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Assay Detail

CHEMBL2114001

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Functional
OSM: Inhibition of Plasmodium falciparum 3D7 growth using a SYBR green I fluorescence based assay. Dose response curves were generated comprising of 8 points using a 2-fold serial dilution for the maximum final concentration of 1000 nM. Ralph Group, Bio21.
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Plasmodium falciparum 3D7
Confidence 1 — Organism
Curated By Autocuration

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

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 16 7.17 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113939 1 8.30
CHEMBL2113942 1 8.10
CHEMBL2113937 1 8.05
CHEMBL599702 1 7.96
CHEMBL2113944 1 7.55
CHEMBL2113945 1 6.81
CHEMBL2113938 1 6.69
CHEMBL2113943 1 6.47
CHEMBL2113946 1 6.36
CHEMBL2113947 1 6.31
CHEMBL2113948 1 6.28
CHEMBL2113931 1 -
CHEMBL2113932 1 -
CHEMBL2113940 1 -
CHEMBL2113941 1 -
CHEMBL1363033 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113939 IC50 = 5.0 nM 8.30
CHEMBL2113942 IC50 = 8.0 nM 8.10
CHEMBL2113937 IC50 = 9.0 nM 8.05
CHEMBL599702 IC50 = 11.0 nM 7.96
CHEMBL2113944 IC50 = 28.0 nM 7.55
CHEMBL2113945 IC50 = 156.0 nM 6.81
CHEMBL2113938 IC50 = 205.0 nM 6.69
CHEMBL2113943 IC50 = 339.0 nM 6.47
CHEMBL2113946 IC50 = 442.0 nM 6.36
CHEMBL2113947 IC50 = 485.0 nM 6.31
CHEMBL2113948 IC50 = 520.0 nM 6.28
CHEMBL2113931 IC50 > 1000.0 nM -
CHEMBL2113932 IC50 > 1000.0 nM -
CHEMBL2113940 IC50 > 1000.0 nM -
CHEMBL2113941 IC50 > 1000.0 nM -
CHEMBL1363033 IC50 > 1000.0 nM -