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Assay Detail

CHEMBL4140740

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiparasitic activity against Leishmania major amastigotes infected in mouse RAW 264.7 cells after 96 hrs by luciferase reporter gene assay
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania major
Confidence 1 — Organism
Curated By Intermediate

Target

Leishmania major (CHEMBL612879)
Type ORGANISM
Organism Leishmania major

Publication

Optimization of physicochemical properties for 4-anilinoquinazoline inhibitors of trypanosome proliferation.
Woodring JL, Bachovchin KA, Brady KG, Gallerstein MF, Erath J, Tanghe S, Leed SE, Rodriguez A, Mensa-Wilmot K, Sciotti RJ, Pollastri MP.
Eur J Med Chem (2017) 141 : 446 -459
PubMed 29049963 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 36 4.94 6.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168740 1 6.17
CHEMBL4164550 1 5.73
CHEMBL4162775 1 5.30
CHEMBL4171831 1 5.28
CHEMBL4172435 1 5.20
CHEMBL4165142 1 5.18
CHEMBL3637894 1 5.09
CHEMBL4163364 1 5.06
CHEMBL4177159 1 4.90
CHEMBL4176839 1 4.64
CHEMBL4163176 1 4.62
CHEMBL4166222 1 4.62
CHEMBL4173481 1 4.60
CHEMBL4171216 1 4.59
CHEMBL4171319 1 4.59
CHEMBL4160723 1 4.59
CHEMBL4160939 1 4.59
CHEMBL4173041 1 4.59
CHEMBL4161711 1 4.59
CHEMBL4176605 1 -
CHEMBL4169642 1 -
CHEMBL4171096 1 -
CHEMBL4175838 1 -
CHEMBL4171684 1 -
CHEMBL4161076 1 -
CHEMBL4175127 1 -
CHEMBL4160007 1 -
CHEMBL4159864 1 -
CHEMBL4173238 1 -
CHEMBL4176462 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168740 EC50 = 670.0 nM 6.17
CHEMBL4164550 EC50 = 1880.0 nM 5.73
CHEMBL4162775 EC50 = 4960.0 nM 5.30
CHEMBL4171831 EC50 = 5220.0 nM 5.28
CHEMBL4172435 EC50 = 6340.0 nM 5.20
CHEMBL4165142 EC50 = 6600.0 nM 5.18
CHEMBL3637894 EC50 = 8110.0 nM 5.09
CHEMBL4163364 EC50 = 8780.0 nM 5.06
CHEMBL4177159 EC50 = 12500.0 nM 4.90
CHEMBL4176839 EC50 = 22700.0 nM 4.64
CHEMBL4163176 EC50 = 23900.0 nM 4.62
CHEMBL4166222 EC50 = 24130.0 nM 4.62
CHEMBL4173481 EC50 = 25090.0 nM 4.60
CHEMBL4171319 EC50 = 25950.0 nM 4.59
CHEMBL4160723 EC50 = 25880.0 nM 4.59
CHEMBL4160939 EC50 = 25950.0 nM 4.59
CHEMBL4173041 EC50 = 25610.0 nM 4.59
CHEMBL4161711 EC50 = 25680.0 nM 4.59
CHEMBL4171216 EC50 = 25880.0 nM 4.59
CHEMBL4167924 EC50 > 15000.0 nM -
CHEMBL4164489 EC50 > 15000.0 nM -
CHEMBL4171268 EC50 > 15000.0 nM -
CHEMBL4166390 EC50 > 15000.0 nM -
CHEMBL4177008 EC50 > 15000.0 nM -
CHEMBL4169813 EC50 > 15000.0 nM -
CHEMBL4176462 EC50 > 15000.0 nM -
CHEMBL4173238 EC50 > 15000.0 nM -
CHEMBL4159864 EC50 > 15000.0 nM -
CHEMBL4160007 EC50 > 15000.0 nM -
CHEMBL4175127 EC50 > 15000.0 nM -
CHEMBL4161076 EC50 > 15000.0 nM -
CHEMBL4171684 EC50 > 15000.0 nM -
CHEMBL4175838 EC50 > 15000.0 nM -
CHEMBL4171096 EC50 > 3000.0 nM -
CHEMBL4169642 EC50 > 15000.0 nM -
CHEMBL4176605 EC50 > 15000.0 nM -