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Assay Detail

CHEMBL4023799

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

Functional
Antileishmanial activity against Leishmania donovani amastigotes expressing Luc gene infected in mouse J774A.1 cells by luciferase reporter gene assay
42
Total Activities
42
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Leishmania donovani
Confidence 1 — Organism
Curated By Autocuration

Target

Leishmania donovani (CHEMBL367)
Type ORGANISM
Organism Leishmania donovani

Publication

Development of (6 R)-2-Nitro-6-[4-(trifluoromethoxy)phenoxy]-6,7-dihydro-5 H-imidazo[2,1- b][1,3]oxazine (DNDI-8219): A New Lead for Visceral Leishmaniasis.
Thompson AM, O'Connor PD, Marshall AJ, Blaser A, Yardley V, Maes L, Gupta S, Launay D, Braillard S, Chatelain E, Wan B, Franzblau SG, Ma Z, Cooper CB, Denny WA.
J Med Chem (2018) 61 : 2329 -2352
PubMed 29461823 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 42 6.19 7.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067816 1 7.22
CHEMBL4097686 1 6.92
CHEMBL4093258 1 6.85
CHEMBL4090381 1 6.82
CHEMBL4092525 1 6.77
CHEMBL4064066 1 6.75
CHEMBL4102643 1 6.75
CHEMBL4078293 1 6.72
CHEMBL4061728 1 6.68
CHEMBL4068473 1 6.64
CHEMBL3608844 1 6.64
CHEMBL4098597 1 6.62
CHEMBL4063124 1 6.58
CHEMBL4065592 1 6.57
CHEMBL4071737 1 6.51
CHEMBL4061272 1 6.51
CHEMBL572070 1 6.44
CHEMBL4086552 1 6.41
CHEMBL450548 1 6.41
CHEMBL1836005 1 6.41
CHEMBL3608846 1 6.34
CHEMBL4073834 1 6.32
CHEMBL4084773 1 6.20
CHEMBL4067944 1 6.19
CHEMBL4087531 1 6.11
CHEMBL4097042 1 6.11
CHEMBL4095234 1 6.07
CHEMBL4102045 1 6.07
CHEMBL480375 1 5.96
CHEMBL4095902 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067816 IC50 = 60.0 nM 7.22
CHEMBL4097686 IC50 = 120.0 nM 6.92
CHEMBL4093258 IC50 = 140.0 nM 6.85
CHEMBL4090381 IC50 = 150.0 nM 6.82
CHEMBL4092525 IC50 = 170.0 nM 6.77
CHEMBL4064066 IC50 = 180.0 nM 6.75
CHEMBL4102643 IC50 = 180.0 nM 6.75
CHEMBL4078293 IC50 = 190.0 nM 6.72
CHEMBL4061728 IC50 = 210.0 nM 6.68
CHEMBL4068473 IC50 = 230.0 nM 6.64
CHEMBL3608844 IC50 = 230.0 nM 6.64
CHEMBL4098597 IC50 = 240.0 nM 6.62
CHEMBL4063124 IC50 = 260.0 nM 6.58
CHEMBL4065592 IC50 = 270.0 nM 6.57
CHEMBL4061272 IC50 = 310.0 nM 6.51
CHEMBL4071737 IC50 = 310.0 nM 6.51
CHEMBL572070 IC50 = 360.0 nM 6.44
CHEMBL4086552 IC50 = 390.0 nM 6.41
CHEMBL450548 IC50 = 390.0 nM 6.41
CHEMBL1836005 IC50 = 390.0 nM 6.41
CHEMBL3608846 IC50 = 460.0 nM 6.34
CHEMBL4073834 IC50 = 480.0 nM 6.32
CHEMBL4084773 IC50 = 630.0 nM 6.20
CHEMBL4067944 IC50 = 640.0 nM 6.19
CHEMBL4087531 IC50 = 780.0 nM 6.11
CHEMBL4097042 IC50 = 770.0 nM 6.11
CHEMBL4095234 IC50 = 860.0 nM 6.07
CHEMBL4102045 IC50 = 860.0 nM 6.07
CHEMBL480375 IC50 = 1100.0 nM 5.96
CHEMBL4095902 IC50 = 1200.0 nM 5.92
CHEMBL4065114 IC50 = 1400.0 nM 5.85
CHEMBL1836062 IC50 = 1700.0 nM 5.77
CHEMBL3608850 IC50 = 2000.0 nM 5.70
CHEMBL3608849 IC50 = 2600.0 nM 5.58
CHEMBL1946794 IC50 = 3300.0 nM 5.48
CHEMBL227875 PRETOMANID IC50 = 3900.0 nM 5.41
CHEMBL4105398 IC50 = 4800.0 nM 5.32
CHEMBL4091750 IC50 = 5500.0 nM 5.26
CHEMBL4076532 IC50 = 28000.0 nM 4.55
CHEMBL4070883 IC50 = 78000.0 nM 4.11
CHEMBL4067141 IC50 > 2000.0 nM -
CHEMBL4088403 IC50 > 2000.0 nM -