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Assay Detail

CHEMBL814915

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

Assay Information

Assay Type Functional
Organism Trypanosoma brucei
Confidence 1 — Organism
Curated By Expert

Target

Trypanosoma brucei (CHEMBL612849)
Type ORGANISM
Organism Trypanosoma brucei

Publication

Synthesis, cytotoxicity, and antiplasmodial and antitrypanosomal activity of new neocryptolepine derivatives.
Jonckers TH, van Miert S, Cimanga K, Bailly C, Colson P, De Pauw-Gillet MC, van den Heuvel H, Claeys M, Lemière F, Esmans EL, Rozenski J, Quirijnen L, Maes L, Dommisse R, Lemière GL, Vlietinck A, Pieters L.
J Med Chem (2002) 45 : 3497 -3508
PubMed 12139461 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 5.67 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL333481 1 7.00
CHEMBL119649 1 6.52
CHEMBL118915 1 6.40
CHEMBL443023 1 6.16
CHEMBL432423 1 6.10
CHEMBL118340 1 6.00
CHEMBL117926 1 6.00
CHEMBL440898 1 6.00
CHEMBL117064 1 5.89
CHEMBL118916 1 5.89
CHEMBL119096 CRYPTOLEPINE 1 5.52
CHEMBL119102 1 5.40
CHEMBL118066 1 5.40
CHEMBL115585 NEOCRYPTOLEPINE 1 5.40
CHEMBL118838 1 5.03
CHEMBL118855 1 4.84
CHEMBL118165 1 4.78
CHEMBL115433 1 4.78
CHEMBL332478 1 4.56
CHEMBL118343 1 -
CHEMBL332113 1 -
CHEMBL331251 1 -
CHEMBL119834 1 -
CHEMBL119475 1 -
CHEMBL117831 1 -
CHEMBL323909 1 -
CHEMBL115592 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL333481 IC50 = 100.0 nM 7.00
CHEMBL119649 IC50 = 300.0 nM 6.52
CHEMBL118915 IC50 = 400.0 nM 6.40
CHEMBL443023 IC50 = 700.0 nM 6.16
CHEMBL432423 IC50 = 800.0 nM 6.10
CHEMBL118340 IC50 = 1000.0 nM 6.00
CHEMBL117926 IC50 = 1000.0 nM 6.00
CHEMBL440898 IC50 = 1000.0 nM 6.00
CHEMBL117064 IC50 = 1300.0 nM 5.89
CHEMBL118916 IC50 = 1300.0 nM 5.89
CHEMBL119096 CRYPTOLEPINE IC50 = 3000.0 nM 5.52
CHEMBL119102 IC50 = 4000.0 nM 5.40
CHEMBL118066 IC50 = 4000.0 nM 5.40
CHEMBL115585 NEOCRYPTOLEPINE IC50 = 4000.0 nM 5.40
CHEMBL118838 IC50 = 9300.0 nM 5.03
CHEMBL118855 IC50 = 14300.0 nM 4.84
CHEMBL118165 IC50 = 16700.0 nM 4.78
CHEMBL115433 IC50 = 16700.0 nM 4.78
CHEMBL332478 IC50 = 27300.0 nM 4.56
CHEMBL118343 IC50 > 32000.0 nM -
CHEMBL332113 IC50 > 32000.0 nM -
CHEMBL331251 IC50 > 32000.0 nM -
CHEMBL119834 IC50 > 32000.0 nM -
CHEMBL119475 IC50 > 32000.0 nM -
CHEMBL117831 IC50 > 32000.0 nM -
CHEMBL323909 IC50 > 32000.0 nM -
CHEMBL115592 IC50 > 32000.0 nM -