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Assay Detail

CHEMBL1020288

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Functional
Antiplasmodial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine uptake
9
Total Activities
9
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

Isoneocryptolepine, a synthetic indoloquinoline alkaloid, as an antiplasmodial lead compound.
Van Miert S, Hostyn S, Maes BU, Cimanga K, Brun R, Kaiser M, Mátyus P, Dommisse R, Lemière G, Vlietinck A, Pieters L.
J Nat Prod (2005) 68 : 674 -677
PubMed 15921407 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.60 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL463913 1 7.77
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE 1 6.92
CHEMBL512770 ISONEOCRYPTOLEPINE HYDROCHLORIDE 1 6.64
CHEMBL518720 BISCRYPTOLEPINE 1 6.57
CHEMBL502768 ISOCRYPTOLEPINE HYDROCHLORIDE 1 6.11
CHEMBL465591 NEOCRYPTOLEPINE HYDROCHLORIDE 1 5.58
CHEMBL463942 CRYPTOQUINDOLINE 1 -
CHEMBL76 CHLOROQUINE 4.0 1 -
CHEMBL269671 ARTEMISININ 3.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL463913 IC50 = 17.0 nM 7.77
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE IC50 = 120.0 nM 6.92
CHEMBL512770 ISONEOCRYPTOLEPINE HYDROCHLORIDE IC50 = 230.0 nM 6.64
CHEMBL518720 BISCRYPTOLEPINE IC50 = 270.0 nM 6.57
CHEMBL502768 ISOCRYPTOLEPINE HYDROCHLORIDE IC50 = 780.0 nM 6.11
CHEMBL465591 NEOCRYPTOLEPINE HYDROCHLORIDE IC50 = 2610.0 nM 5.58
CHEMBL463942 CRYPTOQUINDOLINE IC50 > 10000.0 nM -
CHEMBL76 CHLOROQUINE IC50 = 0.17 ug.mL-1 -
CHEMBL269671 ARTEMISININ IC50 = 0.042 ug.mL-1 -