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Assay Detail

CHEMBL679532

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Binding
Inhibition of Farnesyltransferase
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Tricyclic farnesyl protein transferase inhibitors: crystallographic and calorimetric studies of structure-activity relationships.
Strickland CL, Weber PC, Windsor WT, Wu Z, Le HV, Albanese MM, Alvarez CS, Cesarz D, del Rosario J, Deskus J, Mallams AK, Njoroge FG, Piwinski JJ, Remiszewski S, Rossman RR, Taveras AG, Vibulbhan B, Doll RJ, Girijavallabhan VM, Ganguly AK.
J Med Chem (1999) 42 : 2125 -2135
PubMed 10377218 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.97 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69954 1 8.30
CHEMBL306428 1 7.37
CHEMBL66699 1 6.85
CHEMBL289404 1 6.60
CHEMBL67405 1 6.42
CHEMBL291576 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69954 IC50 = 5.0 nM 8.30
CHEMBL306428 IC50 = 43.0 nM 7.37
CHEMBL66699 IC50 = 140.0 nM 6.85
CHEMBL289404 IC50 = 250.0 nM 6.60
CHEMBL67405 IC50 = 378.0 nM 6.42
CHEMBL291576 IC50 = 500.0 nM 6.30