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Assay Detail

CHEMBL681289

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

Binding
Inhibition of rate of incorporation of [3H]FPP into recombinant Ras-CVIM by human farnesyltransferase.
38
Total Activities
38
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 (CHEMBL2094108)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Diaryl ether inhibitors of farnesyl-protein transferase.
Mactough SC, Desolms SJ, Shaw AW, Abrams MT, Ciccarone TM, Davide JP, Hamilton KA, Hutchinson JH, Koblan KS, Kohl NE, Lobell RB, Robinson RG, Graham SL.
Bioorg Med Chem Lett (2001) 11 : 1257 -1260
PubMed 11392531 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 7.14 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24888 1 9.00
CHEMBL22959 1 8.96
CHEMBL282499 1 8.54
CHEMBL22319 1 8.10
CHEMBL22819 1 8.02
CHEMBL22440 1 7.89
CHEMBL282001 1 7.85
CHEMBL25606 1 7.77
CHEMBL22710 1 7.57
CHEMBL22080 1 7.57
CHEMBL25500 1 7.55
CHEMBL423109 1 7.42
CHEMBL25542 1 7.42
CHEMBL25439 1 7.42
CHEMBL23019 1 7.42
CHEMBL22826 1 7.40
CHEMBL22235 1 7.39
CHEMBL25217 1 7.35
CHEMBL22847 1 7.28
CHEMBL22547 1 7.07
CHEMBL22854 1 7.00
CHEMBL22718 1 6.96
CHEMBL23011 1 6.89
CHEMBL277489 1 6.82
CHEMBL280905 1 6.75
CHEMBL22568 1 6.70
CHEMBL24985 1 6.64
CHEMBL25602 1 6.64
CHEMBL279066 1 6.54
CHEMBL25550 1 6.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24888 IC50 = 1.0 nM 9.00
CHEMBL22959 IC50 = 1.1 nM 8.96
CHEMBL282499 IC50 = 2.9 nM 8.54
CHEMBL22319 IC50 = 8.0 nM 8.10
CHEMBL22819 IC50 = 9.6 nM 8.02
CHEMBL22440 IC50 = 13.0 nM 7.89
CHEMBL282001 IC50 = 14.0 nM 7.85
CHEMBL25606 IC50 = 17.0 nM 7.77
CHEMBL22710 IC50 = 27.0 nM 7.57
CHEMBL22080 IC50 = 27.0 nM 7.57
CHEMBL25500 IC50 = 28.0 nM 7.55
CHEMBL423109 IC50 = 38.0 nM 7.42
CHEMBL23019 IC50 = 38.0 nM 7.42
CHEMBL25439 IC50 = 38.0 nM 7.42
CHEMBL25542 IC50 = 38.0 nM 7.42
CHEMBL22826 IC50 = 40.0 nM 7.40
CHEMBL22235 IC50 = 41.0 nM 7.39
CHEMBL25217 IC50 = 45.0 nM 7.35
CHEMBL22847 IC50 = 53.0 nM 7.28
CHEMBL22547 IC50 = 86.0 nM 7.07
CHEMBL22854 IC50 = 100.0 nM 7.00
CHEMBL22718 IC50 = 110.0 nM 6.96
CHEMBL23011 IC50 = 130.0 nM 6.89
CHEMBL277489 IC50 = 150.0 nM 6.82
CHEMBL280905 IC50 = 180.0 nM 6.75
CHEMBL22568 IC50 = 200.0 nM 6.70
CHEMBL24985 IC50 = 230.0 nM 6.64
CHEMBL25602 IC50 = 230.0 nM 6.64
CHEMBL279066 IC50 = 290.0 nM 6.54
CHEMBL25550 IC50 = 340.0 nM 6.47
CHEMBL280384 IC50 = 390.0 nM 6.41
CHEMBL22800 IC50 = 440.0 nM 6.36
CHEMBL22356 IC50 = 475.0 nM 6.32
CHEMBL22454 IC50 = 860.0 nM 6.07
CHEMBL283323 IC50 = 1500.0 nM 5.82
CHEMBL279923 IC50 = 3400.0 nM 5.47
CHEMBL22238 IC50 = 5400.0 nM 5.27
CHEMBL22659 IC50 < 1.0 nM -