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Assay Detail

CHEMBL2114020

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Functional
OSM: Inhibition of Plasmodium falciparum K1 growth. IC50 values determined from 21 point dose response curves. Avery Group Griffith.
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum K1
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum K1 (CHEMBL612856)
Type ORGANISM
Organism Plasmodium falciparum K1

Publication

Open Source Malaria Deposition 1. http://malaria.ourexperiment.org
Vicky Avery (a), Jonathan Baell (b), Sanjay Batra (c), Jeremy Burrows (d), Soumya Bhattacharyya (c), Felix Calderon (e), Sue Charman(b), James R. Cronshaw (g), Sergio Wittlin (f), Matin Dean (g), Sandra Duffy (a), Sabine Fletcher (a), Javier Gamo (e), Zoe Hungerford (g), James Pham (h), Stuart Ralph (h), Murray N. Robertson (g), Matthew Tarnowski (g), Matthew H. Todd (g), Alice E. Williamson (g), Paul Willis (d), Karen White (b), Laura White (g), Paul M.Ylioja (g). (a) Discovery Biology, Eskitis Institute for Cell and Molecular Therapies, Griffith University, Nathan, QLD 4111, Australia; (b) Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, VIC 3052, Australia; (c) Medicinal Chemistry Division, Central Drug Research Institute, PO Box 173, Lucknow, 226 001, India; (d) Medicines for Malaria Venture, PO Box 1826, 20 rte de Pré-Bois, 1215 Geneva 15, Switzerland; (e) Tres Cantos Medicines Development Campus, Diseases of the Developing World (DDW), GlaxoSmithKline, Severo Ochoa 2, 28760 Tres Cantos, Spain; (f) Swiss Tropical and Public Health Institute, Socinstr. 57, 4051 Basel, Switzerland; (g) School of Chemistry, The University of Sydney, NSW 2006, Australia; (h) Department of Biochemistry & Molecular Biology, Bio21 Molecular Science and Biotechnology Institute, The University of Melbourne, Victoria, 3010, Australia.

· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.78 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL269671 ARTEMISININ 3.0 1 9.00
CHEMBL207990 EPOXOMYCIN 1 8.55
CHEMBL2113926 1 7.18
CHEMBL533269 1 6.82
CHEMBL2113927 1 6.44
CHEMBL549220 1 6.43
CHEMBL36 PYRIMETHAMINE 4.0 1 4.92
CHEMBL2113924 1 4.91
CHEMBL76 CHLOROQUINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL269671 ARTEMISININ IC50 = 1.0 nM 9.00
CHEMBL207990 EPOXOMYCIN IC50 = 2.8 nM 8.55
CHEMBL2113926 IC50 = 66.0 nM 7.18
CHEMBL533269 IC50 = 152.0 nM 6.82
CHEMBL2113927 IC50 = 361.0 nM 6.44
CHEMBL549220 IC50 = 375.0 nM 6.43
CHEMBL36 PYRIMETHAMINE IC50 = 11900.0 nM 4.92
CHEMBL2113924 IC50 = 12400.0 nM 4.91
CHEMBL76 CHLOROQUINE IC50 266.0 nM -