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Assay Detail

CHEMBL3789228

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Functional
Antitrypanosomal activity against Trypanosoma cruzi infected in human MRC5 cells assessed as parasite growth inhibition incubated for 7 days by chlorophenol red alpha-D-galactopyranoside-based assay
ChEMBL ↗
67
Total Activities
67
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Cell Type MRC5
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368) ↗
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Repositioning Antitubercular 6-Nitro-2,3-dihydroimidazo[2,1-b][1,3]oxazoles for Neglected Tropical Diseases: Structure-Activity Studies on a Preclinical Candidate for Visceral Leishmaniasis.
Thompson AM, O'Connor PD, Blaser A, Yardley V, Maes L, Gupta S, Launay D, Martin D, Franzblau SG, Wan B, Wang Y, Ma Z, Denny WA.
J Med Chem (2016) 59 : 2530 -2550
PubMed 26901446 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 67 5.62 6.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3785246 — — 1 6.89
CHEMBL3188499 — — 1 6.40
CHEMBL3787306 — — 1 6.38
CHEMBL218650 DELAMANID 4.0 1 6.37
CHEMBL3787057 — — 1 6.28
CHEMBL3786506 — — 1 6.24
CHEMBL3786438 — — 1 6.24
CHEMBL3787410 — — 1 6.23
CHEMBL3785196 — — 1 6.22
CHEMBL3785539 — — 1 6.19
CHEMBL3786175 — — 1 6.07
CHEMBL3787138 — — 1 6.05
CHEMBL3786151 — — 1 6.05
CHEMBL3785276 — — 1 6.03
CHEMBL3787272 — — 1 6.02
CHEMBL3785138 — — 1 6.00
CHEMBL3786828 — — 1 5.96
CHEMBL3786301 — — 1 5.96
CHEMBL3785985 — — 1 5.92
CHEMBL3786164 — — 1 5.89
CHEMBL3785579 — — 1 5.85
CHEMBL3786471 — — 1 5.85
CHEMBL3785572 — — 1 5.85
CHEMBL3785182 — — 1 5.82
CHEMBL3785856 — — 1 5.82
CHEMBL3785128 — — 1 5.82
CHEMBL3786215 — — 1 5.80
CHEMBL3787357 — — 1 5.80
CHEMBL3786648 — — 1 5.77
CHEMBL3786030 — — 1 5.75

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3785246 — IC50 = 130.0 nM 6.89
CHEMBL3188499 — IC50 = 400.0 nM 6.40
CHEMBL3787306 — IC50 = 420.0 nM 6.38
CHEMBL218650 DELAMANID IC50 = 430.0 nM 6.37
CHEMBL3787057 — IC50 = 520.0 nM 6.28
CHEMBL3786506 — IC50 = 580.0 nM 6.24
CHEMBL3786438 — IC50 = 580.0 nM 6.24
CHEMBL3787410 — IC50 = 590.0 nM 6.23
CHEMBL3785196 — IC50 = 600.0 nM 6.22
CHEMBL3785539 — IC50 = 650.0 nM 6.19
CHEMBL3786175 — IC50 = 850.0 nM 6.07
CHEMBL3787138 — IC50 = 890.0 nM 6.05
CHEMBL3786151 — IC50 = 900.0 nM 6.05
CHEMBL3785276 — IC50 = 940.0 nM 6.03
CHEMBL3787272 — IC50 = 950.0 nM 6.02
CHEMBL3785138 — IC50 = 990.0 nM 6.00
CHEMBL3786828 — IC50 = 1100.0 nM 5.96
CHEMBL3786301 — IC50 = 1100.0 nM 5.96
CHEMBL3785985 — IC50 = 1200.0 nM 5.92
CHEMBL3786164 — IC50 = 1300.0 nM 5.89
CHEMBL3785579 — IC50 = 1400.0 nM 5.85
CHEMBL3786471 — IC50 = 1400.0 nM 5.85
CHEMBL3785572 — IC50 = 1400.0 nM 5.85
CHEMBL3785128 — IC50 = 1500.0 nM 5.82
CHEMBL3785182 — IC50 = 1500.0 nM 5.82
CHEMBL3785856 — IC50 = 1500.0 nM 5.82
CHEMBL3786215 — IC50 = 1600.0 nM 5.80
CHEMBL3787357 — IC50 = 1600.0 nM 5.80
CHEMBL3786648 — IC50 = 1700.0 nM 5.77
CHEMBL3786030 — IC50 = 1800.0 nM 5.75
CHEMBL3787572 — IC50 = 1800.0 nM 5.75
CHEMBL219919 — IC50 = 1800.0 nM 5.75
CHEMBL3787254 — IC50 = 2100.0 nM 5.68
CHEMBL3786741 — IC50 = 2200.0 nM 5.66
CHEMBL3787314 — IC50 = 2400.0 nM 5.62
CHEMBL3787070 — IC50 = 2400.0 nM 5.62
CHEMBL3787583 — IC50 = 2500.0 nM 5.60
CHEMBL3787545 — IC50 = 2500.0 nM 5.60
CHEMBL3787513 — IC50 = 2600.0 nM 5.58
CHEMBL218974 — IC50 = 2600.0 nM 5.58
CHEMBL3787358 — IC50 = 2800.0 nM 5.55
CHEMBL3787645 — IC50 = 2800.0 nM 5.55
CHEMBL3785566 — IC50 = 2800.0 nM 5.55
CHEMBL3786902 — IC50 = 2900.0 nM 5.54
CHEMBL3787018 — IC50 = 3600.0 nM 5.44
CHEMBL3785677 — IC50 = 4500.0 nM 5.35
CHEMBL3787622 — IC50 = 4700.0 nM 5.33
CHEMBL3786077 — IC50 = 4700.0 nM 5.33
CHEMBL3786795 — IC50 = 5600.0 nM 5.25
CHEMBL3786138 — IC50 = 7100.0 nM 5.15