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Assay Detail

CHEMBL4056785

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

Binding
Inhibition of Trypanosoma brucei recombinant farnesyltransferase using dansyl peptide containing GCAIM as substrate in presence of farnesyl pyrophosphate after 15 mins by fluorescence assay
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Trypanosoma brucei
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Structure-activity relationship studies on thiaplidiaquinones A and B as novel inhibitors of Plasmodium falciparum and farnesyltransferase.
Cadelis MM, Bourguet-Kondracki ML, Dubois J, Kaiser M, Brunel JM, Barker D, Copp BR.
Bioorg Med Chem (2017) 25 : 4433 -4443
PubMed 28666857 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.02 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54044 1 8.00
CHEMBL4066468 1 7.01
CHEMBL4087793 1 6.66
CHEMBL4076843 1 6.46
CHEMBL4079913 1 6.13
CHEMBL4086502 1 6.00
CHEMBL4096919 1 5.80
CHEMBL4098096 1 5.64
CHEMBL4104673 1 5.54
CHEMBL4104149 1 5.52
CHEMBL4090877 1 5.48
CHEMBL4105597 1 5.28
CHEMBL4075066 1 4.71
CHEMBL4075495 1 -
CHEMBL4095500 1 -
CHEMBL4063801 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54044 IC50 = 10.0 nM 8.00
CHEMBL4066468 IC50 = 98.0 nM 7.01
CHEMBL4087793 IC50 = 220.0 nM 6.66
CHEMBL4076843 IC50 = 350.0 nM 6.46
CHEMBL4079913 IC50 = 740.0 nM 6.13
CHEMBL4086502 IC50 = 1000.0 nM 6.00
CHEMBL4096919 IC50 = 1600.0 nM 5.80
CHEMBL4098096 IC50 = 2300.0 nM 5.64
CHEMBL4104673 IC50 = 2900.0 nM 5.54
CHEMBL4104149 IC50 = 3040.0 nM 5.52
CHEMBL4090877 IC50 = 3300.0 nM 5.48
CHEMBL4105597 IC50 = 5200.0 nM 5.28
CHEMBL4075066 IC50 = 19600.0 nM 4.71
CHEMBL4075495 IC50 > 22000.0 nM -
CHEMBL4095500 IC50 > 22000.0 nM -
CHEMBL4063801 IC50 > 22300.0 nM -