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Assay Detail

CHEMBL4706783

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

Functional
Antiplasmodial activity against Plasmodium falciparum 3D7 infected in RBC assessed as reduction in parasitemia incubated for 72 hrs by SYBR green dye-based assay
34
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium falciparum (CHEMBL364)
Type ORGANISM
Organism Plasmodium falciparum

Publication

Tetrahydro-2-naphthyl and 2-Indanyl Triazolopyrimidines Targeting Plasmodium falciparum Dihydroorotate Dehydrogenase Display Potent and Selective Antimalarial Activity.
Kokkonda S,Deng X,White KL,Coteron JM,Marco M,de Las Heras L,White J,El Mazouni F,Tomchick DR,Manjalanagara K,Rudra KR,Chen G,Morizzi J,Ryan E,Kaminsky W,Leroy D,Martínez-Martínez MS,Jimenez-Diaz MB,Bazaga SF,Angulo-Barturen I,Waterson D,Burrows JN,Matthews D,Charman SA,Phillips MA,Rathod PK
J Med Chem (2016) 59 : 5416 -5431
PubMed 27127993 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 34 7.29 9.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4753862 2 9.41
CHEMBL4790441 1 9.41
CHEMBL4751920 1 8.92
CHEMBL4747214 2 8.59
CHEMBL4751321 1 8.55
CHEMBL4761666 2 8.42
CHEMBL4760735 1 8.37
CHEMBL1956285 DSM-265 2.0 1 8.37
CHEMBL4740960 1 8.12
CHEMBL4741128 1 7.77
CHEMBL3689094 1 7.68
CHEMBL4760917 2 7.66
CHEMBL4744317 2 7.60
CHEMBL4750037 2 7.48
CHEMBL4784152 1 7.44
CHEMBL4794107 1 7.40
CHEMBL4791257 1 7.34
CHEMBL4740342 1 7.19
CHEMBL4797521 1 7.18
CHEMBL4777941 1 7.01
CHEMBL4784677 1 6.92
CHEMBL4797946 1 6.82
CHEMBL4754938 1 6.24
CHEMBL4756700 1 6.23
CHEMBL4764723 1 5.55
CHEMBL4764319 1 5.48
CHEMBL4746414 1 5.19
CHEMBL4748163 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4753862 EC50 = 0.39 nM 9.41
CHEMBL4790441 EC50 = 0.39 nM 9.41
CHEMBL4751920 EC50 = 1.2 nM 8.92
CHEMBL4747214 EC50 = 2.6 nM 8.59
CHEMBL4751321 EC50 = 2.8 nM 8.55
CHEMBL4761666 EC50 = 3.8 nM 8.42
CHEMBL1956285 DSM-265 EC50 = 4.3 nM 8.37
CHEMBL4760735 EC50 = 4.3 nM 8.37
CHEMBL4740960 EC50 = 7.5 nM 8.12
CHEMBL4741128 EC50 = 17.0 nM 7.77
CHEMBL3689094 EC50 = 21.0 nM 7.68
CHEMBL4760917 EC50 = 22.0 nM 7.66
CHEMBL4744317 EC50 = 25.0 nM 7.60
CHEMBL4750037 EC50 = 33.0 nM 7.48
CHEMBL4784152 EC50 = 36.0 nM 7.44
CHEMBL4794107 EC50 = 40.0 nM 7.40
CHEMBL4791257 EC50 = 46.0 nM 7.34
CHEMBL4740342 EC50 = 64.0 nM 7.19
CHEMBL4797521 EC50 = 66.0 nM 7.18
CHEMBL4777941 EC50 = 97.0 nM 7.01
CHEMBL4784677 EC50 = 120.0 nM 6.92
CHEMBL4747214 EC50 = 140.0 nM 6.85
CHEMBL4797946 EC50 = 150.0 nM 6.82
CHEMBL4761666 EC50 = 420.0 nM 6.38
CHEMBL4754938 EC50 = 580.0 nM 6.24
CHEMBL4756700 EC50 = 590.0 nM 6.23
CHEMBL4744317 EC50 = 640.0 nM 6.19
CHEMBL4753862 EC50 = 1400.0 nM 5.85
CHEMBL4750037 EC50 = 1500.0 nM 5.82
CHEMBL4764723 EC50 = 2800.0 nM 5.55
CHEMBL4764319 EC50 = 3300.0 nM 5.48
CHEMBL4746414 EC50 = 6500.0 nM 5.19
CHEMBL4748163 EC50 - -
CHEMBL4760917 EC50 > 2500.0 nM -