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Assay Detail

CHEMBL680826

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Functional
Inhibition of [3H]FPP incorporation into Ha-ras protein by Farnesyltransferase
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

3-Aryl-4-aryloyl-1-(1H-imidazol-5-yl)methylpyrrole, a novel class of farnesyltransferase inhibitors.
Lee H, Lee J, Shin Y, Jung W, Kim JH, Park K, Ro S, Chung HH, Koh JS.
Bioorg Med Chem Lett (2001) 11 : 2963 -2965
PubMed 11677136 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 7.15 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54044 1 9.30
CHEMBL431828 1 8.85
CHEMBL98692 1 8.34
CHEMBL101889 1 7.80
CHEMBL330655 1 7.50
CHEMBL98806 1 7.19
CHEMBL317408 1 7.06
CHEMBL102187 1 6.94
CHEMBL319100 1 6.82
CHEMBL319294 1 6.33
CHEMBL98498 1 5.87
CHEMBL101551 1 5.64
CHEMBL101897 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54044 IC50 = 0.5 nM 9.30
CHEMBL431828 IC50 = 1.4 nM 8.85
CHEMBL98692 IC50 = 4.6 nM 8.34
CHEMBL101889 IC50 = 16.0 nM 7.80
CHEMBL330655 IC50 = 32.0 nM 7.50
CHEMBL98806 IC50 = 65.0 nM 7.19
CHEMBL317408 IC50 = 88.0 nM 7.06
CHEMBL102187 IC50 = 115.0 nM 6.94
CHEMBL319100 IC50 = 150.0 nM 6.82
CHEMBL319294 IC50 = 470.0 nM 6.33
CHEMBL98498 IC50 = 1350.0 nM 5.87
CHEMBL101551 IC50 = 2300.0 nM 5.64
CHEMBL101897 IC50 = 5000.0 nM 5.30