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Assay Detail

CHEMBL1106971

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

Functional
Antitrypanosomal activity against Trypanosoma brucei brucei after 48 hrs by luminescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Trypanosoma brucei brucei (CHEMBL612851)
Type ORGANISM
Organism Trypanosoma brucei brucei

Publication

Podophyllotoxin analogues active versus Trypanosoma brucei.
Uddin MJ, Smithson DC, Brown KM, Crews BC, Connelly M, Zhu F, Marnett LJ, Guy RK.
Bioorg Med Chem Lett (2010) 20 : 1787 -1791
PubMed 20129783 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 5.80 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1076638 1 7.29
CHEMBL379989 RHIZOXIN 1 6.82
CHEMBL1076642 1 6.77
CHEMBL1076674 1 6.66
CHEMBL1076641 1 6.34
CHEMBL1076675 1 6.00
CHEMBL1076639 1 5.47
CHEMBL1076643 1 5.35
CHEMBL1076640 1 5.28
CHEMBL1076673 1 4.57
CHEMBL1076672 1 4.51
CHEMBL1076645 1 4.50
CHEMBL1076644 1 -
CHEMBL1081214 SUCCINYLPODOPHYLLOTOXIN 1 -
CHEMBL61 PODOFILOX 4.0 1 -
CHEMBL6 INDOMETHACIN 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1076638 IC50 = 51.0 nM 7.29
CHEMBL379989 RHIZOXIN IC50 = 150.0 nM 6.82
CHEMBL1076642 IC50 = 170.0 nM 6.77
CHEMBL1076674 IC50 = 220.0 nM 6.66
CHEMBL1076641 IC50 = 460.0 nM 6.34
CHEMBL1076675 IC50 = 990.0 nM 6.00
CHEMBL1076639 IC50 = 3400.0 nM 5.47
CHEMBL1076643 IC50 = 4500.0 nM 5.35
CHEMBL1076640 IC50 = 5300.0 nM 5.28
CHEMBL1076673 IC50 = 27000.0 nM 4.57
CHEMBL1076672 IC50 = 31000.0 nM 4.51
CHEMBL1076645 IC50 = 32000.0 nM 4.50
CHEMBL1076644 IC50 > 50000.0 nM -
CHEMBL1081214 SUCCINYLPODOPHYLLOTOXIN IC50 > 50000.0 nM -
CHEMBL61 PODOFILOX IC50 > 50000.0 nM -
CHEMBL6 INDOMETHACIN IC50 > 50000.0 nM -