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Assay Detail

CHEMBL680514

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

Binding
Inhibitory concentration against Farnesyltransferase for Farnesylation of H-ras protein InNIH 3T3 cells transformed with activated H-ras
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NIH3T3
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Protein farnesyltransferase (CHEMBL2096912)
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Synthesis and evaluation of hydroxyproline-derived isoprenyltransferase inhibitors.
O'Connell CE, Ackermann K, Rowell CA, Garcia AM, Lewis MD, Schwartz CE.
Bioorg Med Chem Lett (1999) 9 : 2095 -2100
PubMed 10450988 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 5.89 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303859 1 7.40
CHEMBL302834 1 6.46
CHEMBL62387 1 6.43
CHEMBL433102 1 6.31
CHEMBL305772 1 6.08
CHEMBL303363 1 5.70
CHEMBL302025 1 5.52
CHEMBL304823 1 5.50
CHEMBL66788 1 5.48
CHEMBL2092732 1 5.28
CHEMBL3349355 1 4.65
CHEMBL3350681 1 -
CHEMBL3349356 1 -
CHEMBL304680 1 -
CHEMBL3349311 1 -
CHEMBL3350225 1 -
CHEMBL294277 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303859 IC50 = 40.0 nM 7.40
CHEMBL302834 IC50 = 350.0 nM 6.46
CHEMBL62387 IC50 = 370.0 nM 6.43
CHEMBL433102 IC50 = 490.0 nM 6.31
CHEMBL305772 IC50 = 840.0 nM 6.08
CHEMBL303363 IC50 = 2000.0 nM 5.70
CHEMBL302025 IC50 = 3000.0 nM 5.52
CHEMBL304823 IC50 = 3200.0 nM 5.50
CHEMBL66788 IC50 = 3300.0 nM 5.48
CHEMBL2092732 IC50 = 5300.0 nM 5.28
CHEMBL3349355 IC50 = 22500.0 nM 4.65
CHEMBL3350681 IC50 > 50000.0 nM -
CHEMBL3349356 IC50 > 10000.0 nM -
CHEMBL304680 IC50 > 50000.0 nM -
CHEMBL3349311 IC50 > 10000.0 nM -
CHEMBL3350225 IC50 > 50000.0 nM -
CHEMBL294277 IC50 > 50000.0 nM -