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Assay Detail

CHEMBL911615

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Functional
Inhibition of [3H]hypoxanthine uptake in Plasmodium falciparum 3D7
9
Total Activities
9
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum
Confidence 1 — Organism
Curated By Intermediate

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Lead compounds for antimalarial chemotherapy: purine base analogs discriminate between human and P. falciparum 6-oxopurine phosphoribosyltransferases.
Keough DT, Skinner-Adams T, Jones MK, Ng AL, Brereton IM, Guddat LW, de Jersey J.
J Med Chem (2006) 49 : 7479 -7486
PubMed 17149876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.83 5.89
Activity 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1425 MERCAPTOPURINE ANHYDROUS 4.0 1 5.89
CHEMBL1427 HYPOXANTHINE 1 5.38
CHEMBL374107 8-AZAGUANINE 1 5.18
CHEMBL727 THIOGUANINE 4.0 1 4.67
CHEMBL219568 GUANINE 3.0 1 4.45
CHEMBL226396 6-CHLOROGUANINE 1 4.17
CHEMBL219416 1 4.05
CHEMBL1467 ALLOPURINOL 4.0 1 -
CHEMBL219341 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1425 MERCAPTOPURINE ANHYDROUS IC50 = 1300.0 nM 5.89
CHEMBL1427 HYPOXANTHINE IC50 = 4200.0 nM 5.38
CHEMBL374107 8-AZAGUANINE IC50 = 6600.0 nM 5.18
CHEMBL727 THIOGUANINE IC50 = 21300.0 nM 4.67
CHEMBL219568 GUANINE IC50 = 35300.0 nM 4.45
CHEMBL226396 6-CHLOROGUANINE IC50 = 67000.0 nM 4.17
CHEMBL219416 IC50 = 90000.0 nM 4.05
CHEMBL1467 ALLOPURINOL IC50 >= 150000.0 nM -
CHEMBL219341 Activity - -