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Assay Detail

CHEMBL681645

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Binding
In vitro inhibitory concentration evaluated against P21ras Farnesyl transferase
27
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 (CHEMBL2095197)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Peptide based P21RAS farnesyl transferase inhibitors: systematic modification of the tetrapeptide CA1A2X motif
Leftheris K, Kline T, Natarajan S, DeVirgilio M, Cho Y, Pluscec J, Ricca C, Robinson S, Seizinger B, Manne V, Meyers C
Bioorg Med Chem Lett (1994) 4 : 887 -892
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.56 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL327674 1 7.92
CHEMBL353715 1 7.92
CHEMBL326131 1 7.85
CHEMBL300237 1 7.77
CHEMBL353040 1 7.54
CHEMBL289302 1 7.43
CHEMBL354194 1 7.17
CHEMBL171783 1 6.92
CHEMBL171250 1 6.90
CHEMBL367733 1 6.62
CHEMBL169988 1 6.60
CHEMBL171367 1 6.44
CHEMBL426931 1 6.40
CHEMBL352414 1 6.40
CHEMBL169799 1 6.38
CHEMBL354044 2 6.29
CHEMBL2371610 1 6.16
CHEMBL49942 1 6.02
CHEMBL171168 1 5.92
CHEMBL48470 1 5.85
CHEMBL352408 1 5.75
CHEMBL52150 1 5.65
CHEMBL78855 1 5.28
CHEMBL333870 1 5.17
CHEMBL172335 1 -
CHEMBL354880 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL327674 IC50 = 12.0 nM 7.92
CHEMBL353715 IC50 = 12.0 nM 7.92
CHEMBL326131 IC50 = 14.0 nM 7.85
CHEMBL300237 IC50 = 17.0 nM 7.77
CHEMBL353040 IC50 = 29.0 nM 7.54
CHEMBL289302 IC50 = 37.0 nM 7.43
CHEMBL354194 IC50 = 68.0 nM 7.17
CHEMBL171783 IC50 = 120.0 nM 6.92
CHEMBL171250 IC50 = 126.0 nM 6.90
CHEMBL367733 IC50 = 241.0 nM 6.62
CHEMBL169988 IC50 = 250.0 nM 6.60
CHEMBL171367 IC50 = 360.0 nM 6.44
CHEMBL426931 IC50 = 400.0 nM 6.40
CHEMBL352414 IC50 = 400.0 nM 6.40
CHEMBL169799 IC50 = 420.0 nM 6.38
CHEMBL354044 IC50 = 510.0 nM 6.29
CHEMBL2371610 IC50 = 696.0 nM 6.16
CHEMBL49942 IC50 = 950.0 nM 6.02
CHEMBL171168 IC50 = 1200.0 nM 5.92
CHEMBL48470 IC50 = 1400.0 nM 5.85
CHEMBL352408 IC50 = 1800.0 nM 5.75
CHEMBL52150 IC50 = 2220.0 nM 5.65
CHEMBL354044 IC50 = 2700.0 nM 5.57
CHEMBL78855 IC50 = 5200.0 nM 5.28
CHEMBL333870 IC50 = 6800.0 nM 5.17
CHEMBL172335 IC50 = 250000.0 nM -
CHEMBL354880 IC50 = 120000.0 nM -