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Assay Detail

CHEMBL4606261

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Functional
Antimalarial activity against multidrug resistant Plasmodium falciparum Dd2 infected in human erythrocytes measured after after 72 hrs by SYBR green dye based fluorescence assay
ChEMBL ↗
72
Total Activities
72
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

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 72 8.73 10.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4642651 — — 1 10.70
CHEMBL4643592 — — 1 10.42
CHEMBL4640537 — — 1 10.39
CHEMBL4647043 — — 1 10.35
CHEMBL4645747 — — 1 10.34
CHEMBL4649093 — — 1 10.33
CHEMBL4643264 — — 1 10.22
CHEMBL4644159 — — 1 10.20
CHEMBL4646921 — — 1 10.18
CHEMBL4639615 — — 1 10.11
CHEMBL1450 ATOVAQUONE 4.0 1 10.00
CHEMBL4634684 — — 1 9.92
CHEMBL4644592 — — 1 9.92
CHEMBL4632695 — — 1 9.85
CHEMBL4636890 — — 1 9.85
CHEMBL4641685 — — 1 9.77
CHEMBL4646969 — — 1 9.74
CHEMBL4643282 — — 1 9.72
CHEMBL4642414 — — 1 9.68
CHEMBL4646340 — — 1 9.60
CHEMBL4632424 — — 1 9.55
CHEMBL4640206 — — 1 9.51
CHEMBL4641129 — — 1 9.41
CHEMBL4649202 — — 1 9.38
CHEMBL4634780 — — 1 9.22
CHEMBL4637090 — — 1 9.12
CHEMBL4649060 — — 1 9.12
CHEMBL4634377 — — 1 9.08
CHEMBL4648872 — — 1 9.06
CHEMBL4642666 — — 1 8.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4642651 — IC50 = 0.02 nM 10.70
CHEMBL4643592 — IC50 = 0.038 nM 10.42
CHEMBL4640537 — IC50 = 0.041 nM 10.39
CHEMBL4647043 — IC50 = 0.045 nM 10.35
CHEMBL4645747 — IC50 = 0.046 nM 10.34
CHEMBL4649093 — IC50 = 0.047 nM 10.33
CHEMBL4643264 — IC50 = 0.06 nM 10.22
CHEMBL4644159 — IC50 = 0.063 nM 10.20
CHEMBL4646921 — IC50 = 0.066 nM 10.18
CHEMBL4639615 — IC50 = 0.078 nM 10.11
CHEMBL1450 ATOVAQUONE IC50 = 0.1 nM 10.00
CHEMBL4634684 — IC50 = 0.12 nM 9.92
CHEMBL4644592 — IC50 = 0.12 nM 9.92
CHEMBL4636890 — IC50 = 0.14 nM 9.85
CHEMBL4632695 — IC50 = 0.14 nM 9.85
CHEMBL4641685 — IC50 = 0.17 nM 9.77
CHEMBL4646969 — IC50 = 0.18 nM 9.74
CHEMBL4643282 — IC50 = 0.19 nM 9.72
CHEMBL4642414 — IC50 = 0.21 nM 9.68
CHEMBL4646340 — IC50 = 0.25 nM 9.60
CHEMBL4632424 — IC50 = 0.28 nM 9.55
CHEMBL4640206 — IC50 = 0.31 nM 9.51
CHEMBL4641129 — IC50 = 0.39 nM 9.41
CHEMBL4649202 — IC50 = 0.42 nM 9.38
CHEMBL4634780 — IC50 = 0.6 nM 9.22
CHEMBL4637090 — IC50 = 0.75 nM 9.12
CHEMBL4649060 — IC50 = 0.76 nM 9.12
CHEMBL4634377 — IC50 = 0.83 nM 9.08
CHEMBL4648872 — IC50 = 0.88 nM 9.06
CHEMBL4642666 — IC50 = 1.2 nM 8.92
CHEMBL4639326 — IC50 = 1.2 nM 8.92
CHEMBL4639240 — IC50 = 1.3 nM 8.89
CHEMBL4639323 — IC50 = 1.3 nM 8.89
CHEMBL4638186 — IC50 = 1.5 nM 8.82
CHEMBL4644361 — IC50 = 1.8 nM 8.74
CHEMBL4635811 — IC50 = 1.9 nM 8.72
CHEMBL4640720 — IC50 = 1.9 nM 8.72
CHEMBL4644082 — IC50 = 2.0 nM 8.70
CHEMBL4640006 — IC50 = 2.4 nM 8.62
CHEMBL4639209 — IC50 = 2.4 nM 8.62
CHEMBL4634180 — IC50 = 2.9 nM 8.54
CHEMBL4649716 — IC50 = 3.0 nM 8.52
CHEMBL4647566 — IC50 = 3.2 nM 8.49
CHEMBL4638013 — IC50 = 3.3 nM 8.48
CHEMBL4646227 — IC50 = 3.5 nM 8.46
CHEMBL4642934 — IC50 = 4.8 nM 8.32
CHEMBL4637212 — IC50 = 6.8 nM 8.17
CHEMBL4643150 — IC50 = 6.7 nM 8.17
CHEMBL4635459 — IC50 = 7.7 nM 8.11
CHEMBL4637990 — IC50 = 9.2 nM 8.04