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Assay Detail

CHEMBL4023801

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Functional
Antitrypanosomal activity against Trypanosoma cruzi infected in human MRC5 cells after 7 days by alpha-galactosidase reporter gene assay
ChEMBL ↗
92
Total Activities
92
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368) ↗
Type ORGANISM
Organism Trypanosoma cruzi

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 92 6.07 7.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4083135 — — 1 7.60
CHEMBL4098597 — — 1 7.37
CHEMBL4084065 — — 1 7.14
CHEMBL4065592 — — 1 7.11
CHEMBL4102045 — — 1 7.11
CHEMBL4100270 — — 1 7.08
CHEMBL4077167 — — 1 6.96
CHEMBL4076665 — — 1 6.96
CHEMBL4095902 — — 1 6.92
CHEMBL4061272 — — 1 6.92
CHEMBL4085479 — — 1 6.82
CHEMBL4074828 — — 1 6.82
CHEMBL4078293 — — 1 6.82
CHEMBL4065239 — — 1 6.82
CHEMBL4064066 — — 1 6.80
CHEMBL4073834 — — 1 6.72
CHEMBL4100987 — — 1 6.70
CHEMBL4086552 — — 1 6.64
CHEMBL4094416 — — 1 6.62
CHEMBL4067816 — — 1 6.60
CHEMBL4079653 — — 1 6.58
CHEMBL4097042 — — 1 6.57
CHEMBL4105533 — — 1 6.57
CHEMBL4065114 — — 1 6.57
CHEMBL4065451 — — 1 6.57
CHEMBL4062862 — — 1 6.55
CHEMBL4100012 — — 1 6.52
CHEMBL4090795 — — 1 6.51
CHEMBL4090381 — — 1 6.47
CHEMBL4062393 — — 1 6.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4083135 — IC50 = 25.0 nM 7.60
CHEMBL4098597 — IC50 = 43.0 nM 7.37
CHEMBL4084065 — IC50 = 72.0 nM 7.14
CHEMBL4065592 — IC50 = 78.0 nM 7.11
CHEMBL4102045 — IC50 = 78.0 nM 7.11
CHEMBL4100270 — IC50 = 84.0 nM 7.08
CHEMBL4077167 — IC50 = 110.0 nM 6.96
CHEMBL4076665 — IC50 = 110.0 nM 6.96
CHEMBL4095902 — IC50 = 120.0 nM 6.92
CHEMBL4061272 — IC50 = 120.0 nM 6.92
CHEMBL4085479 — IC50 = 150.0 nM 6.82
CHEMBL4074828 — IC50 = 150.0 nM 6.82
CHEMBL4078293 — IC50 = 150.0 nM 6.82
CHEMBL4065239 — IC50 = 150.0 nM 6.82
CHEMBL4064066 — IC50 = 160.0 nM 6.80
CHEMBL4073834 — IC50 = 190.0 nM 6.72
CHEMBL4100987 — IC50 = 200.0 nM 6.70
CHEMBL4086552 — IC50 = 230.0 nM 6.64
CHEMBL4094416 — IC50 = 240.0 nM 6.62
CHEMBL4067816 — IC50 = 250.0 nM 6.60
CHEMBL4079653 — IC50 = 260.0 nM 6.58
CHEMBL4097042 — IC50 = 270.0 nM 6.57
CHEMBL4105533 — IC50 = 270.0 nM 6.57
CHEMBL4065114 — IC50 = 270.0 nM 6.57
CHEMBL4065451 — IC50 = 270.0 nM 6.57
CHEMBL4062862 — IC50 = 280.0 nM 6.55
CHEMBL4100012 — IC50 = 300.0 nM 6.52
CHEMBL4090795 — IC50 = 310.0 nM 6.51
CHEMBL4090381 — IC50 = 340.0 nM 6.47
CHEMBL4062393 — IC50 = 350.0 nM 6.46
CHEMBL4097686 — IC50 = 360.0 nM 6.44
CHEMBL480375 — IC50 = 380.0 nM 6.42
CHEMBL4093258 — IC50 = 390.0 nM 6.41
CHEMBL1836005 — IC50 = 390.0 nM 6.41
CHEMBL4103409 — IC50 = 400.0 nM 6.40
CHEMBL4071737 — IC50 = 430.0 nM 6.37
CHEMBL4100963 — IC50 = 480.0 nM 6.32
CHEMBL4091750 — IC50 = 530.0 nM 6.28
CHEMBL4072660 — IC50 = 520.0 nM 6.28
CHEMBL4087650 — IC50 = 550.0 nM 6.26
CHEMBL4086678 — IC50 = 560.0 nM 6.25
CHEMBL4089957 — IC50 = 560.0 nM 6.25
CHEMBL4092525 — IC50 = 640.0 nM 6.19
CHEMBL4103100 — IC50 = 640.0 nM 6.19
CHEMBL4061728 — IC50 = 650.0 nM 6.19
CHEMBL4074208 — IC50 = 640.0 nM 6.19
CHEMBL4084507 — IC50 = 680.0 nM 6.17
CHEMBL4101223 — IC50 = 730.0 nM 6.14
CHEMBL4098235 — IC50 = 870.0 nM 6.06
CHEMBL4080211 — IC50 = 960.0 nM 6.02