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Assay Detail

CHEMBL3382913

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

Functional
Trypanocidal activity against nifurtimox-sensitive Trypanosoma cruzi Tulahuen CL2 infected in human MRC5 SV2 cells assessed as parasite growth inhibition after 168 hrs by beta-galactosidase assay
78
Total Activities
78
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

From human immunodeficiency virus non-nucleoside reverse transcriptase inhibitors to potent and selective antitrypanosomal compounds.
Venkatraj M, Ariën KK, Heeres J, Joossens J, Dirié B, Lyssens S, Michiels J, Cos P, Lewi PJ, Vanham G, Maes L, Van der Veken P, Augustyns K.
Bioorg Med Chem (2014) 22 : 5241 -5248
PubMed 25199582 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 78 5.25 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3338018 1 6.20
CHEMBL290960 NIFURTIMOX 4.0 1 6.16
CHEMBL70663 DAPIVIRINE 3.0 1 5.90
CHEMBL3338027 1 5.78
CHEMBL3338030 1 5.77
CHEMBL3338032 1 5.70
CHEMBL3338035 1 5.69
CHEMBL3338029 1 5.67
CHEMBL3338034 1 5.62
CHEMBL69503 1 5.60
CHEMBL110 BENZNIDAZOLE 4.0 1 5.59
CHEMBL3338009 1 5.49
CHEMBL3338048 1 5.41
CHEMBL3338025 1 5.41
CHEMBL3338033 1 5.40
CHEMBL3337998 1 5.39
CHEMBL578061 1 5.35
CHEMBL3338054 1 5.35
CHEMBL3338023 1 5.31
CHEMBL3338020 1 5.31
CHEMBL3338045 1 5.28
CHEMBL3338013 1 5.28
CHEMBL3338028 1 5.25
CHEMBL470025 1 5.18
CHEMBL302791 1 5.17
CHEMBL3338041 1 5.17
CHEMBL71659 1 5.15
CHEMBL3338038 1 5.13
CHEMBL3338026 1 5.13
CHEMBL71521 1 5.13

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3338018 IC50 = 630.0 nM 6.20
CHEMBL290960 NIFURTIMOX IC50 = 700.0 nM 6.16
CHEMBL70663 DAPIVIRINE IC50 = 1250.0 nM 5.90
CHEMBL3338027 IC50 = 1650.0 nM 5.78
CHEMBL3338030 IC50 = 1690.0 nM 5.77
CHEMBL3338032 IC50 = 1980.0 nM 5.70
CHEMBL3338035 IC50 = 2040.0 nM 5.69
CHEMBL3338029 IC50 = 2140.0 nM 5.67
CHEMBL3338034 IC50 = 2410.0 nM 5.62
CHEMBL69503 IC50 = 2520.0 nM 5.60
CHEMBL110 BENZNIDAZOLE IC50 = 2560.0 nM 5.59
CHEMBL3338009 IC50 = 3270.0 nM 5.49
CHEMBL3338025 IC50 = 3860.0 nM 5.41
CHEMBL3338048 IC50 = 3920.0 nM 5.41
CHEMBL3338033 IC50 = 4020.0 nM 5.40
CHEMBL3337998 IC50 = 4080.0 nM 5.39
CHEMBL578061 IC50 = 4450.0 nM 5.35
CHEMBL3338054 IC50 = 4510.0 nM 5.35
CHEMBL3338023 IC50 = 4870.0 nM 5.31
CHEMBL3338020 IC50 = 4860.0 nM 5.31
CHEMBL3338045 IC50 = 5210.0 nM 5.28
CHEMBL3338013 IC50 = 5250.0 nM 5.28
CHEMBL3338028 IC50 = 5620.0 nM 5.25
CHEMBL470025 IC50 = 6650.0 nM 5.18
CHEMBL3338041 IC50 = 6780.0 nM 5.17
CHEMBL302791 IC50 = 6800.0 nM 5.17
CHEMBL71659 IC50 = 7150.0 nM 5.15
CHEMBL3338038 IC50 = 7430.0 nM 5.13
CHEMBL3338026 IC50 = 7450.0 nM 5.13
CHEMBL71521 IC50 = 7370.0 nM 5.13
CHEMBL3338047 IC50 = 8100.0 nM 5.09
CHEMBL3338040 IC50 = 8420.0 nM 5.08
CHEMBL223228 EFAVIRENZ IC50 = 8560.0 nM 5.07
CHEMBL3338022 IC50 = 8660.0 nM 5.06
CHEMBL421114 IC50 = 8690.0 nM 5.06
CHEMBL3338024 IC50 = 9350.0 nM 5.03
CHEMBL3338044 IC50 = 11080.0 nM 4.96
CHEMBL74174 IC50 = 11510.0 nM 4.94
CHEMBL3338031 IC50 = 11810.0 nM 4.93
CHEMBL3338052 IC50 = 14980.0 nM 4.82
CHEMBL3338043 IC50 = 22600.0 nM 4.65
CHEMBL3338049 IC50 = 27880.0 nM 4.55
CHEMBL3338036 IC50 = 30110.0 nM 4.52
CHEMBL3338006 IC50 = 46910.0 nM 4.33
CHEMBL3338012 IC50 = 47740.0 nM 4.32
CHEMBL3338050 IC50 > 64000.0 nM -
CHEMBL3338051 IC50 > 64000.0 nM -
CHEMBL3338053 IC50 > 64000.0 nM -
CHEMBL3337999 IC50 > 64000.0 nM -
CHEMBL57 NEVIRAPINE IC50 > 64000.0 nM -