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Assay Detail

CHEMBL2327112

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Functional
Antimalarial activity against chloroquine-resistant Plasmodium falciparum K1 after 72 hrs by [3H]hypoxanthine incorporation assay
28
Total Activities
28
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 28 7.23 8.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2151383 1 8.66
CHEMBL269671 ARTEMISININ 3.0 1 8.55
CHEMBL2322218 1 8.03
CHEMBL2322220 1 7.92
CHEMBL2322213 1 7.67
CHEMBL2322221 1 7.66
CHEMBL2058009 1 7.53
CHEMBL2322224 1 7.52
CHEMBL2322510 1 7.41
CHEMBL2322223 1 7.31
CHEMBL2322216 1 6.95
CHEMBL2322212 1 6.95
CHEMBL2322505 1 6.91
CHEMBL2322509 1 6.84
CHEMBL2322508 1 6.84
CHEMBL76 CHLOROQUINE 4.0 1 6.68
CHEMBL2322222 1 6.50
CHEMBL115585 NEOCRYPTOLEPINE 1 5.77
CHEMBL484522 11-CHLORONEOCRYPTOLEPINE 1 5.70
CHEMBL2322214 1 -
CHEMBL2322215 1 -
CHEMBL2058024 1 -
CHEMBL2322507 1 -
CHEMBL2322506 1 -
CHEMBL2058015 1 -
CHEMBL2058020 1 -
CHEMBL2322217 1 -
CHEMBL2322219 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2151383 IC50 = 2.2 nM 8.66
CHEMBL269671 ARTEMISININ IC50 = 2.8 nM 8.55
CHEMBL2322218 IC50 = 9.4 nM 8.03
CHEMBL2322220 IC50 = 11.9 nM 7.92
CHEMBL2322213 IC50 = 21.3 nM 7.67
CHEMBL2322221 IC50 = 21.8 nM 7.66
CHEMBL2058009 IC50 = 29.6 nM 7.53
CHEMBL2322224 IC50 = 29.9 nM 7.52
CHEMBL2322510 IC50 = 38.8 nM 7.41
CHEMBL2322223 IC50 = 48.8 nM 7.31
CHEMBL2322216 IC50 = 111.5 nM 6.95
CHEMBL2322212 IC50 = 112.3 nM 6.95
CHEMBL2322505 IC50 = 123.7 nM 6.91
CHEMBL2322509 IC50 = 143.2 nM 6.84
CHEMBL2322508 IC50 = 143.7 nM 6.84
CHEMBL76 CHLOROQUINE IC50 = 209.5 nM 6.68
CHEMBL2322222 IC50 = 312.6 nM 6.50
CHEMBL115585 NEOCRYPTOLEPINE IC50 = 1696.0 nM 5.77
CHEMBL484522 11-CHLORONEOCRYPTOLEPINE IC50 = 1998.0 nM 5.70
CHEMBL2322214 IC50 - -
CHEMBL2322215 IC50 - -
CHEMBL2058024 IC50 - -
CHEMBL2322507 IC50 - -
CHEMBL2322506 IC50 - -
CHEMBL2058015 IC50 - -
CHEMBL2058020 IC50 - -
CHEMBL2322217 IC50 - -
CHEMBL2322219 IC50 - -