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Assay Detail

CHEMBL2045537

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Functional
Antitrypanosomal activity against Trypanosoma brucei rhodesiense STIB900 infected in rat L6 cells after 72 hrs by alamar blue assay
85
Total Activities
85
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma brucei rhodesiense
Cell Type L6
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma brucei rhodesiense (CHEMBL612348)
Type ORGANISM
Organism Trypanosoma brucei rhodesiense

Publication

Synthesis and structure-activity analysis of new phosphonium salts with potent activity against African trypanosomes.
Taladriz A, Healy A, Flores Pérez EJ, Herrero García V, Ríos Martínez C, Alkhaldi AA, Eze AA, Kaiser M, de Koning HP, Chana A, Dardonville C.
J Med Chem (2012) 55 : 2606 -2622
PubMed 22390399 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 85 6.29 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2041843 1 8.70
CHEMBL166 MELARSOPROL 3.0 1 8.12
CHEMBL2041616 1 7.85
CHEMBL2041820 1 7.57
CHEMBL2041823 1 7.30
CHEMBL2041825 1 7.20
CHEMBL2041821 1 7.14
CHEMBL2041842 1 7.09
CHEMBL2041824 1 7.09
CHEMBL2041822 1 7.08
CHEMBL2041973 1 7.08
CHEMBL2041617 1 7.00
CHEMBL2041818 1 6.99
CHEMBL2041805 1 6.96
CHEMBL2041807 1 6.95
CHEMBL2041624 1 6.85
CHEMBL2041845 1 6.82
CHEMBL601068 1 6.80
CHEMBL2041828 1 6.80
CHEMBL2041826 1 6.77
CHEMBL2041827 1 6.76
CHEMBL2041806 1 6.75
CHEMBL601708 1 6.71
CHEMBL2041619 1 6.70
CHEMBL2041795 1 6.70
CHEMBL2041618 1 6.68
CHEMBL2041840 1 6.67
CHEMBL590266 1 6.66
CHEMBL2041972 1 6.66
CHEMBL2041829 1 6.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2041843 EC50 = 2.0 nM 8.70
CHEMBL166 MELARSOPROL EC50 = 7.5 nM 8.12
CHEMBL2041616 EC50 = 14.0 nM 7.85
CHEMBL2041820 EC50 = 27.0 nM 7.57
CHEMBL2041823 EC50 = 50.0 nM 7.30
CHEMBL2041825 EC50 = 63.0 nM 7.20
CHEMBL2041821 EC50 = 73.0 nM 7.14
CHEMBL2041842 EC50 = 81.0 nM 7.09
CHEMBL2041824 EC50 = 81.0 nM 7.09
CHEMBL2041822 EC50 = 84.0 nM 7.08
CHEMBL2041973 EC50 = 84.0 nM 7.08
CHEMBL2041617 EC50 = 99.0 nM 7.00
CHEMBL2041818 EC50 = 103.0 nM 6.99
CHEMBL2041805 EC50 = 109.0 nM 6.96
CHEMBL2041807 EC50 = 112.0 nM 6.95
CHEMBL2041624 EC50 = 142.0 nM 6.85
CHEMBL2041845 EC50 = 153.0 nM 6.82
CHEMBL601068 EC50 = 160.0 nM 6.80
CHEMBL2041828 EC50 = 159.0 nM 6.80
CHEMBL2041826 EC50 = 170.0 nM 6.77
CHEMBL2041827 EC50 = 173.0 nM 6.76
CHEMBL2041806 EC50 = 180.0 nM 6.75
CHEMBL601708 EC50 = 197.0 nM 6.71
CHEMBL2041619 EC50 = 200.0 nM 6.70
CHEMBL2041795 EC50 = 200.0 nM 6.70
CHEMBL2041618 EC50 = 209.0 nM 6.68
CHEMBL2041840 EC50 = 216.0 nM 6.67
CHEMBL590266 EC50 = 220.0 nM 6.66
CHEMBL2041972 EC50 = 220.0 nM 6.66
CHEMBL2041829 EC50 = 231.0 nM 6.64
CHEMBL2041620 EC50 = 230.0 nM 6.64
CHEMBL601066 EC50 = 260.0 nM 6.58
CHEMBL590505 EC50 = 260.0 nM 6.58
CHEMBL2041815 EC50 = 267.0 nM 6.57
CHEMBL2041844 EC50 = 274.0 nM 6.56
CHEMBL2041831 EC50 = 290.0 nM 6.54
CHEMBL539632 EC50 = 289.0 nM 6.54
CHEMBL2041621 EC50 = 290.0 nM 6.54
CHEMBL2041838 EC50 = 299.0 nM 6.52
CHEMBL590385 EC50 = 320.0 nM 6.50
CHEMBL2041811 EC50 = 326.0 nM 6.49
CHEMBL601706 EC50 = 355.0 nM 6.45
CHEMBL2041841 EC50 = 364.0 nM 6.44
CHEMBL2041839 EC50 = 384.0 nM 6.42
CHEMBL2041817 EC50 = 376.0 nM 6.42
CHEMBL2041837 EC50 = 400.0 nM 6.40
CHEMBL2041623 EC50 = 410.0 nM 6.39
CHEMBL2041796 EC50 = 430.0 nM 6.37
CHEMBL2041622 EC50 = 450.0 nM 6.35
CHEMBL2041832 EC50 = 480.0 nM 6.32