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Assay Detail

CHEMBL4737841

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

Binding
Inhibition of human ERG incubated for 4 hrs by fluorescene microplate reader assay
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

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 3 5.73 5.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4756352 1 5.80
CHEMBL4743418 1 5.66
CHEMBL4764956 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4756352 IC50 = 1600.0 nM 5.80
CHEMBL4743418 IC50 = 2200.0 nM 5.66
CHEMBL4764956 IC50 > 30000.0 nM -