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Assay Detail

CHEMBL4231438

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

Functional
Gametocytocidal activity against Plasmodium falciparum 3D7 elo1-pfs16-CBG99 late-stage (4 to 5) gametocytes assessed as inhibition of parasite viability after 72 hrs by luciferase reporter assay
23
Total Activities
23
Compounds Tested
1
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

Antimalarial agents against both sexual and asexual parasites stages: structure-activity relationships and biological studies of the Malaria Box compound 1-[5-(4-bromo-2-chlorophenyl)furan-2-yl]-N-[(piperidin-4-yl)methyl]methanamine (MMV019918) and analogues.
Vallone A, D'Alessandro S, Brogi S, Brindisi M, Chemi G, Alfano G, Lamponi S, Lee SG, Jez JM, Koolen KJM, Dechering KJ, Saponara S, Fusi F, Gorelli B, Taramelli D, Parapini S, Caldelari R, Campiani G, Gemma S, Butini S.
Eur J Med Chem (2018) 150 : 698 -718
PubMed 29571157 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 5.76 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL207990 EPOXOMYCIN 1 8.15
CHEMBL405110 METHYLENE BLUE ANHYDROUS 4.0 1 7.52
CHEMBL4245012 1 6.08
CHEMBL4245471 1 6.07
CHEMBL4240668 1 5.96
CHEMBL4238529 1 5.96
CHEMBL537152 1 5.92
CHEMBL4242609 1 5.85
CHEMBL4246869 1 5.85
CHEMBL4249272 1 5.85
CHEMBL4242227 1 5.72
CHEMBL4238335 1 5.40
CHEMBL4246056 1 5.36
CHEMBL4242704 1 5.32
CHEMBL4248315 1 5.23
CHEMBL4241797 1 5.22
CHEMBL4245585 1 5.08
CHEMBL4244830 1 5.07
CHEMBL4241601 1 4.93
CHEMBL4238087 1 4.74
CHEMBL4248815 1 -
CHEMBL4238777 1 -
CHEMBL4246962 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL207990 EPOXOMYCIN IC50 = 7.0 nM 8.15
CHEMBL405110 METHYLENE BLUE ANHYDROUS IC50 = 30.0 nM 7.52
CHEMBL4245012 IC50 = 830.0 nM 6.08
CHEMBL4245471 IC50 = 850.0 nM 6.07
CHEMBL4240668 IC50 = 1100.0 nM 5.96
CHEMBL4238529 IC50 = 1100.0 nM 5.96
CHEMBL537152 IC50 = 1200.0 nM 5.92
CHEMBL4242609 IC50 = 1400.0 nM 5.85
CHEMBL4246869 IC50 = 1400.0 nM 5.85
CHEMBL4249272 IC50 = 1400.0 nM 5.85
CHEMBL4242227 IC50 = 1900.0 nM 5.72
CHEMBL4238335 IC50 = 4000.0 nM 5.40
CHEMBL4246056 IC50 = 4400.0 nM 5.36
CHEMBL4242704 IC50 = 4800.0 nM 5.32
CHEMBL4248315 IC50 = 5900.0 nM 5.23
CHEMBL4241797 IC50 = 6000.0 nM 5.22
CHEMBL4245585 IC50 = 8300.0 nM 5.08
CHEMBL4244830 IC50 = 8600.0 nM 5.07
CHEMBL4241601 IC50 = 11800.0 nM 4.93
CHEMBL4238087 IC50 = 18400.0 nM 4.74
CHEMBL4248815 IC50 > 13000.0 nM -
CHEMBL4238777 IC50 > 26000.0 nM -
CHEMBL4246962 IC50 > 24000.0 nM -