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Assay Detail

CHEMBL1067384

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antimalarial activity against chloroquine and pyrimethamine-resistant Plasmodium falciparum K1 by [3H]hypoxanthine incorporation assay
27
Total Activities
27
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

Structure-activity relationship of antiparasitic and cytotoxic indoloquinoline alkaloids, and their tricyclic and bicyclic analogues.
Van Baelen G, Hostyn S, Dhooghe L, Tapolcsányi P, Mátyus P, Lemière G, Dommisse R, Kaiser M, Brun R, Cos P, Maes L, Hajós G, Riedl Z, Nagy I, Maes BU, Pieters L.
Bioorg Med Chem (2009) 17 : 7209 -7217
PubMed 19781948 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.80 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL593792 1 7.50
CHEMBL607530 1 7.40
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE 1 6.92
CHEMBL512770 ISONEOCRYPTOLEPINE HYDROCHLORIDE 1 6.64
CHEMBL76 CHLOROQUINE 4.0 1 6.62
CHEMBL455600 1 6.47
CHEMBL593231 1 6.42
CHEMBL594240 1 6.35
CHEMBL367738 1 6.32
CHEMBL594246 1 6.24
CHEMBL593930 1 6.19
CHEMBL502768 ISOCRYPTOLEPINE HYDROCHLORIDE 1 6.11
CHEMBL408157 1 5.68
CHEMBL596112 1 5.62
CHEMBL465591 NEOCRYPTOLEPINE HYDROCHLORIDE 1 5.58
CHEMBL593018 1 5.50
CHEMBL593073 1 5.19
CHEMBL594030 1 5.11
CHEMBL593688 1 4.89
CHEMBL608989 1 4.87
CHEMBL593094 1 4.83
CHEMBL595665 1 4.75
CHEMBL593072 1 4.72
CHEMBL609575 1 4.63
CHEMBL593929 1 4.53
CHEMBL594467 1 -
CHEMBL594400 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL593792 IC50 = 32.0 nM 7.50
CHEMBL607530 IC50 = 40.0 nM 7.40
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE IC50 = 120.0 nM 6.92
CHEMBL512770 ISONEOCRYPTOLEPINE HYDROCHLORIDE IC50 = 230.0 nM 6.64
CHEMBL76 CHLOROQUINE IC50 = 240.0 nM 6.62
CHEMBL455600 IC50 = 340.0 nM 6.47
CHEMBL593231 IC50 = 380.0 nM 6.42
CHEMBL594240 IC50 = 450.0 nM 6.35
CHEMBL367738 IC50 = 480.0 nM 6.32
CHEMBL594246 IC50 = 570.0 nM 6.24
CHEMBL593930 IC50 = 640.0 nM 6.19
CHEMBL502768 ISOCRYPTOLEPINE HYDROCHLORIDE IC50 = 780.0 nM 6.11
CHEMBL408157 IC50 = 2100.0 nM 5.68
CHEMBL596112 IC50 = 2400.0 nM 5.62
CHEMBL465591 NEOCRYPTOLEPINE HYDROCHLORIDE IC50 = 2610.0 nM 5.58
CHEMBL593018 IC50 = 3200.0 nM 5.50
CHEMBL593073 IC50 = 6400.0 nM 5.19
CHEMBL594030 IC50 = 7800.0 nM 5.11
CHEMBL593688 IC50 = 13000.0 nM 4.89
CHEMBL608989 IC50 = 13400.0 nM 4.87
CHEMBL593094 IC50 = 14700.0 nM 4.83
CHEMBL595665 IC50 = 17600.0 nM 4.75
CHEMBL593072 IC50 = 19000.0 nM 4.72
CHEMBL609575 IC50 = 23200.0 nM 4.63
CHEMBL593929 IC50 = 29300.0 nM 4.53
CHEMBL594467 IC50 > 37000.0 nM -
CHEMBL594400 IC50 > 37000.0 nM -