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Assay Detail

CHEMBL682705

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Binding
Inhibitory concentration against farnesyltransferase was determined
17
Total Activities
17
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

Inhibitors of farnesyltransferase: a rational approach to cancer chemotherapy?
Bell IM.
J Med Chem (2004) 47 : 1869 -1878
PubMed 15055985 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 8.34 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL294888 1 10.22
CHEMBL252953 1 9.82
CHEMBL52073 1 9.70
CHEMBL54044 1 9.22
CHEMBL289228 TIPIFARNIB 3.0 1 9.07
CHEMBL27486 1 9.00
CHEMBL55826 1 8.96
CHEMBL351706 BMS-214662 1.0 1 8.85
CHEMBL1790332 1 8.74
CHEMBL298734 LONAFARNIB 4.0 1 8.72
CHEMBL430778 1 7.62
CHEMBL27449 1 7.27
CHEMBL55431 1 6.75
CHEMBL289404 1 6.60
CHEMBL10971 SCH-37370 1 4.57
CHEMBL279433 L-778123 FREE BASE 1.0 1 -
CHEMBL442552 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL294888 IC50 = 0.06 nM 10.22
CHEMBL252953 IC50 = 0.15 nM 9.82
CHEMBL52073 IC50 = 0.2 nM 9.70
CHEMBL54044 IC50 = 0.6 nM 9.22
CHEMBL289228 TIPIFARNIB IC50 = 0.86 nM 9.07
CHEMBL27486 IC50 = 1.0 nM 9.00
CHEMBL55826 IC50 = 1.1 nM 8.96
CHEMBL351706 BMS-214662 IC50 = 1.4 nM 8.85
CHEMBL1790332 IC50 = 1.8 nM 8.74
CHEMBL298734 LONAFARNIB IC50 = 1.9 nM 8.72
CHEMBL430778 IC50 = 24.0 nM 7.62
CHEMBL27449 IC50 = 54.0 nM 7.27
CHEMBL55431 IC50 = 180.0 nM 6.75
CHEMBL289404 IC50 = 250.0 nM 6.60
CHEMBL10971 SCH-37370 IC50 = 27000.0 nM 4.57
CHEMBL279433 L-778123 FREE BASE IC50 = 2.0 nM -
CHEMBL442552 IC50 < 1.0 nM -