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Assay Detail

CHEMBL681410

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

Binding
In vitro concentration required to reduce Farnesyltransferase catalyzed incorporation of [3H]FPP into recombinant Ha-Ras protein by 50%
26
Total Activities
26
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

Pseudodipeptide inhibitors of protein farnesyltransferase.
deSolms SJ, Deana AA, Giuliani EA, Graham SL, Kohl NE, Mosser SD, Oliff AI, Pompliano DL, Rands E, Scholz TH.
J Med Chem (1995) 38 : 3967 -3971
PubMed 7562930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.35 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128967 1 7.64
CHEMBL132155 1 7.40
CHEMBL129140 1 7.34
CHEMBL340735 1 7.22
CHEMBL129718 1 7.16
CHEMBL129603 1 7.01
CHEMBL129589 1 6.92
CHEMBL433854 1 6.46
CHEMBL128448 1 6.43
CHEMBL129723 1 6.40
CHEMBL338527 1 6.35
CHEMBL128937 1 6.22
CHEMBL128611 1 6.18
CHEMBL130769 1 6.15
CHEMBL340960 1 6.05
CHEMBL339731 1 6.03
CHEMBL129175 1 6.00
CHEMBL2370669 1 6.00
CHEMBL129110 1 5.96
CHEMBL339824 1 5.89
CHEMBL127610 1 5.70
CHEMBL129109 1 5.55
CHEMBL131001 1 5.22
CHEMBL128898 1 5.05
CHEMBL337477 1 -
CHEMBL129116 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128967 IC50 = 23.0 nM 7.64
CHEMBL132155 IC50 = 40.0 nM 7.40
CHEMBL129140 IC50 = 46.0 nM 7.34
CHEMBL340735 IC50 = 60.0 nM 7.22
CHEMBL129718 IC50 = 70.0 nM 7.16
CHEMBL129603 IC50 = 97.0 nM 7.01
CHEMBL129589 IC50 = 120.0 nM 6.92
CHEMBL433854 IC50 = 350.0 nM 6.46
CHEMBL128448 IC50 = 370.0 nM 6.43
CHEMBL129723 IC50 = 400.0 nM 6.40
CHEMBL338527 IC50 = 450.0 nM 6.35
CHEMBL128937 IC50 = 600.0 nM 6.22
CHEMBL128611 IC50 = 660.0 nM 6.18
CHEMBL130769 IC50 = 707.0 nM 6.15
CHEMBL340960 IC50 = 900.0 nM 6.05
CHEMBL339731 IC50 = 945.0 nM 6.03
CHEMBL129175 IC50 = 1000.0 nM 6.00
CHEMBL2370669 IC50 = 1000.0 nM 6.00
CHEMBL129110 IC50 = 1100.0 nM 5.96
CHEMBL339824 IC50 = 1300.0 nM 5.89
CHEMBL127610 IC50 = 2000.0 nM 5.70
CHEMBL129109 IC50 = 2800.0 nM 5.55
CHEMBL131001 IC50 = 6000.0 nM 5.22
CHEMBL128898 IC50 = 9000.0 nM 5.05
CHEMBL337477 IC50 > 10000.0 nM -
CHEMBL129116 IC50 > 10000.0 nM -