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Assay Detail

CHEMBL3301557

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Functional
MMV: Measure of pLDH activity as indication of parasite viability. Gametocytogenesis of 3D7 Plasmodium falciparum strain was induced in vitro and asexual parasites were depleted with N-acetylglucosamine. Gametocytes were treated with dihydroartemisinin, epoxomicin, methylene blue, primaquine, puromycin or chloroquine in 96-well plates and the pLDH activity was evaluated using a modified Makler protocol. Mosquito infectivity was measured by the standard membrane feeding assay. The IC50 value was extrapolated as the concentration that induced a 50% inhibition of gametocyte viability.
ChEMBL ↗
39
Total Activities
39
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

MMV Malaria Box screening in pLDH viability assay against Plasmodium falciparum gametocytes.
Taramelli Lab, University of Milan, Italy.

· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.71 6.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL592105 METHYLROSANILINE -1.0 1 6.80
CHEMBL586031 — — 1 6.63
CHEMBL546799 — — 1 6.54
CHEMBL582767 — — 1 6.39
CHEMBL602580 — — 1 6.24
CHEMBL1437888 — — 1 6.16
CHEMBL106525 — — 1 6.13
CHEMBL588481 — — 1 6.12
CHEMBL601156 — — 1 6.04
CHEMBL533855 — — 1 5.87
CHEMBL470514 — — 1 5.86
CHEMBL546531 — — 1 5.84
CHEMBL2028064 — — 1 5.79
CHEMBL600235 — — 1 5.72
CHEMBL588501 — — 1 5.71
CHEMBL537087 — — 1 5.68
CHEMBL530531 — — 1 5.66
CHEMBL534319 — — 1 5.62
CHEMBL532597 — — 1 5.58
CHEMBL533917 — — 1 5.58
CHEMBL583555 — — 1 5.57
CHEMBL530223 — — 1 5.56
CHEMBL584235 — — 1 5.55
CHEMBL590683 — — 1 5.51
CHEMBL124006 — — 1 5.50
CHEMBL584015 — — 1 5.49
CHEMBL591183 — — 1 5.48
CHEMBL580516 — — 1 5.47
CHEMBL533598 — — 1 5.42
CHEMBL592123 — — 1 5.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL592105 METHYLROSANILINE IC50 = 157.88 nM 6.80
CHEMBL586031 — IC50 = 235.65 nM 6.63
CHEMBL546799 — IC50 = 287.65 nM 6.54
CHEMBL582767 — IC50 = 406.9 nM 6.39
CHEMBL602580 — IC50 = 575.7 nM 6.24
CHEMBL1437888 — IC50 = 696.44 nM 6.16
CHEMBL106525 — IC50 = 732.02 nM 6.13
CHEMBL588481 — IC50 = 757.65 nM 6.12
CHEMBL601156 — IC50 = 902.2 nM 6.04
CHEMBL533855 — IC50 = 1339.7 nM 5.87
CHEMBL470514 — IC50 = 1376.26 nM 5.86
CHEMBL546531 — IC50 = 1436.85 nM 5.84
CHEMBL2028064 — IC50 = 1621.0 nM 5.79
CHEMBL600235 — IC50 = 1900.53 nM 5.72
CHEMBL588501 — IC50 = 1927.98 nM 5.71
CHEMBL537087 — IC50 = 2079.75 nM 5.68
CHEMBL530531 — IC50 = 2210.72 nM 5.66
CHEMBL534319 — IC50 = 2388.73 nM 5.62
CHEMBL533917 — IC50 = 2648.25 nM 5.58
CHEMBL532597 — IC50 = 2641.95 nM 5.58
CHEMBL583555 — IC50 = 2716.95 nM 5.57
CHEMBL530223 — IC50 = 2753.07 nM 5.56
CHEMBL584235 — IC50 = 2825.82 nM 5.55
CHEMBL590683 — IC50 = 3085.2 nM 5.51
CHEMBL124006 — IC50 = 3136.6 nM 5.50
CHEMBL584015 — IC50 = 3220.62 nM 5.49
CHEMBL591183 — IC50 = 3281.18 nM 5.48
CHEMBL580516 — IC50 = 3406.95 nM 5.47
CHEMBL592123 — IC50 = 3800.97 nM 5.42
CHEMBL533598 — IC50 = 3805.43 nM 5.42
CHEMBL586033 — IC50 = 3889.65 nM 5.41
CHEMBL525106 — IC50 = 3925.45 nM 5.41
CHEMBL585966 — IC50 = 4037.43 nM 5.39
CHEMBL602586 — IC50 = 4160.5 nM 5.38
CHEMBL591637 — IC50 = 4607.6 nM 5.34
CHEMBL125044 — IC50 = 5007.65 nM 5.30
CHEMBL2028063 — IC50 = 5616.28 nM 5.25
CHEMBL530308 — IC50 = 6522.6 nM 5.19
CHEMBL600488 — IC50 = 8898.85 nM 5.05