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Assay Detail

CHEMBL2033737

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei TC221 infected in mouse J774.1 cells after 72 hrs by alamar blue assay
31
Total Activities
31
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei brucei
Cell Type J774.1
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Synthesis and structure-activity relationships of new quinolone-type molecules against Trypanosoma brucei.
Hiltensperger G, Jones NG, Niedermeier S, Stich A, Kaiser M, Jung J, Puhl S, Damme A, Braunschweig H, Meinel L, Engstler M, Holzgrabe U.
J Med Chem (2012) 55 : 2538 -2548
PubMed 22376072 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 29 5.53 7.30
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2031131 1 7.30
CHEMBL2031127 1 6.24
CHEMBL2031130 1 6.04
CHEMBL2031128 1 5.98
CHEMBL2031123 1 5.90
CHEMBL2031121 1 5.84
CHEMBL2031118 1 5.74
CHEMBL2031122 1 5.72
CHEMBL2031124 1 5.70
CHEMBL2031119 1 5.59
CHEMBL2031120 1 5.51
CHEMBL2031125 1 5.38
CHEMBL2031117 1 5.32
CHEMBL2031126 1 5.29
CHEMBL2031108 1 5.20
CHEMBL2031129 1 4.97
CHEMBL2031116 1 4.92
CHEMBL2031112 1 4.74
CHEMBL2031113 1 4.65
CHEMBL2031114 1 4.64
CHEMBL1958275 1 -
CHEMBL2031104 1 -
CHEMBL2031105 1 -
CHEMBL2031106 1 -
CHEMBL2031107 1 -
CHEMBL2031109 1 -
CHEMBL2031110 1 -
CHEMBL2031111 1 -
CHEMBL550018 1 -
CHEMBL2031115 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2031131 IC50 = 50.0 nM 7.30
CHEMBL2031127 IC50 = 580.0 nM 6.24
CHEMBL2031130 IC50 = 920.0 nM 6.04
CHEMBL2031128 IC50 = 1040.0 nM 5.98
CHEMBL2031123 IC50 = 1250.0 nM 5.90
CHEMBL2031121 IC50 = 1450.0 nM 5.84
CHEMBL2031118 IC50 = 1840.0 nM 5.74
CHEMBL2031122 IC50 = 1910.0 nM 5.72
CHEMBL2031124 IC50 = 1980.0 nM 5.70
CHEMBL2031119 IC50 = 2560.0 nM 5.59
CHEMBL2031120 IC50 = 3120.0 nM 5.51
CHEMBL2031125 IC50 = 4140.0 nM 5.38
CHEMBL2031117 IC50 = 4840.0 nM 5.32
CHEMBL2031126 IC50 = 5120.0 nM 5.29
CHEMBL2031108 IC50 = 6370.0 nM 5.20
CHEMBL2031129 IC50 = 10770.0 nM 4.97
CHEMBL2031116 IC50 = 12100.0 nM 4.92
CHEMBL2031112 IC50 = 18100.0 nM 4.74
CHEMBL2031113 IC50 = 22200.0 nM 4.65
CHEMBL2031114 IC50 = 23000.0 nM 4.64
CHEMBL1958275 Activity - -
CHEMBL2031104 Activity - -
CHEMBL2031105 IC50 > 40000.0 nM -
CHEMBL2031106 IC50 > 40000.0 nM -
CHEMBL2031107 IC50 > 40000.0 nM -
CHEMBL2031109 IC50 > 40000.0 nM -
CHEMBL2031110 IC50 > 40000.0 nM -
CHEMBL2031111 IC50 > 40000.0 nM -
CHEMBL550018 IC50 > 40000.0 nM -
CHEMBL2031115 IC50 > 40000.0 nM -
CHEMBL2031132 IC50 > 40000.0 nM -