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Assay Detail

CHEMBL4718759

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Functional
Antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 strain blood stream forms incubated for 48 hrs by resazurin dye based fluorescence assay
ChEMBL ↗
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides.
Russell S,Rahmani R,Jones AJ,Newson HL,Neilde K,Cotillo I,Rahmani Khajouei M,Ferrins L,Qureishi S,Nguyen N,Martinez-Martinez MS,Weaver DF,Kaiser M,Riley J,Thomas J,De Rycker M,Read KD,Flematti GR,Ryan E,Tanghe S,Rodriguez A,Charman SA,Kessler A,Avery VM,Baell JB,Piggott MJ
J Med Chem (2016) 59 : 9686 -9720
PubMed 27548560 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 72 6.11 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4745633 — — 1 7.80
CHEMBL4759398 — — 1 7.62
CHEMBL4756928 — — 1 7.62
CHEMBL4756063 — — 1 7.58
CHEMBL3798895 — — 1 7.55
CHEMBL3800137 — — 1 7.30
CHEMBL3797352 — — 1 7.04
CHEMBL3800541 — — 1 6.89
CHEMBL4797356 — — 1 6.89
CHEMBL4793195 — — 1 6.80
CHEMBL4754246 — — 1 6.72
CHEMBL3797262 — — 1 6.72
CHEMBL4744957 — — 1 6.66
CHEMBL3797221 — — 1 6.64
CHEMBL1872842 — — 1 6.60
CHEMBL2093262 — — 1 6.60
CHEMBL4741752 — — 1 6.58
CHEMBL4749722 — — 1 6.55
CHEMBL4758947 — — 1 6.52
CHEMBL4782902 — — 1 6.52
CHEMBL3799413 — — 1 6.51
CHEMBL4763710 — — 1 6.48
CHEMBL1499901 — — 1 6.46
CHEMBL4742943 — — 1 6.46
CHEMBL4793100 — — 1 6.41
CHEMBL3799915 — — 1 6.38
CHEMBL1459740 — — 1 6.33
CHEMBL4762697 — — 1 6.30
CHEMBL4744383 — — 1 6.25
CHEMBL4749036 — — 1 6.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4745633 — IC50 = 16.0 nM 7.80
CHEMBL4759398 — IC50 = 24.0 nM 7.62
CHEMBL4756928 — IC50 = 24.0 nM 7.62
CHEMBL4756063 — IC50 = 26.0 nM 7.58
CHEMBL3798895 — IC50 = 28.0 nM 7.55
CHEMBL3800137 — IC50 = 50.0 nM 7.30
CHEMBL3797352 — IC50 = 91.0 nM 7.04
CHEMBL3800541 — IC50 = 130.0 nM 6.89
CHEMBL4797356 — IC50 = 130.0 nM 6.89
CHEMBL4793195 — IC50 = 160.0 nM 6.80
CHEMBL4754246 — IC50 = 190.0 nM 6.72
CHEMBL3797262 — IC50 = 190.0 nM 6.72
CHEMBL4744957 — IC50 = 220.0 nM 6.66
CHEMBL3797221 — IC50 = 230.0 nM 6.64
CHEMBL2093262 — IC50 = 250.0 nM 6.60
CHEMBL1872842 — IC50 = 250.0 nM 6.60
CHEMBL4741752 — IC50 = 260.0 nM 6.58
CHEMBL4749722 — IC50 = 280.0 nM 6.55
CHEMBL4758947 — IC50 = 300.0 nM 6.52
CHEMBL4782902 — IC50 = 300.0 nM 6.52
CHEMBL3799413 — IC50 = 310.0 nM 6.51
CHEMBL4763710 — IC50 = 330.0 nM 6.48
CHEMBL1499901 — IC50 = 350.0 nM 6.46
CHEMBL4742943 — IC50 = 350.0 nM 6.46
CHEMBL4793100 — IC50 = 390.0 nM 6.41
CHEMBL3799915 — IC50 = 420.0 nM 6.38
CHEMBL1459740 — IC50 = 470.0 nM 6.33
CHEMBL4762697 — IC50 = 500.0 nM 6.30
CHEMBL4744383 — IC50 = 560.0 nM 6.25
CHEMBL4749036 — IC50 = 670.0 nM 6.17
CHEMBL3797773 — IC50 = 690.0 nM 6.16
CHEMBL4748388 — IC50 = 740.0 nM 6.13
CHEMBL4750943 — IC50 = 760.0 nM 6.12
CHEMBL3799188 — IC50 = 760.0 nM 6.12
CHEMBL3797350 — IC50 = 770.0 nM 6.11
CHEMBL1541044 — IC50 = 800.0 nM 6.10
CHEMBL4758077 — IC50 = 900.0 nM 6.05
CHEMBL4743734 — IC50 = 970.0 nM 6.01
CHEMBL3797763 — IC50 = 1100.0 nM 5.96
CHEMBL4740927 — IC50 = 1100.0 nM 5.96
CHEMBL4796530 — IC50 = 1200.0 nM 5.92
CHEMBL3798596 — IC50 = 1500.0 nM 5.82
CHEMBL4762283 — IC50 = 1500.0 nM 5.82
CHEMBL3799815 — IC50 = 1500.0 nM 5.82
CHEMBL3800098 — IC50 = 1600.0 nM 5.80
CHEMBL4793805 — IC50 = 1700.0 nM 5.77
CHEMBL4760866 — IC50 = 1900.0 nM 5.72
CHEMBL4748161 — IC50 = 1900.0 nM 5.72
CHEMBL4783918 — IC50 = 2300.0 nM 5.64
CHEMBL4747949 — IC50 = 2400.0 nM 5.62