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Assay Detail

CHEMBL938342

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Functional
Antimicrobial activity against Trypanosoma brucei brucei clone 427-221a after 48 hrs
ChEMBL ↗
38
Total Activities
19
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Bis-acridines as lead antiparasitic agents: structure-activity analysis of a discrete compound library in vitro.
Caffrey CR, Steverding D, Swenerton RK, Kelly B, Walshe D, Debnath A, Zhou YM, Doyle PS, Fafarman AT, Zorn JA, Land KM, Beauchene J, Schreiber K, Moll H, Ponte-Sucre A, Schirmeister T, Saravanamuthu A, Fairlamb AH, Cohen FE, McKerrow JH, Weisman JL, May BC.
Antimicrob Agents Chemother (2007) 51 : 2164 -2172
PubMed 17371810 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 19 8.43 9.15
MIC 19 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL56640 — — 2 9.15
CHEMBL258727 — — 2 9.05
CHEMBL227559 — — 2 9.05
CHEMBL264512 — — 2 8.96
CHEMBL263380 — — 2 8.89
CHEMBL404610 — — 2 8.85
CHEMBL264145 — — 2 8.85
CHEMBL258944 — — 2 8.85
CHEMBL92547 — — 2 8.74
CHEMBL260934 — — 2 8.72
CHEMBL405356 — — 2 8.62
CHEMBL258645 — — 2 8.46
CHEMBL258675 — — 2 8.24
CHEMBL259289 — — 2 8.19
CHEMBL328742 — — 2 8.07
CHEMBL166 MELARSOPROL 3.0 2 7.80
CHEMBL329647 — — 2 7.60
CHEMBL264408 — — 2 7.51
CHEMBL90969 — — 2 6.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL56640 — EC50 = 0.7 nM 9.15
CHEMBL227559 — EC50 = 0.9 nM 9.05
CHEMBL258727 — EC50 = 0.9 nM 9.05
CHEMBL264512 — EC50 = 1.1 nM 8.96
CHEMBL263380 — EC50 = 1.3 nM 8.89
CHEMBL258944 — EC50 = 1.4 nM 8.85
CHEMBL404610 — EC50 = 1.4 nM 8.85
CHEMBL264145 — EC50 = 1.4 nM 8.85
CHEMBL92547 — EC50 = 1.8 nM 8.74
CHEMBL260934 — EC50 = 1.9 nM 8.72
CHEMBL405356 — EC50 = 2.4 nM 8.62
CHEMBL258645 — EC50 = 3.5 nM 8.46
CHEMBL258675 — EC50 = 5.8 nM 8.24
CHEMBL259289 — EC50 = 6.4 nM 8.19
CHEMBL328742 — EC50 = 8.6 nM 8.07
CHEMBL166 MELARSOPROL EC50 = 16.0 nM 7.80
CHEMBL329647 — EC50 = 25.0 nM 7.60
CHEMBL264408 — EC50 = 31.0 nM 7.51
CHEMBL90969 — EC50 = 218.0 nM 6.66
CHEMBL90969 — MIC = 10000.0 nM -
CHEMBL166 MELARSOPROL MIC = 100.0 nM -
CHEMBL264408 — MIC = 1000.0 nM -
CHEMBL404610 — MIC = 100.0 nM -
CHEMBL258675 — MIC = 1000.0 nM -
CHEMBL329647 — MIC = 1000.0 nM -
CHEMBL328742 — MIC = 1000.0 nM -
CHEMBL405356 — MIC = 1000.0 nM -
CHEMBL258645 — MIC = 1000.0 nM -
CHEMBL258727 — MIC = 1000.0 nM -
CHEMBL92547 — MIC = 100.0 nM -
CHEMBL258944 — MIC = 1000.0 nM -
CHEMBL264512 — MIC = 1000.0 nM -
CHEMBL56640 — MIC = 1000.0 nM -
CHEMBL263380 — MIC = 1000.0 nM -
CHEMBL259289 — MIC = 10000.0 nM -
CHEMBL260934 — MIC = 1000.0 nM -
CHEMBL264145 — MIC = 1000.0 nM -
CHEMBL227559 — MIC = 100.0 nM -