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Assay Detail

CHEMBL679531

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Binding
Inhibition of Farnesyl protein transferase
7
Total Activities
7
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 7 7.65 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL298734 LONAFARNIB 4.0 1 8.72
CHEMBL66462 1 8.41
CHEMBL305798 1 7.96
CHEMBL432911 1 7.60
CHEMBL305431 1 7.30
CHEMBL41934 1 7.28
CHEMBL63804 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL298734 LONAFARNIB IC50 = 1.9 nM 8.72
CHEMBL66462 IC50 = 3.9 nM 8.41
CHEMBL305798 IC50 = 11.0 nM 7.96
CHEMBL432911 IC50 = 25.0 nM 7.60
CHEMBL305431 IC50 = 50.0 nM 7.30
CHEMBL41934 IC50 = 52.0 nM 7.28
CHEMBL63804 IC50 = 530.0 nM 6.28