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Assay Detail

CHEMBL910294

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Binding
Inhibition of rat PFT
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2095197)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Structurally simple, potent, Plasmodium selective farnesyltransferase inhibitors that arrest the growth of malaria parasites.
Glenn MP, Chang SY, Hornéy C, Rivas K, Yokoyama K, Pusateri EE, Fletcher S, Cummings CG, Buckner FS, Pendyala PR, Chakrabarti D, Sebti SM, Gelb M, Van Voorhis WC, Hamilton AD.
J Med Chem (2006) 49 : 5710 -5727
PubMed 16970397 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 12 7.17 8.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL379766 1 8.12
CHEMBL384373 1 7.89
CHEMBL214610 1 7.81
CHEMBL215769 1 7.60
CHEMBL385845 1 7.37
CHEMBL215229 1 7.08
CHEMBL383966 1 6.75
CHEMBL215083 1 6.54
CHEMBL215780 1 6.46
CHEMBL386292 1 6.06
CHEMBL211989 1 -
CHEMBL213330 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL379766 IC50 = 7.5 nM 8.12
CHEMBL384373 IC50 = 13.0 nM 7.89
CHEMBL214610 IC50 = 15.5 nM 7.81
CHEMBL215769 IC50 = 25.0 nM 7.60
CHEMBL385845 IC50 = 43.0 nM 7.37
CHEMBL215229 IC50 = 83.0 nM 7.08
CHEMBL383966 IC50 = 180.0 nM 6.75
CHEMBL215083 IC50 = 290.0 nM 6.54
CHEMBL215780 IC50 = 350.0 nM 6.46
CHEMBL386292 IC50 = 880.0 nM 6.06
CHEMBL211989 IC50 > 1000.0 nM -
CHEMBL213330 IC50 > 1000.0 nM -