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Assay Detail

CHEMBL4811591

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

Functional
Antiplasmodial activity against drug-sensitive asexual intraerythrocytic stage of Plasmodium falciparum 3D7 infected in human O+ erythrocytes assessed as inhibition of parasite growth incubated for 48 hrs followed by addition of [3H]hypoxanthine for 24 hrs by [3H]hypoxanthine incorporation assay
18
Total Activities
18
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

Investigation of the in vitro and in vivo efficacy of peptoid-based HDAC inhibitors with dual-stage antiplasmodial activity.
Mackwitz MKW, Hesping E, Eribez K, Schöler A, Antonova-Koch Y, Held J, Winzeler EA, Andrews KT, Hansen FK.
Eur J Med Chem (2021) 211 : 113065 -113065
PubMed 33360801 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.10 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 8.15
CHEMBL4853947 1 8.10
CHEMBL4849568 1 7.80
CHEMBL4868526 1 7.62
CHEMBL4862927 1 7.55
CHEMBL4854577 1 7.47
CHEMBL4847978 1 7.16
CHEMBL98 VORINOSTAT 4.0 1 7.16
CHEMBL4873872 1 7.12
CHEMBL4858841 1 7.00
CHEMBL4854335 1 6.90
CHEMBL4878499 1 6.85
CHEMBL4866446 1 6.79
CHEMBL4873978 1 6.67
CHEMBL4851776 1 6.67
CHEMBL4849235 1 6.55
CHEMBL4878538 1 6.29
CHEMBL4868592 1 5.98

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE IC50 = 7.0 nM 8.15
CHEMBL4853947 IC50 = 8.0 nM 8.10
CHEMBL4849568 IC50 = 16.0 nM 7.80
CHEMBL4868526 IC50 = 24.0 nM 7.62
CHEMBL4862927 IC50 = 28.0 nM 7.55
CHEMBL4854577 IC50 = 34.0 nM 7.47
CHEMBL4847978 IC50 = 70.0 nM 7.16
CHEMBL98 VORINOSTAT IC50 = 69.0 nM 7.16
CHEMBL4873872 IC50 = 76.0 nM 7.12
CHEMBL4858841 IC50 = 101.0 nM 7.00
CHEMBL4854335 IC50 = 127.0 nM 6.90
CHEMBL4878499 IC50 = 142.0 nM 6.85
CHEMBL4866446 IC50 = 161.0 nM 6.79
CHEMBL4873978 IC50 = 215.0 nM 6.67
CHEMBL4851776 IC50 = 213.0 nM 6.67
CHEMBL4849235 IC50 = 281.0 nM 6.55
CHEMBL4878538 IC50 = 509.0 nM 6.29
CHEMBL4868592 IC50 = 1040.0 nM 5.98