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Assay Detail

CHEMBL2033738

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 48 hrs by alamar blue assay
35
Total Activities
35
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 33 5.90 8.59
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL166 MELARSOPROL 3.0 1 8.59
CHEMBL361506 PENTAMIDINE ISETHIONATE 4.0 1 8.54
CHEMBL2031131 1 7.33
CHEMBL413376 SURAMIN HEXASODIUM 3.0 1 6.51
CHEMBL2031127 1 6.27
CHEMBL2031128 1 6.17
CHEMBL2031130 1 6.17
CHEMBL2031123 1 6.12
CHEMBL2031121 1 6.11
CHEMBL2031118 1 5.99
CHEMBL2031122 1 5.97
CHEMBL2031124 1 5.96
CHEMBL2031120 1 5.64
CHEMBL2031119 1 5.56
CHEMBL2031126 1 5.51
CHEMBL2031125 1 5.51
CHEMBL2031117 1 5.34
CHEMBL2031129 1 5.27
CHEMBL2031108 1 5.14
CHEMBL2031116 1 5.05
CHEMBL2031112 1 4.84
CHEMBL2031114 1 4.76
CHEMBL2031113 1 4.72
CHEMBL1201037 EFLORNITHINE HYDROCHLORIDE 4.0 1 4.64
CHEMBL2031110 1 -
CHEMBL2031109 1 -
CHEMBL2031111 1 -
CHEMBL2031107 1 -
CHEMBL2031106 1 -
CHEMBL2031105 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL166 MELARSOPROL IC50 = 2.6 nM 8.59
CHEMBL361506 PENTAMIDINE ISETHIONATE IC50 = 2.9 nM 8.54
CHEMBL2031131 IC50 = 47.0 nM 7.33
CHEMBL413376 SURAMIN HEXASODIUM IC50 = 310.0 nM 6.51
CHEMBL2031127 IC50 = 540.0 nM 6.27
CHEMBL2031128 IC50 = 670.0 nM 6.17
CHEMBL2031130 IC50 = 680.0 nM 6.17
CHEMBL2031123 IC50 = 750.0 nM 6.12
CHEMBL2031121 IC50 = 780.0 nM 6.11
CHEMBL2031118 IC50 = 1030.0 nM 5.99
CHEMBL2031122 IC50 = 1070.0 nM 5.97
CHEMBL2031124 IC50 = 1090.0 nM 5.96
CHEMBL2031120 IC50 = 2280.0 nM 5.64
CHEMBL2031119 IC50 = 2750.0 nM 5.56
CHEMBL2031125 IC50 = 3070.0 nM 5.51
CHEMBL2031126 IC50 = 3090.0 nM 5.51
CHEMBL2031117 IC50 = 4600.0 nM 5.34
CHEMBL2031129 IC50 = 5400.0 nM 5.27
CHEMBL2031108 IC50 = 7310.0 nM 5.14
CHEMBL2031116 IC50 = 8890.0 nM 5.05
CHEMBL2031112 IC50 = 14600.0 nM 4.84
CHEMBL2031114 IC50 = 17200.0 nM 4.76
CHEMBL2031113 IC50 = 19200.0 nM 4.72
CHEMBL1201037 EFLORNITHINE HYDROCHLORIDE IC50 = 22900.0 nM 4.64
CHEMBL2031132 IC50 > 40000.0 nM -
CHEMBL2031115 IC50 > 40000.0 nM -
CHEMBL550018 IC50 > 40000.0 nM -
CHEMBL1958275 Activity - -
CHEMBL2031104 Activity - -
CHEMBL2031105 IC50 > 40000.0 nM -
CHEMBL2031106 IC50 > 40000.0 nM -
CHEMBL2031107 IC50 > 40000.0 nM -
CHEMBL2031111 IC50 > 40000.0 nM -
CHEMBL2031109 IC50 > 40000.0 nM -
CHEMBL2031110 IC50 > 40000.0 nM -