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Assay Detail

CHEMBL4717438

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

Binding
Inhibition of bovine brain FTase using 3H-farnesyl diphosphate as substrate incubated for 30 mins by beta-plate counting method
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery and preliminary structure-activity relationship studies on tecomaquinone I and tectol as novel farnesyltransferase and plasmodial inhibitors.
Cadelis MM,Bourguet-Kondracki ML,Dubois J,Valentin A,Barker D,Copp BR
Bioorg Med Chem (2016) 24 : 3102 -3107
PubMed 27240468 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.90 7.26

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL103955 CHAETOMELLIC ACID A 1 7.26
CHEMBL4745820 1 7.00
CHEMBL4794392 1 7.00
CHEMBL335691 1 6.82
CHEMBL100815 CHAETOMELLIC ACID B 1 6.73
CHEMBL4749161 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL103955 CHAETOMELLIC ACID A IC50 = 55.0 nM 7.26
CHEMBL4745820 IC50 = 100.0 nM 7.00
CHEMBL4794392 IC50 = 100.0 nM 7.00
CHEMBL335691 IC50 = 150.0 nM 6.82
CHEMBL100815 CHAETOMELLIC ACID B IC50 = 185.0 nM 6.73
CHEMBL4749161 IC50 = 250.0 nM 6.60