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Assay Detail

CHEMBL3603054

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Functional
Trypanocidal activity against bloodstream form of Trypanosoma brucei 221 assessed as inhibition of parasite growth at pH 7.4 after 48 hrs by Spectramax plate reader analysis
ChEMBL ↗
64
Total Activities
32
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei (CHEMBL612849) ↗
Type ORGANISM
Organism Trypanosoma brucei

Publication

Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity.
Sola I, Castellà S, Viayna E, Galdeano C, Taylor MC, Gbedema SY, Pérez B, Clos MV, Jones DC, Fairlamb AH, Wright CW, Kelly JM, Muñoz-Torrero D.
Bioorg Med Chem (2015) 23 : 5156 -5167
PubMed 25678015 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC90 32 - -
IC50 32 6.54 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3600468 — — 2 6.92
CHEMBL2021630 — — 2 6.85
CHEMBL255056 — — 2 6.82
CHEMBL3600464 — — 2 6.77
CHEMBL2021659 — — 2 6.77
CHEMBL252424 — — 2 6.77
CHEMBL3600554 — — 2 6.68
CHEMBL2021640 — — 2 6.68
CHEMBL3600553 — — 2 6.62
CHEMBL401339 — — 2 6.62
CHEMBL2021669 — — 2 6.62
CHEMBL3600467 — — 2 6.58
CHEMBL401273 — — 2 6.57
CHEMBL3600549 — — 2 6.57
CHEMBL1186370 — — 2 6.55
CHEMBL400544 — — 2 6.55
CHEMBL2021632 — — 2 6.54
CHEMBL3600466 — — 2 6.54
CHEMBL3600465 — — 2 6.54
CHEMBL1186058 — — 2 6.52
CHEMBL252753 — — 2 6.50
CHEMBL3600550 — — 2 6.47
CHEMBL3600555 — — 2 6.47
CHEMBL3600551 — — 2 6.46
CHEMBL1187001 — — 2 6.42
CHEMBL1187082 — — 2 6.39
CHEMBL410770 — — 2 6.33
CHEMBL3600463 — — 2 6.31
CHEMBL3600556 — — 2 6.26
CHEMBL401340 — — 2 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3600468 — IC50 = 120.0 nM 6.92
CHEMBL2021630 — IC50 = 140.0 nM 6.85
CHEMBL255056 — IC50 = 150.0 nM 6.82
CHEMBL3600464 — IC50 = 170.0 nM 6.77
CHEMBL2021659 — IC50 = 170.0 nM 6.77
CHEMBL252424 — IC50 = 170.0 nM 6.77
CHEMBL2021640 — IC50 = 210.0 nM 6.68
CHEMBL3600554 — IC50 = 210.0 nM 6.68
CHEMBL2021669 — IC50 = 240.0 nM 6.62
CHEMBL401339 — IC50 = 240.0 nM 6.62
CHEMBL3600553 — IC50 = 240.0 nM 6.62
CHEMBL3600467 — IC50 = 260.0 nM 6.58
CHEMBL401273 — IC50 = 270.0 nM 6.57
CHEMBL3600549 — IC50 = 270.0 nM 6.57
CHEMBL400544 — IC50 = 280.0 nM 6.55
CHEMBL1186370 — IC50 = 280.0 nM 6.55
CHEMBL3600465 — IC50 = 290.0 nM 6.54
CHEMBL3600466 — IC50 = 290.0 nM 6.54
CHEMBL2021632 — IC50 = 290.0 nM 6.54
CHEMBL1186058 — IC50 = 300.0 nM 6.52
CHEMBL252753 — IC50 = 320.0 nM 6.50
CHEMBL3600550 — IC50 = 340.0 nM 6.47
CHEMBL3600555 — IC50 = 340.0 nM 6.47
CHEMBL3600551 — IC50 = 350.0 nM 6.46
CHEMBL1187001 — IC50 = 380.0 nM 6.42
CHEMBL1187082 — IC50 = 410.0 nM 6.39
CHEMBL410770 — IC50 = 470.0 nM 6.33
CHEMBL3600463 — IC50 = 490.0 nM 6.31
CHEMBL3600556 — IC50 = 550.0 nM 6.26
CHEMBL401340 — IC50 = 560.0 nM 6.25
CHEMBL3600552 — IC50 = 590.0 nM 6.23
CHEMBL1187774 — IC50 = 970.0 nM 6.01
CHEMBL3600549 — IC90 = 660.0 nM -
CHEMBL1187001 — IC90 = 790.0 nM -
CHEMBL255056 — IC90 = 290.0 nM -
CHEMBL401273 — IC90 = 430.0 nM -
CHEMBL400544 — IC90 = 400.0 nM -
CHEMBL252424 — IC90 = 460.0 nM -
CHEMBL2021669 — IC90 = 520.0 nM -
CHEMBL2021659 — IC90 = 490.0 nM -
CHEMBL3600463 — IC90 = 1180.0 nM -
CHEMBL3600464 — IC90 = 350.0 nM -
CHEMBL401340 — IC90 = 790.0 nM -
CHEMBL1186058 — IC90 = 680.0 nM -
CHEMBL1186370 — IC90 = 620.0 nM -
CHEMBL1187082 — IC90 = 880.0 nM -
CHEMBL3600467 — IC90 = 1330.0 nM -
CHEMBL3600466 — IC90 = 720.0 nM -
CHEMBL3600465 — IC90 = 700.0 nM -
CHEMBL3600468 — IC90 = 170.0 nM -