Assay Detail

CHEMBL1248669

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Functional

Antimalarial activity against Plasmodium falciparum Dd2 containing attB site inserted in parasite genome and expressing parental ATP4 after 72 hrs by SYBR green based fluorescence assay

ChEMBL ↗

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Target

Plasmodium falciparum (CHEMBL364) ↗

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Primary target Plasmodium falciparum

CHEMBL364

Anchored from Assay target.

Protein identity Plasmodium falciparum

Disease frame Disease evidence pending

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Total Activities

Compounds Tested

Activity Types

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

Spiroindolones, a potent compound class for the treatment of malaria.

Rottmann M, McNamara C, Yeung BK, Lee MC, Zou B, Russell B, Seitz P, Plouffe DM, Dharia NV, Tan J, Cohen SB, Spencer KR, González-Páez GE, Lakshminarayana SB, Goh A, Suwanarusk R, Jegla T, Schmitt EK, Beck HP, Brun R, Nosten F, Renia L, Dartois V, Keller TH, Fidock DA, Winzeler EA, Diagana TT.
Science (2010) 329 : 1175 -1180
PubMed 20813948 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
IC50	4	8.00	9.07

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1082723	CIPARGAMIN	2.0	1	9.07
CHEMBL269671	ARTEMISININ	3.0	1	7.81
CHEMBL416956	MEFLOQUINE	4.0	1	7.70
CHEMBL1083769	—	—	1	7.41

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1082723	CIPARGAMIN	IC50	=	0.85	nM	9.07
CHEMBL269671	ARTEMISININ	IC50	=	15.36	nM	7.81
CHEMBL416956	MEFLOQUINE	IC50	=	19.85	nM	7.70
CHEMBL1083769	—	IC50	=	39.2	nM	7.41