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Assay Detail

CHEMBL2045642

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 24 hrs by hypoxanthine incorporation assay
32
Total Activities
32
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

3,5-Diaryl-2-aminopyridines as a novel class of orally active antimalarials demonstrating single dose cure in mice and clinical candidate potential.
Younis Y, Douelle F, Feng TS, González Cabrera D, Le Manach C, Nchinda AT, Duffy S, White KL, Shackleford DM, Morizzi J, Mannila J, Katneni K, Bhamidipati R, Zabiulla KM, Joseph JT, Bashyam S, Waterson D, Witty MJ, Hardick D, Wittlin S, Avery V, Charman SA, Chibale K.
J Med Chem (2012) 55 : 3479 -3487
PubMed 22390538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 6.71 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2041987 1 7.72
CHEMBL2041991 1 7.70
CHEMBL2041980 MMV-048 2.0 1 7.60
CHEMBL2041978 1 7.54
CHEMBL2042003 1 7.52
CHEMBL2041994 1 7.48
CHEMBL528966 1 7.31
CHEMBL531475 1 7.29
CHEMBL2041988 1 7.24
CHEMBL2042002 1 7.15
CHEMBL2041993 1 7.10
CHEMBL2041985 1 7.05
CHEMBL2041977 1 6.92
CHEMBL2041992 1 6.82
CHEMBL2041983 1 6.81
CHEMBL2041981 1 6.77
CHEMBL2041984 1 6.75
CHEMBL2041998 1 6.66
CHEMBL2041976 1 6.55
CHEMBL2041997 1 6.48
CHEMBL2041979 1 6.30
CHEMBL2041996 1 6.28
CHEMBL2041982 1 6.27
CHEMBL2041995 1 6.23
CHEMBL2041986 1 6.20
CHEMBL2041990 1 6.09
CHEMBL2041974 1 6.09
CHEMBL2041975 1 5.96
CHEMBL2042001 1 5.95
CHEMBL2041989 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2041987 IC50 = 19.0 nM 7.72
CHEMBL2041991 IC50 = 20.0 nM 7.70
CHEMBL2041980 MMV-048 IC50 = 25.0 nM 7.60
CHEMBL2041978 IC50 = 29.0 nM 7.54
CHEMBL2042003 IC50 = 30.0 nM 7.52
CHEMBL2041994 IC50 = 33.0 nM 7.48
CHEMBL528966 IC50 = 49.0 nM 7.31
CHEMBL531475 IC50 = 51.0 nM 7.29
CHEMBL2041988 IC50 = 58.0 nM 7.24
CHEMBL2042002 IC50 = 71.0 nM 7.15
CHEMBL2041993 IC50 = 80.0 nM 7.10
CHEMBL2041985 IC50 = 90.0 nM 7.05
CHEMBL2041977 IC50 = 120.0 nM 6.92
CHEMBL2041992 IC50 = 150.0 nM 6.82
CHEMBL2041983 IC50 = 155.0 nM 6.81
CHEMBL2041981 IC50 = 169.0 nM 6.77
CHEMBL2041984 IC50 = 180.0 nM 6.75
CHEMBL2041998 IC50 = 220.0 nM 6.66
CHEMBL2041976 IC50 = 280.0 nM 6.55
CHEMBL2041997 IC50 = 330.0 nM 6.48
CHEMBL2041979 IC50 = 500.0 nM 6.30
CHEMBL2041996 IC50 = 520.0 nM 6.28
CHEMBL2041982 IC50 = 540.0 nM 6.27
CHEMBL2041995 IC50 = 590.0 nM 6.23
CHEMBL2041986 IC50 = 634.0 nM 6.20
CHEMBL2041990 IC50 = 818.0 nM 6.09
CHEMBL2041974 IC50 = 818.0 nM 6.09
CHEMBL2041975 IC50 = 1106.0 nM 5.96
CHEMBL2042001 IC50 = 1120.0 nM 5.95
CHEMBL2041989 IC50 = 2132.0 nM 5.67
CHEMBL2042000 IC50 = 2160.0 nM 5.67
CHEMBL2041999 IC50 = 2400.0 nM 5.62