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Assay Detail

CHEMBL2444844

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Functional
Antiplasmodial activity against Plasmodium falciparum K1 assessed as [3H]-hypoxanthine incorporation after 48 hrs by liquid scintillation counting analysis
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Synthesis and antiprotozoal activity of dicationic 2,6-diphenylpyrazines and aza-analogues.
Hu L, Patel A, Bondada L, Yang S, Wang MZ, Munde M, Wilson WD, Wenzler T, Brun R, Boykin DW.
Bioorg Med Chem (2013) 21 : 6732 -6741
PubMed 24012380 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.82 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL403091 1 9.40
CHEMBL145251 1 8.19
CHEMBL2442601 1 8.00
CHEMBL2442609 1 8.00
CHEMBL24057 FURAMIDINE -1.0 1 7.81
CHEMBL2442605 1 7.57
CHEMBL2442612 1 7.51
CHEMBL55 PENTAMIDINE 4.0 1 7.33
CHEMBL2442606 1 7.28
CHEMBL358287 1 7.08
CHEMBL2442700 1 7.07
CHEMBL2442604 1 6.49
CHEMBL2442702 1 6.48
CHEMBL2442603 1 6.39
CHEMBL2442610 1 6.34
CHEMBL2442611 1 6.34
CHEMBL2442701 1 6.11
CHEMBL2442602 1 6.06
CHEMBL2442608 1 5.25
CHEMBL2442613 1 5.15
CHEMBL2442614 1 5.13
CHEMBL2442607 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL403091 IC50 = 0.4 nM 9.40
CHEMBL145251 IC50 = 6.5 nM 8.19
CHEMBL2442601 IC50 = 10.0 nM 8.00
CHEMBL2442609 IC50 = 10.0 nM 8.00
CHEMBL24057 FURAMIDINE IC50 = 15.5 nM 7.81
CHEMBL2442605 IC50 = 27.0 nM 7.57
CHEMBL2442612 IC50 = 31.0 nM 7.51
CHEMBL55 PENTAMIDINE IC50 = 46.4 nM 7.33
CHEMBL2442606 IC50 = 52.0 nM 7.28
CHEMBL358287 IC50 = 83.0 nM 7.08
CHEMBL2442700 IC50 = 85.0 nM 7.07
CHEMBL2442604 IC50 = 323.0 nM 6.49
CHEMBL2442702 IC50 = 328.0 nM 6.48
CHEMBL2442603 IC50 = 410.0 nM 6.39
CHEMBL2442610 IC50 = 453.0 nM 6.34
CHEMBL2442611 IC50 = 453.0 nM 6.34
CHEMBL2442701 IC50 = 785.0 nM 6.11
CHEMBL2442602 IC50 = 870.0 nM 6.06
CHEMBL2442608 IC50 = 5600.0 nM 5.25
CHEMBL2442613 IC50 = 7010.0 nM 5.15
CHEMBL2442614 IC50 = 7390.0 nM 5.13
CHEMBL2442607 IC50 = 8400.0 nM 5.08