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Assay Detail

CHEMBL4606273

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

Functional
Antimalarial activity against luciferase-expressing Plasmodium berghei ANKA 676m1cl1 sporozoites infected in human HepG2A16 cells measured after 45 hrs by luciferase-luciferin based reporter gene assay
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Plasmodium berghei (CHEMBL612653)
Type ORGANISM
Organism Plasmodium berghei

Publication

Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.
Kancharla P, Dodean RA, Li Y, Pou S, Pybus B, Melendez V, Read L, Bane CE, Vesely B, Kreishman-Deitrick M, Black C, Li Q, Sciotti RJ, Olmeda R, Luong TL, Gaona H, Potter B, Sousa J, Marcsisin S, Caridha D, Xie L, Vuong C, Zeng Q, Zhang J, Zhang P, Lin H, Butler K, Roncal N, Gaynor-Ohnstad L, Leed SE, Nolan C, Ceja FG, Rasmussen SA, Tumwebaze PK, Rosenthal PJ, Mu J, Bayles BR, Cooper RA, Reynolds KA, Smilkstein MJ, Riscoe MK, Kelly JX.
J Med Chem (2020) 63 : 6179 -6202
PubMed 32390431 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 67 7.64 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4642414 1 9.92
CHEMBL4638979 1 9.70
CHEMBL4644361 1 9.39
CHEMBL4640206 1 9.35
CHEMBL4643264 1 9.34
CHEMBL4640537 1 9.30
CHEMBL4641685 1 9.29
CHEMBL4646921 1 9.22
CHEMBL4632816 1 9.19
CHEMBL4649202 1 9.15
CHEMBL4638013 1 8.82
CHEMBL4639249 1 8.80
CHEMBL4639615 1 8.77
CHEMBL4634377 1 8.66
CHEMBL4634684 1 8.62
CHEMBL4639326 1 8.36
CHEMBL4647043 1 8.35
CHEMBL4640162 1 8.33
CHEMBL4641224 1 8.25
CHEMBL4637212 1 8.23
CHEMBL4649093 1 8.23
CHEMBL1450 ATOVAQUONE 4.0 1 8.19
CHEMBL4642666 1 8.17
CHEMBL4632424 1 8.13
CHEMBL4649060 1 8.13
CHEMBL4644159 1 8.12
CHEMBL4645747 1 8.10
CHEMBL4634780 1 8.09
CHEMBL4641129 1 7.85
CHEMBL4639240 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4642414 IC50 = 0.12 nM 9.92
CHEMBL4638979 IC50 = 0.2 nM 9.70
CHEMBL4644361 IC50 = 0.41 nM 9.39
CHEMBL4640206 IC50 = 0.45 nM 9.35
CHEMBL4643264 IC50 = 0.46 nM 9.34
CHEMBL4640537 IC50 = 0.5 nM 9.30
CHEMBL4641685 IC50 = 0.51 nM 9.29
CHEMBL4646921 IC50 = 0.6 nM 9.22
CHEMBL4632816 IC50 = 0.64 nM 9.19
CHEMBL4649202 IC50 = 0.7 nM 9.15
CHEMBL4638013 IC50 = 1.5 nM 8.82
CHEMBL4639249 IC50 = 1.6 nM 8.80
CHEMBL4639615 IC50 = 1.7 nM 8.77
CHEMBL4634377 IC50 = 2.2 nM 8.66
CHEMBL4634684 IC50 = 2.4 nM 8.62
CHEMBL4639326 IC50 = 4.4 nM 8.36
CHEMBL4647043 IC50 = 4.5 nM 8.35
CHEMBL4640162 IC50 = 4.7 nM 8.33
CHEMBL4641224 IC50 = 5.6 nM 8.25
CHEMBL4637212 IC50 = 5.9 nM 8.23
CHEMBL4649093 IC50 = 5.9 nM 8.23
CHEMBL1450 ATOVAQUONE IC50 = 6.5 nM 8.19
CHEMBL4642666 IC50 = 6.8 nM 8.17
CHEMBL4632424 IC50 = 7.4 nM 8.13
CHEMBL4649060 IC50 = 7.4 nM 8.13
CHEMBL4644159 IC50 = 7.5 nM 8.12
CHEMBL4645747 IC50 = 8.0 nM 8.10
CHEMBL4634780 IC50 = 8.2 nM 8.09
CHEMBL4641129 IC50 = 14.0 nM 7.85
CHEMBL4639240 IC50 = 15.0 nM 7.82
CHEMBL4643592 IC50 = 17.0 nM 7.77
CHEMBL4643150 IC50 = 26.0 nM 7.58
CHEMBL4643282 IC50 = 29.0 nM 7.54
CHEMBL4646969 IC50 = 32.0 nM 7.50
CHEMBL4642934 IC50 = 36.0 nM 7.44
CHEMBL4648872 IC50 = 37.0 nM 7.43
CHEMBL4634180 IC50 = 41.0 nM 7.39
CHEMBL4637990 IC50 = 48.0 nM 7.32
CHEMBL4635811 IC50 = 52.0 nM 7.28
CHEMBL4642508 IC50 = 59.0 nM 7.23
CHEMBL4639209 IC50 = 66.0 nM 7.18
CHEMBL4635459 IC50 = 66.0 nM 7.18
CHEMBL4648905 IC50 = 66.0 nM 7.18
CHEMBL4640006 IC50 = 69.0 nM 7.16
CHEMBL4636824 IC50 = 73.0 nM 7.14
CHEMBL4637090 IC50 = 84.0 nM 7.08
CHEMBL4644082 IC50 = 86.0 nM 7.07
CHEMBL4642651 IC50 = 86.0 nM 7.07
CHEMBL4632642 IC50 = 98.0 nM 7.01
CHEMBL4638186 IC50 = 109.0 nM 6.96