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Assay Detail

CHEMBL2327114

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Functional
Antimalarial activity against chloroquine-sensitive Plasmodium falciparum NF54 after 72 hrs by [3H]hypoxanthine incorporation assay
30
Total Activities
30
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 in vitro antimalarial testing of neocryptolepines: SAR study for improved activity by introduction and modifications of side chains at C2 and C11 on indolo[2,3-b]quinolines.
Mei ZW, Wang L, Lu WJ, Pang CQ, Maeda T, Peng W, Kaiser M, El Sayed I, Inokuchi T.
J Med Chem (2013) 56 : 1431 -1442
PubMed 23360309 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 30 7.57 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2322224 1 8.68
CHEMBL2322221 1 8.66
CHEMBL2322220 1 8.40
CHEMBL2322223 1 8.39
CHEMBL269671 ARTEMISININ 3.0 1 8.37
CHEMBL2151383 1 8.36
CHEMBL2322216 1 8.04
CHEMBL76 CHLOROQUINE 4.0 1 8.03
CHEMBL2058020 1 7.98
CHEMBL2322507 1 7.97
CHEMBL2322504 1 7.94
CHEMBL2058015 1 7.93
CHEMBL2322214 1 7.85
CHEMBL2322218 1 7.67
CHEMBL2322222 1 7.60
CHEMBL2322219 1 7.59
CHEMBL2322213 1 7.58
CHEMBL2322212 1 7.42
CHEMBL2322506 1 7.30
CHEMBL2322510 1 7.28
CHEMBL2322509 1 7.26
CHEMBL2322505 1 7.20
CHEMBL2322508 1 7.19
CHEMBL2058024 1 7.13
CHEMBL2058009 1 7.10
CHEMBL2322503 1 7.01
CHEMBL2322217 1 6.98
CHEMBL2322215 1 6.59
CHEMBL115585 NEOCRYPTOLEPINE 1 5.80
CHEMBL484522 11-CHLORONEOCRYPTOLEPINE 1 5.69

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2322224 IC50 = 2.1 nM 8.68
CHEMBL2322221 IC50 = 2.2 nM 8.66
CHEMBL2322220 IC50 = 4.0 nM 8.40
CHEMBL2322223 IC50 = 4.1 nM 8.39
CHEMBL269671 ARTEMISININ IC50 = 4.3 nM 8.37
CHEMBL2151383 IC50 = 4.4 nM 8.36
CHEMBL2322216 IC50 = 9.1 nM 8.04
CHEMBL76 CHLOROQUINE IC50 = 9.4 nM 8.03
CHEMBL2058020 IC50 = 10.4 nM 7.98
CHEMBL2322507 IC50 = 10.7 nM 7.97
CHEMBL2322504 IC50 = 11.4 nM 7.94
CHEMBL2058015 IC50 = 11.8 nM 7.93
CHEMBL2322214 IC50 = 14.2 nM 7.85
CHEMBL2322218 IC50 = 21.3 nM 7.67
CHEMBL2322222 IC50 = 24.9 nM 7.60
CHEMBL2322219 IC50 = 25.8 nM 7.59
CHEMBL2322213 IC50 = 26.6 nM 7.58
CHEMBL2322212 IC50 = 38.1 nM 7.42
CHEMBL2322506 IC50 = 49.6 nM 7.30
CHEMBL2322510 IC50 = 52.4 nM 7.28
CHEMBL2322509 IC50 = 54.9 nM 7.26
CHEMBL2322505 IC50 = 63.0 nM 7.20
CHEMBL2322508 IC50 = 63.9 nM 7.19
CHEMBL2058024 IC50 = 74.8 nM 7.13
CHEMBL2058009 IC50 = 78.8 nM 7.10
CHEMBL2322503 IC50 = 98.1 nM 7.01
CHEMBL2322217 IC50 = 104.1 nM 6.98
CHEMBL2322215 IC50 = 258.1 nM 6.59
CHEMBL115585 NEOCRYPTOLEPINE IC50 = 1580.0 nM 5.80
CHEMBL484522 11-CHLORONEOCRYPTOLEPINE IC50 = 2055.0 nM 5.69