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Assay Detail

CHEMBL4737832

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Functional
Antiplasmodial activity against multidrug-resistant Plasmodium falciparum Dd2 KAF156 mutant transfected with Pfs16-GFP-Luc infected in human erythrocytes assessed as reduction in [3H]-hypoxanthine incorporation pretreated for 48 hrs followed by [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counting method
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.
Le Manach C,Dam J,Woodland JG,Kaur G,Khonde LP,Brunschwig C,Njoroge M,Wicht KJ,Horatscheck A,Paquet T,Boyle GA,Gibhard L,Taylor D,Lawrence N,Yeo T,Mok S,Eastman RT,Dorjsuren D,Talley DC,Guo H,Simeonov A,Reader J,van der Watt M,Erlank E,Venter N,Zawada JW,Aswat A,Nardini L,Coetzer TL,Lauterbach SB,Bezuidenhout BC,Theron A,Mancama D,Koekemoer LL,Birkholtz LM,Wittlin S,Delves M,Ottilie S,Winzeler EA,von Geldern TW,Smith D,Fidock DA,Street LJ,Basarab GS,Duffy J,Chibale K
J Med Chem (2021) 64 : 2291 -2309
PubMed 33573376 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.73 6.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4743418 1 6.11
CHEMBL4764956 1 5.35

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4743418 IC50 = 774.0 nM 6.11
CHEMBL4764956 IC50 = 4502.0 nM 5.35