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Assay Detail

CHEMBL2343476

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

Functional
Antimalarial activity against erythrocytic stage of chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 assessed as inhibition of [3H]-hypoxanthine incorporation incubated for 48 hrs prior to [3H]-hypoxanthine addition measured after 24 hrs by liquid scintillation counting
63
Total Activities
63
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

Discovery and structure-activity relationships of pyrrolone antimalarials.
Murugesan D, Mital A, Kaiser M, Shackleford DM, Morizzi J, Katneni K, Campbell M, Hudson A, Charman SA, Yeates C, Gilbert IH.
J Med Chem (2013) 56 : 2975 -2990
PubMed 23517371 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 63 6.49 10.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL76 CHLOROQUINE 4.0 1 10.02
CHEMBL269671 ARTEMISININ 3.0 1 8.22
CHEMBL2335632 1 8.15
CHEMBL2335594 1 8.10
CHEMBL600928 1 8.05
CHEMBL2335990 1 7.72
CHEMBL2335611 1 7.70
CHEMBL2335991 1 7.68
CHEMBL2335592 1 7.58
CHEMBL2335989 1 7.57
CHEMBL2335595 1 7.54
CHEMBL2335987 1 7.50
CHEMBL2335986 1 7.42
CHEMBL2335597 1 7.35
CHEMBL2335629 1 7.30
CHEMBL2335591 1 7.20
CHEMBL2335988 1 7.19
CHEMBL1602168 1 7.19
CHEMBL2335600 1 7.15
CHEMBL2335607 1 7.11
CHEMBL2335606 1 7.05
CHEMBL2335993 1 7.02
CHEMBL2335604 1 6.92
CHEMBL2335590 1 6.89
CHEMBL2335602 1 6.72
CHEMBL2335609 1 6.72
CHEMBL2335622 1 6.57
CHEMBL2335618 1 6.54
CHEMBL2335628 1 6.52
CHEMBL2335605 1 6.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL76 CHLOROQUINE EC50 = 0.095 nM 10.02
CHEMBL269671 ARTEMISININ EC50 = 6.0 nM 8.22
CHEMBL2335632 EC50 = 7.0 nM 8.15
CHEMBL2335594 EC50 = 8.0 nM 8.10
CHEMBL600928 EC50 = 9.0 nM 8.05
CHEMBL2335990 EC50 = 19.0 nM 7.72
CHEMBL2335611 EC50 = 20.0 nM 7.70
CHEMBL2335991 EC50 = 21.0 nM 7.68
CHEMBL2335592 EC50 = 26.0 nM 7.58
CHEMBL2335989 EC50 = 27.0 nM 7.57
CHEMBL2335595 EC50 = 29.0 nM 7.54
CHEMBL2335987 EC50 = 32.0 nM 7.50
CHEMBL2335986 EC50 = 38.0 nM 7.42
CHEMBL2335597 EC50 = 45.0 nM 7.35
CHEMBL2335629 EC50 = 50.0 nM 7.30
CHEMBL2335591 EC50 = 63.0 nM 7.20
CHEMBL2335988 EC50 = 65.0 nM 7.19
CHEMBL1602168 EC50 = 65.0 nM 7.19
CHEMBL2335600 EC50 = 71.0 nM 7.15
CHEMBL2335607 EC50 = 77.0 nM 7.11
CHEMBL2335606 EC50 = 89.0 nM 7.05
CHEMBL2335993 EC50 = 95.0 nM 7.02
CHEMBL2335604 EC50 = 120.0 nM 6.92
CHEMBL2335590 EC50 = 130.0 nM 6.89
CHEMBL2335609 EC50 = 190.0 nM 6.72
CHEMBL2335602 EC50 = 190.0 nM 6.72
CHEMBL2335622 EC50 = 270.0 nM 6.57
CHEMBL2335618 EC50 = 290.0 nM 6.54
CHEMBL2335628 EC50 = 300.0 nM 6.52
CHEMBL2335605 EC50 = 300.0 nM 6.52
CHEMBL2335631 EC50 = 430.0 nM 6.37
CHEMBL2335610 EC50 = 470.0 nM 6.33
CHEMBL2335608 EC50 = 480.0 nM 6.32
CHEMBL2335620 EC50 = 550.0 nM 6.26
CHEMBL2335984 EC50 = 580.0 nM 6.24
CHEMBL2335633 EC50 = 620.0 nM 6.21
CHEMBL2335171 EC50 = 650.0 nM 6.19
CHEMBL2335613 EC50 = 820.0 nM 6.09
CHEMBL2335170 EC50 = 1000.0 nM 6.00
CHEMBL2335985 EC50 = 1000.0 nM 6.00
CHEMBL2335589 EC50 = 1300.0 nM 5.89
CHEMBL2335983 EC50 = 1400.0 nM 5.85
CHEMBL2335630 EC50 = 1500.0 nM 5.82
CHEMBL2335612 EC50 = 1500.0 nM 5.82
CHEMBL2335619 EC50 = 1600.0 nM 5.80
CHEMBL2335598 EC50 = 1600.0 nM 5.80
CHEMBL2335603 EC50 = 1700.0 nM 5.77
CHEMBL2335168 EC50 = 1700.0 nM 5.77
CHEMBL2335623 EC50 = 2100.0 nM 5.68
CHEMBL2335616 EC50 = 2100.0 nM 5.68