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Assay Detail

CHEMBL680442

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of transfer of [3H]FPP to biotin K-ras peptide (KKSKTKCVIM) catalyzed by bovine FTase
36
Total Activities
36
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Protein farnesyltransferase (CHEMBL2095178)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Discovery of potent imidazole and cyanophenyl containing farnesyltransferase inhibitors with improved oral bioavailability.
Tong Y, Lin NH, Wang L, Hasvold L, Wang W, Leonard N, Li T, Li Q, Cohen J, Gu WZ, Zhang H, Stoll V, Bauch J, Marsh K, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2003) 13 : 1571 -1574
PubMed 12699757 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 36 8.85 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL41515 1 9.80
CHEMBL41951 1 9.74
CHEMBL37194 1 9.74
CHEMBL434396 1 9.60
CHEMBL38615 1 9.40
CHEMBL43631 1 9.37
CHEMBL41268 1 9.35
CHEMBL39096 1 9.29
CHEMBL38941 1 9.29
CHEMBL290760 1 9.24
CHEMBL43455 1 9.21
CHEMBL289844 1 9.19
CHEMBL43082 1 9.15
CHEMBL288901 1 9.14
CHEMBL38616 1 9.12
CHEMBL38438 1 9.09
CHEMBL288449 1 9.08
CHEMBL432477 1 9.06
CHEMBL288046 1 9.05
CHEMBL39117 1 9.04
CHEMBL39805 1 9.01
CHEMBL41682 1 9.00
CHEMBL41936 1 9.00
CHEMBL287729 1 8.77
CHEMBL288838 1 8.74
CHEMBL290161 1 8.72
CHEMBL41454 1 8.70
CHEMBL38595 1 8.70
CHEMBL41540 1 8.41
CHEMBL38974 1 8.09

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL41515 IC50 = 0.16 nM 9.80
CHEMBL41951 IC50 = 0.18 nM 9.74
CHEMBL37194 IC50 = 0.18 nM 9.74
CHEMBL434396 IC50 = 0.25 nM 9.60
CHEMBL38615 IC50 = 0.4 nM 9.40
CHEMBL43631 IC50 = 0.43 nM 9.37
CHEMBL41268 IC50 = 0.45 nM 9.35
CHEMBL39096 IC50 = 0.51 nM 9.29
CHEMBL38941 IC50 = 0.51 nM 9.29
CHEMBL290760 IC50 = 0.57 nM 9.24
CHEMBL43455 IC50 = 0.62 nM 9.21
CHEMBL289844 IC50 = 0.64 nM 9.19
CHEMBL43082 IC50 = 0.71 nM 9.15
CHEMBL288901 IC50 = 0.73 nM 9.14
CHEMBL38616 IC50 = 0.75 nM 9.12
CHEMBL38438 IC50 = 0.82 nM 9.09
CHEMBL288449 IC50 = 0.84 nM 9.08
CHEMBL432477 IC50 = 0.88 nM 9.06
CHEMBL288046 IC50 = 0.9 nM 9.05
CHEMBL39117 IC50 = 0.92 nM 9.04
CHEMBL39805 IC50 = 0.98 nM 9.01
CHEMBL41682 IC50 = 1.0 nM 9.00
CHEMBL41936 IC50 = 0.99 nM 9.00
CHEMBL287729 IC50 = 1.7 nM 8.77
CHEMBL288838 IC50 = 1.8 nM 8.74
CHEMBL290161 IC50 = 1.9 nM 8.72
CHEMBL38595 IC50 = 2.0 nM 8.70
CHEMBL41454 IC50 = 2.0 nM 8.70
CHEMBL41540 IC50 = 3.9 nM 8.41
CHEMBL38974 IC50 = 8.2 nM 8.09
CHEMBL38567 IC50 = 8.5 nM 8.07
CHEMBL288523 IC50 = 12.0 nM 7.92
CHEMBL418059 IC50 = 25.0 nM 7.60
CHEMBL41518 IC50 = 44.0 nM 7.36
CHEMBL38802 IC50 = 58.0 nM 7.24
CHEMBL290315 IC50 = 68.0 nM 7.17