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Assay Detail

CHEMBL2393747

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Functional
Antimalarial activity against chloroquine-sensitive erythrocytic stage of Plasmodium falciparum NF54 infected in human red blood cells assessed as growth inhibition after 48 hrs by [3H]-hypoxanthine incorporation assay
29
Total Activities
29
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

Synthesis and antimalarial testing of neocryptolepine analogues: addition of ester function in SAR study of 2,11-disubstituted indolo[2,3-b]quinolines.
Lu WJ, Wicht KJ, Wang L, Imai K, Mei ZW, Kaiser M, El Sayed Iel T, Egan TJ, Inokuchi T.
Eur J Med Chem (2013) 64 : 498 -511
PubMed 23685569 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 7.49 8.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2391095 1 8.74
CHEMBL2391090 1 8.67
CHEMBL2391088 1 8.64
CHEMBL2391094 1 8.38
CHEMBL2391089 1 8.34
CHEMBL2391087 1 8.25
CHEMBL2391097 1 8.22
CHEMBL2391086 1 8.15
CHEMBL2391248 1 8.12
CHEMBL2391243 1 8.09
CHEMBL2391246 1 8.08
CHEMBL76 CHLOROQUINE 4.0 1 8.03
CHEMBL2391247 1 8.02
CHEMBL2391242 1 7.87
CHEMBL2391096 1 7.84
CHEMBL2391241 1 7.84
CHEMBL2391240 1 7.78
CHEMBL2391249 1 7.61
CHEMBL2391252 1 7.48
CHEMBL2391251 1 7.37
CHEMBL2391250 1 7.25
CHEMBL2058009 1 7.10
CHEMBL2391253 1 6.56
CHEMBL2391244 1 6.12
CHEMBL115585 NEOCRYPTOLEPINE 1 5.80
CHEMBL2391091 1 5.77
CHEMBL2391245 1 5.75
CHEMBL2391093 1 5.67
CHEMBL2391092 1 5.59

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2391095 IC50 = 1.81 nM 8.74
CHEMBL2391090 IC50 = 2.16 nM 8.67
CHEMBL2391088 IC50 = 2.27 nM 8.64
CHEMBL2391094 IC50 = 4.16 nM 8.38
CHEMBL2391089 IC50 = 4.54 nM 8.34
CHEMBL2391087 IC50 = 5.59 nM 8.25
CHEMBL2391097 IC50 = 6.03 nM 8.22
CHEMBL2391086 IC50 = 7.15 nM 8.15
CHEMBL2391248 IC50 = 7.57 nM 8.12
CHEMBL2391243 IC50 = 8.05 nM 8.09
CHEMBL2391246 IC50 = 8.28 nM 8.08
CHEMBL76 CHLOROQUINE IC50 = 9.4 nM 8.03
CHEMBL2391247 IC50 = 9.52 nM 8.02
CHEMBL2391242 IC50 = 13.6 nM 7.87
CHEMBL2391096 IC50 = 14.5 nM 7.84
CHEMBL2391241 IC50 = 14.4 nM 7.84
CHEMBL2391240 IC50 = 16.7 nM 7.78
CHEMBL2391249 IC50 = 24.8 nM 7.61
CHEMBL2391252 IC50 = 33.3 nM 7.48
CHEMBL2391251 IC50 = 42.5 nM 7.37
CHEMBL2391250 IC50 = 55.8 nM 7.25
CHEMBL2058009 IC50 = 78.8 nM 7.10
CHEMBL2391253 IC50 = 278.0 nM 6.56
CHEMBL2391244 IC50 = 750.0 nM 6.12
CHEMBL115585 NEOCRYPTOLEPINE IC50 = 1580.0 nM 5.80
CHEMBL2391091 IC50 = 1690.0 nM 5.77
CHEMBL2391245 IC50 = 1770.0 nM 5.75
CHEMBL2391093 IC50 = 2160.0 nM 5.67
CHEMBL2391092 IC50 = 2550.0 nM 5.59