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Assay Detail

CHEMBL5368798

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Functional
Antitrypanosomal activity against blood stream form of Trypanosoma brucei 221a variant assessed as parasite growth inhibition measured after 48 hrs by resazurin dye based fluorescence analysis
ChEMBL ↗
44
Total Activities
22
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

Bis-6-amidino-benzothiazole Derivative that Cures Experimental Stage 1 African Trypanosomiasis with a Single Dose.
Racané L, Ptiček L, Kostrun S, Raić-Malić S, Taylor MC, Delves M, Alsford S, Olmo F, Francisco AF, Kelly JM.
J Med Chem (2023) 66 : 13043 -13057
PubMed 37722077 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 22 6.56 9.00
EC90 22 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5425887 — — 2 9.00
CHEMBL5417161 — — 2 7.92
CHEMBL5399066 — — 2 7.68
CHEMBL5404790 — — 2 7.55
CHEMBL5410902 — — 2 7.20
CHEMBL5400545 — — 2 7.01
CHEMBL5432670 — — 2 7.00
CHEMBL5416356 — — 2 6.72
CHEMBL5396341 — — 2 6.72
CHEMBL5405752 — — 2 6.62
CHEMBL5430502 — — 2 6.60
CHEMBL5430418 — — 2 6.47
CHEMBL5396205 — — 2 6.13
CHEMBL5394795 — — 2 6.09
CHEMBL5396323 — — 2 6.05
CHEMBL5416172 — — 2 5.94
CHEMBL5420181 — — 2 5.83
CHEMBL5412493 — — 2 5.81
CHEMBL1631694 FEXINIDAZOLE 4.0 2 5.62
CHEMBL5401969 — — 2 5.62
CHEMBL5415516 — — 2 5.44
CHEMBL5416542 — — 2 5.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5425887 — EC50 = 1.0 nM 9.00
CHEMBL5417161 — EC50 = 12.0 nM 7.92
CHEMBL5399066 — EC50 = 21.0 nM 7.68
CHEMBL5404790 — EC50 = 28.0 nM 7.55
CHEMBL5410902 — EC50 = 63.0 nM 7.20
CHEMBL5400545 — EC50 = 98.0 nM 7.01
CHEMBL5432670 — EC50 = 100.0 nM 7.00
CHEMBL5416356 — EC50 = 190.0 nM 6.72
CHEMBL5396341 — EC50 = 190.0 nM 6.72
CHEMBL5405752 — EC50 = 240.0 nM 6.62
CHEMBL5430502 — EC50 = 250.0 nM 6.60
CHEMBL5430418 — EC50 = 340.0 nM 6.47
CHEMBL5396205 — EC50 = 740.0 nM 6.13
CHEMBL5394795 — EC50 = 820.0 nM 6.09
CHEMBL5396323 — EC50 = 890.0 nM 6.05
CHEMBL5416172 — EC50 = 1140.0 nM 5.94
CHEMBL5420181 — EC50 = 1490.0 nM 5.83
CHEMBL5412493 — EC50 = 1560.0 nM 5.81
CHEMBL1631694 FEXINIDAZOLE EC50 = 2400.0 nM 5.62
CHEMBL5401969 — EC50 = 2380.0 nM 5.62
CHEMBL5415516 — EC50 = 3640.0 nM 5.44
CHEMBL5416542 — EC50 = 5390.0 nM 5.27
CHEMBL5430502 — EC90 = 0.4 uM -
CHEMBL5415516 — EC90 = 7.82 uM -
CHEMBL5401969 — EC90 = 3.48 uM -
CHEMBL5430418 — EC90 = 0.75 uM -
CHEMBL5416542 — EC90 = 9.01 uM -
CHEMBL5410902 — EC90 = 0.131 uM -
CHEMBL5416172 — EC90 = 1.87 uM -
CHEMBL5396341 — EC90 = 0.31 uM -
CHEMBL5400545 — EC90 = 0.145 uM -
CHEMBL5412493 — EC90 = 2.11 uM -
CHEMBL5396323 — EC90 = 1.52 uM -
CHEMBL5394795 — EC90 = 1.88 uM -
CHEMBL5404790 — EC90 = 0.056 uM -
CHEMBL5396205 — EC90 = 1.39 uM -
CHEMBL5420181 — EC90 = 2.52 uM -
CHEMBL5425887 — EC90 = 0.001 uM -
CHEMBL5405752 — EC90 = 0.49 uM -
CHEMBL5399066 — EC90 = 0.031 uM -
CHEMBL5417161 — EC90 = 0.022 uM -
CHEMBL5416356 — EC90 = 0.68 uM -
CHEMBL5432670 — EC90 = 0.16 uM -
CHEMBL1631694 FEXINIDAZOLE EC90 = 4.51 uM -