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Assay Detail

CHEMBL4711537

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Functional
Antitrypanosomal activity against Trypanosoma cruzi Tulahuen strain C2C4 amastigotes infected in rat L6 cells assessed as inhibition of parasite growth incubated for 96 hrs by chlorophenol red-fl-D-galactopyranoside based colorimetric analysis
ChEMBL ↗
72
Total Activities
38
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Trypanosoma cruzi
Cell Type L6
Confidence 1 — Organism
Curated By Autocuration

Target

Trypanosoma cruzi (CHEMBL368) ↗
Type ORGANISM
Organism Trypanosoma cruzi

Publication

Re-evaluating pretomanid analogues for Chagas disease: Hit-to-lead studies reveal both in vitro and in vivo trypanocidal efficacy.
Thompson AM,O'Connor PD,Marshall AJ,Francisco AF,Kelly JM,Riley J,Read KD,Perez CJ,Cornwall S,Thompson RCA,Keenan M,White KL,Charman SA,Zulfiqar B,Sykes ML,Avery VM,Chatelain E,Denny WA
Eur J Med Chem (2020) 207 : 112849 -112849
PubMed 33007723 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.42 7.75
IC90 34 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4105162 — — 2 7.75
CHEMBL3608949 — — 2 7.66
CHEMBL4776598 — — 2 7.46
CHEMBL4097978 — — 2 7.40
CHEMBL471108 — — 2 7.33
CHEMBL4098597 — — 2 7.31
CHEMBL4755787 — — 2 7.28
CHEMBL4746261 — — 2 7.08
CHEMBL4090270 — — 2 6.77
CHEMBL4792815 — — 2 6.68
CHEMBL1836445 — — 2 6.64
CHEMBL4091850 — — 2 6.62
CHEMBL4784920 — — 2 6.62
CHEMBL4778209 — — 2 6.60
CHEMBL4764892 — — 2 6.55
CHEMBL4746300 — — 2 6.52
CHEMBL4095540 — — 2 6.51
CHEMBL4776282 — — 2 6.51
CHEMBL1836443 — — 2 6.50
CHEMBL4762586 — — 2 6.48
CHEMBL4792832 — — 2 6.42
CHEMBL4078293 — — 2 6.40
CHEMBL4066553 — — 2 6.35
CHEMBL4776970 — — 2 6.34
CHEMBL4741859 — — 2 6.25
CHEMBL4785448 — — 2 6.17
CHEMBL4783283 — — 2 6.16
CHEMBL480728 — — 1 6.05
CHEMBL4760509 — — 2 5.96
CHEMBL480375 — — 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4105162 — IC50 = 18.0 nM 7.75
CHEMBL3608949 — IC50 = 22.0 nM 7.66
CHEMBL4776598 — IC50 = 35.0 nM 7.46
CHEMBL4097978 — IC50 = 40.0 nM 7.40
CHEMBL471108 — IC50 = 47.0 nM 7.33
CHEMBL4098597 — IC50 = 49.0 nM 7.31
CHEMBL4755787 — IC50 = 53.0 nM 7.28
CHEMBL4746261 — IC50 = 83.0 nM 7.08
CHEMBL4090270 — IC50 = 170.0 nM 6.77
CHEMBL4792815 — IC50 = 210.0 nM 6.68
CHEMBL1836445 — IC50 = 230.0 nM 6.64
CHEMBL4091850 — IC50 = 240.0 nM 6.62
CHEMBL4784920 — IC50 = 240.0 nM 6.62
CHEMBL4778209 — IC50 = 250.0 nM 6.60
CHEMBL4764892 — IC50 = 280.0 nM 6.55
CHEMBL4746300 — IC50 = 300.0 nM 6.52
CHEMBL4776282 — IC50 = 310.0 nM 6.51
CHEMBL4095540 — IC50 = 310.0 nM 6.51
CHEMBL1836443 — IC50 = 320.0 nM 6.50
CHEMBL4762586 — IC50 = 330.0 nM 6.48
CHEMBL4792832 — IC50 = 380.0 nM 6.42
CHEMBL4078293 — IC50 = 400.0 nM 6.40
CHEMBL4066553 — IC50 = 450.0 nM 6.35
CHEMBL4776970 — IC50 = 460.0 nM 6.34
CHEMBL4741859 — IC50 = 560.0 nM 6.25
CHEMBL4785448 — IC50 = 670.0 nM 6.17
CHEMBL4783283 — IC50 = 700.0 nM 6.16
CHEMBL480728 — IC50 = 900.0 nM 6.05
CHEMBL4760509 — IC50 = 1100.0 nM 5.96
CHEMBL480375 — IC50 = 1200.0 nM 5.92
CHEMBL4796885 — IC50 = 1600.0 nM 5.80
CHEMBL4790077 — IC50 = 1600.0 nM 5.80
CHEMBL4791840 — IC50 = 2700.0 nM 5.57
CHEMBL583256 — IC50 = 3700.0 nM 5.43
CHEMBL4763590 — IC50 = 4800.0 nM 5.32
CHEMBL569379 — IC50 = 5700.0 nM 5.24
CHEMBL576112 — IC50 = 60000.0 nM 4.22
CHEMBL4066553 — IC90 = 930.0 nM -
CHEMBL4095540 — IC90 = 900.0 nM -
CHEMBL1836445 — IC90 = 590.0 nM -
CHEMBL4098597 — IC90 = 310.0 nM -
CHEMBL569157 — IC90 > 10000.0 nM -
CHEMBL4796885 — IC90 = 6300.0 nM -
CHEMBL471108 — IC90 = 130.0 nM -
CHEMBL3608949 — IC90 = 190.0 nM -
CHEMBL569379 — IC90 > 10000.0 nM -
CHEMBL4763590 — IC90 > 10000.0 nM -
CHEMBL4746300 — IC90 = 1400.0 nM -
CHEMBL4778209 — IC90 = 710.0 nM -
CHEMBL1836443 — IC90 = 990.0 nM -