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Assay Detail

CHEMBL1066769

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

Functional
Antitrypanosomal activity against Trypanosoma cruzi
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368)
Type ORGANISM
Organism Trypanosoma cruzi

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 5.00 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE 1 6.66
CHEMBL110 BENZNIDAZOLE 4.0 1 5.90
CHEMBL502768 ISOCRYPTOLEPINE HYDROCHLORIDE 1 5.90
CHEMBL594246 1 5.82
CHEMBL593930 1 5.78
CHEMBL465591 NEOCRYPTOLEPINE HYDROCHLORIDE 1 5.70
CHEMBL593792 1 4.92
CHEMBL512770 ISONEOCRYPTOLEPINE HYDROCHLORIDE 1 4.68
CHEMBL607530 1 4.68
CHEMBL594030 1 4.39
CHEMBL593688 1 4.19
CHEMBL609575 1 4.16
CHEMBL593018 1 4.12
CHEMBL593073 1 4.09
CHEMBL593094 1 4.05
CHEMBL595665 1 -
CHEMBL594240 1 -
CHEMBL408157 1 -
CHEMBL367738 1 -
CHEMBL593072 1 -
CHEMBL608989 1 -
CHEMBL593929 1 -
CHEMBL594467 1 -
CHEMBL594400 1 -
CHEMBL455600 1 -
CHEMBL596112 1 -
CHEMBL593231 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92129 CRYPTOLEPINE HYDROCHLORIDE IC50 = 220.0 nM 6.66
CHEMBL110 BENZNIDAZOLE IC50 = 1250.0 nM 5.90
CHEMBL502768 ISOCRYPTOLEPINE HYDROCHLORIDE IC50 = 1270.0 nM 5.90
CHEMBL594246 IC50 = 1530.0 nM 5.82
CHEMBL593930 IC50 = 1660.0 nM 5.78
CHEMBL465591 NEOCRYPTOLEPINE HYDROCHLORIDE IC50 = 2010.0 nM 5.70
CHEMBL593792 IC50 = 11900.0 nM 4.92
CHEMBL512770 ISONEOCRYPTOLEPINE HYDROCHLORIDE IC50 = 21000.0 nM 4.68
CHEMBL607530 IC50 = 20700.0 nM 4.68
CHEMBL594030 IC50 = 40900.0 nM 4.39
CHEMBL593688 IC50 = 64500.0 nM 4.19
CHEMBL609575 IC50 = 69600.0 nM 4.16
CHEMBL593018 IC50 = 76800.0 nM 4.12
CHEMBL593073 IC50 = 81000.0 nM 4.09
CHEMBL593094 IC50 = 89200.0 nM 4.05
CHEMBL595665 IC50 > 115000.0 nM -
CHEMBL594240 IC50 > 160000.0 nM -
CHEMBL408157 IC50 > 160000.0 nM -
CHEMBL367738 IC50 > 160000.0 nM -
CHEMBL593072 IC50 > 225000.0 nM -
CHEMBL608989 IC50 > 225000.0 nM -
CHEMBL593929 IC50 > 225000.0 nM -
CHEMBL594467 IC50 > 225000.0 nM -
CHEMBL594400 IC50 > 225000.0 nM -
CHEMBL455600 IC50 > 95000.0 nM -
CHEMBL596112 IC50 > 95000.0 nM -
CHEMBL593231 IC50 > 95000.0 nM -