHEMBL1277898 IC50 > 1000000.0 nM -
CHEMBL1275661 IC50 > 1000000.0 nM -
CHEMBL1275701 Ki = 136000.0 nM -
CHEMBL1275702 Ki = 105000.0 nM -
CHEMBL1275719 Ki = 113000.0 nM -
CHEMBL1275699 IC50 = 141000.0 nM -
CHEMBL1275700 IC50 = 230000.0 nM -
CHEMBL1275701 IC50 = 712000.0 nM -
CHEMBL1275702 IC50 = 524000.0 nM -
CHEMBL1275719 IC50 = 592000.0 nM -
CHEMBL1275721 IC50 = 366000.0 nM -