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Assay Detail

CHEMBL768472

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

Binding
Inhibitory activity against protein farnesyltransferase.
32
Total Activities
32
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

Novel tricyclic aminoacetyl and sulfonamide inhibitors of Ras farnesyl protein transferase
Njoroge F, Vibulbhan B, Alvarez CS, Bishop W, Petrin J, Doll RJ, Girijavallabhan V, Ganguly AK
Bioorg Med Chem Lett (1996) 6 : 2977 -2982
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 5.36 6.18

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL100302 1 6.18
CHEMBL101100 1 6.00
CHEMBL329983 1 6.00
CHEMBL101603 1 5.92
CHEMBL316890 1 5.72
CHEMBL318211 1 5.72
CHEMBL317144 1 5.70
CHEMBL318268 1 5.52
CHEMBL100738 1 5.44
CHEMBL322847 1 5.34
CHEMBL318840 1 5.33
CHEMBL328427 1 5.32
CHEMBL327507 1 5.32
CHEMBL100288 1 5.28
CHEMBL329519 1 5.20
CHEMBL323298 1 5.17
CHEMBL444325 1 5.09
CHEMBL101936 1 5.08
CHEMBL432011 1 5.07
CHEMBL318886 1 5.06
CHEMBL421576 1 5.02
CHEMBL317427 1 4.97
CHEMBL316888 1 4.94
CHEMBL101782 1 4.89
CHEMBL316889 1 4.65
CHEMBL431227 1 -
CHEMBL318189 1 -
CHEMBL431622 1 -
CHEMBL101465 1 -
CHEMBL317845 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL100302 IC50 = 660.0 nM 6.18
CHEMBL101100 IC50 = 1000.0 nM 6.00
CHEMBL329983 IC50 = 1000.0 nM 6.00
CHEMBL101603 IC50 = 1200.0 nM 5.92
CHEMBL316890 IC50 = 1900.0 nM 5.72
CHEMBL318211 IC50 = 1900.0 nM 5.72
CHEMBL317144 IC50 = 2000.0 nM 5.70
CHEMBL318268 IC50 = 3050.0 nM 5.52
CHEMBL100738 IC50 = 3600.0 nM 5.44
CHEMBL322847 IC50 = 4600.0 nM 5.34
CHEMBL318840 IC50 = 4700.0 nM 5.33
CHEMBL328427 IC50 = 4800.0 nM 5.32
CHEMBL327507 IC50 = 4800.0 nM 5.32
CHEMBL100288 IC50 = 5200.0 nM 5.28
CHEMBL329519 IC50 = 6290.0 nM 5.20
CHEMBL323298 IC50 = 6800.0 nM 5.17
CHEMBL444325 IC50 = 8200.0 nM 5.09
CHEMBL101936 IC50 = 8400.0 nM 5.08
CHEMBL432011 IC50 = 8500.0 nM 5.07
CHEMBL318886 IC50 = 8800.0 nM 5.06
CHEMBL421576 IC50 = 9600.0 nM 5.02
CHEMBL317427 IC50 = 10600.0 nM 4.97
CHEMBL316888 IC50 = 11400.0 nM 4.94
CHEMBL101782 IC50 = 13000.0 nM 4.89
CHEMBL316889 IC50 = 22300.0 nM 4.65
CHEMBL431227 IC50 > 12000.0 nM -
CHEMBL318189 IC50 > 10000.0 nM -
CHEMBL431622 IC50 > 10000.0 nM -
CHEMBL101465 IC50 > 11000.0 nM -
CHEMBL317845 IC50 > 10000.0 nM -
CHEMBL101570 IC50 > 12000.0 nM -
CHEMBL102085 IC50 > 12000.0 nM -