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Assay Detail

CHEMBL4429519

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Functional
Antimalarial activity against chloroquine/mefloquine-sensitive Plasmodium falciparum 3D7 infected-erythrocytes assessed as parasite growth inhibition after 48 to 54 hrs by SYBR green 1-based replication method
21
Total Activities
21
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

Parallel inhibition of amino acid efflux and growth of erythrocytic Plasmodium falciparum by mefloquine and non-piperidine analogs: Implication for the mechanism of antimalarial action.
Ghavami M, Dapper CH, Dalal S, Holzschneider K, Klemba M, Carlier PR.
Bioorg Med Chem Lett (2016) 26 : 4846 -4850
PubMed 27544402 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.44 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL129788 1 9.92
CHEMBL1450 ATOVAQUONE 4.0 1 9.22
CHEMBL4545745 1 8.42
CHEMBL3229607 1 8.38
CHEMBL598534 1 8.33
CHEMBL602912 1 8.31
CHEMBL4521687 1 8.23
CHEMBL598533 1 8.13
CHEMBL605788 1 8.07
CHEMBL172 (S,R)-MEFLOQUINE 1 8.04
CHEMBL4586469 1 7.47
CHEMBL4441697 1 7.31
CHEMBL4435954 1 6.96
CHEMBL4483516 1 6.92
CHEMBL4435208 1 6.85
CHEMBL1822318 1 6.62
CHEMBL598930 1 6.47
CHEMBL4448380 1 6.46
CHEMBL4557449 1 5.80
CHEMBL604953 1 5.70
CHEMBL4532597 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL129788 IC50 = 0.12 nM 9.92
CHEMBL1450 ATOVAQUONE IC50 = 0.6 nM 9.22
CHEMBL4545745 IC50 = 3.8 nM 8.42
CHEMBL3229607 IC50 = 4.2 nM 8.38
CHEMBL598534 IC50 = 4.7 nM 8.33
CHEMBL602912 IC50 = 4.9 nM 8.31
CHEMBL4521687 IC50 = 5.9 nM 8.23
CHEMBL598533 IC50 = 7.4 nM 8.13
CHEMBL605788 IC50 = 8.5 nM 8.07
CHEMBL172 (S,R)-MEFLOQUINE IC50 = 9.1 nM 8.04
CHEMBL4586469 IC50 = 34.0 nM 7.47
CHEMBL4441697 IC50 = 49.0 nM 7.31
CHEMBL4435954 IC50 = 110.0 nM 6.96
CHEMBL4483516 IC50 = 120.0 nM 6.92
CHEMBL4435208 IC50 = 140.0 nM 6.85
CHEMBL1822318 IC50 = 240.0 nM 6.62
CHEMBL598930 IC50 = 340.0 nM 6.47
CHEMBL4448380 IC50 = 350.0 nM 6.46
CHEMBL4557449 IC50 = 1600.0 nM 5.80
CHEMBL604953 IC50 = 2000.0 nM 5.70
CHEMBL4532597 IC50 = 22000.0 nM 4.66