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Assay Detail

CHEMBL5215411

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

Functional
Antiplasmodial activity against multidrug resistant asexual blood stage Plasmodium falciparum Dd2 assessed as inhibition of parasite growth incubated for 1 hr by HRP2-ELISA
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

3-Hydroxy-propanamidines, a New Class of Orally Active Antimalarials Targeting Plasmodium falciparum.
Knaab TC, Held J, Burckhardt BB, Rubiano K, Okombo J, Yeo T, Mok S, Uhlemann AC, Lungerich B, Fischli C, Pessanha de Carvalho L, Mordmüller B, Wittlin S, Fidock DA, Kurz T.
J Med Chem (2021) 64 : 3035 -3047
PubMed 33666415 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 6.41 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL38827 LUMEFANTRINE 4.0 1 8.70
CHEMBL5218652 1 8.05
CHEMBL5219819 1 7.92
CHEMBL5218647 1 7.85
CHEMBL5220570 1 7.40
CHEMBL5218669 1 7.30
CHEMBL5218836 1 6.92
CHEMBL76 CHLOROQUINE 4.0 1 6.64
CHEMBL5218774 1 6.64
CHEMBL5221044 1 6.54
CHEMBL5218927 1 6.46
CHEMBL5218542 1 6.19
CHEMBL5220102 1 6.16
CHEMBL5219009 1 6.03
CHEMBL5220409 1 5.96
CHEMBL5219351 1 5.82
CHEMBL5221115 1 5.62
CHEMBL5219192 1 5.29
CHEMBL5219233 1 5.25
CHEMBL5219148 1 5.00
CHEMBL5219672 1 4.70
CHEMBL5219083 1 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL38827 LUMEFANTRINE IC50 = 2.0 nM 8.70
CHEMBL5218652 IC50 = 9.0 nM 8.05
CHEMBL5219819 IC50 = 12.0 nM 7.92
CHEMBL5218647 IC50 = 14.0 nM 7.85
CHEMBL5220570 IC50 = 40.0 nM 7.40
CHEMBL5218669 IC50 = 50.0 nM 7.30
CHEMBL5218836 IC50 = 120.0 nM 6.92
CHEMBL76 CHLOROQUINE IC50 = 230.0 nM 6.64
CHEMBL5218774 IC50 = 230.0 nM 6.64
CHEMBL5221044 IC50 = 290.0 nM 6.54
CHEMBL5218927 IC50 = 350.0 nM 6.46
CHEMBL5218542 IC50 = 640.0 nM 6.19
CHEMBL5220102 IC50 = 700.0 nM 6.16
CHEMBL5219009 IC50 = 940.0 nM 6.03
CHEMBL5220409 IC50 = 1100.0 nM 5.96
CHEMBL5219351 IC50 = 1500.0 nM 5.82
CHEMBL5221115 IC50 = 2400.0 nM 5.62
CHEMBL5219192 IC50 = 5100.0 nM 5.29
CHEMBL5219233 IC50 = 5600.0 nM 5.25
CHEMBL5219148 IC50 = 10000.0 nM 5.00
CHEMBL5219672 IC50 = 20000.0 nM 4.70
CHEMBL5219083 IC50 = 22800.0 nM 4.64