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Assay Detail

CHEMBL1776673

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

Functional
Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum Dd2 by FACS-based assay
16
Total Activities
16
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

Enone- and chalcone-chloroquinoline hybrid analogues: in silico guided design, synthesis, antiplasmodial activity, in vitro metabolism, and mechanistic studies.
Guantai EM, Ncokazi K, Egan TJ, Gut J, Rosenthal PJ, Bhampidipati R, Kopinathan A, Smith PJ, Chibale K.
J Med Chem (2011) 54 : 3637 -3649
PubMed 21500839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.06 7.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1290314 1 7.16
CHEMBL76 CHLOROQUINE 4.0 1 7.01
CHEMBL1774611 1 6.30
CHEMBL1774609 1 6.30
CHEMBL1774607 1 6.30
CHEMBL1289100 1 6.16
CHEMBL236696 1 6.05
CHEMBL1774606 1 6.00
CHEMBL31000 1 6.00
CHEMBL1774605 1 5.96
CHEMBL1774604 1 5.82
CHEMBL1774608 1 5.77
CHEMBL1774610 1 5.51
CHEMBL1774603 1 5.42
CHEMBL1774602 1 5.14
CHEMBL106509 DEHYDROZINGERONE 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1290314 IC50 = 70.0 nM 7.16
CHEMBL76 CHLOROQUINE IC50 = 97.0 nM 7.01
CHEMBL1774611 IC50 = 500.0 nM 6.30
CHEMBL1774609 IC50 = 500.0 nM 6.30
CHEMBL1774607 IC50 = 500.0 nM 6.30
CHEMBL1289100 IC50 = 700.0 nM 6.16
CHEMBL236696 IC50 = 900.0 nM 6.05
CHEMBL1774606 IC50 = 1000.0 nM 6.00
CHEMBL31000 IC50 = 1000.0 nM 6.00
CHEMBL1774605 IC50 = 1100.0 nM 5.96
CHEMBL1774604 IC50 = 1500.0 nM 5.82
CHEMBL1774608 IC50 = 1700.0 nM 5.77
CHEMBL1774610 IC50 = 3100.0 nM 5.51
CHEMBL1774603 IC50 = 3800.0 nM 5.42
CHEMBL1774602 IC50 = 7300.0 nM 5.14
CHEMBL106509 DEHYDROZINGERONE IC50 > 20000.0 nM -