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Assay Detail

CHEMBL679579

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

Binding
FPT inhibitory activity was determined by the ability to inhibit the transfer of [3H]farnesyl from farnesyl pyrophosphate to H-ras-CLVS
45
Total Activities
44
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

Synthesis of 5,6-dihydro-11H-benzo[5,6]-cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidine-N-cyanoguanidine derivatives as inhibitors of ras farnesyl protein transferase.
Cooper AB, Strickland CL, Wang J, Desai J, Kirschmeier P, Patton R, Bishop WR, Weber PC, Girijavallabhan V.
Bioorg Med Chem Lett (2002) 12 : 601 -605
PubMed 11844681 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 7.15 8.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL348647 1 8.77
CHEMBL352022 1 8.22
CHEMBL440732 1 8.22
CHEMBL155363 1 8.09
CHEMBL348395 1 7.92
CHEMBL155232 1 7.89
CHEMBL155434 1 7.82
CHEMBL157570 1 7.82
CHEMBL153911 1 7.75
CHEMBL443816 1 7.70
CHEMBL345575 1 7.54
CHEMBL345846 1 7.52
CHEMBL154138 1 7.50
CHEMBL347625 1 7.46
CHEMBL347003 1 7.42
CHEMBL347798 1 7.42
CHEMBL155381 1 7.38
CHEMBL348576 1 7.37
CHEMBL157908 1 7.37
CHEMBL348110 1 7.24
CHEMBL158245 1 7.21
CHEMBL415739 1 7.13
CHEMBL434857 1 7.09
CHEMBL157803 1 7.08
CHEMBL433885 1 7.07
CHEMBL41934 1 7.05
CHEMBL440365 1 7.00
CHEMBL348370 1 6.98
CHEMBL346039 1 6.94
CHEMBL154417 1 6.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL348647 IC50 = 1.7 nM 8.77
CHEMBL352022 IC50 = 6.0 nM 8.22
CHEMBL440732 IC50 = 6.0 nM 8.22
CHEMBL155363 IC50 = 8.2 nM 8.09
CHEMBL348395 IC50 = 12.0 nM 7.92
CHEMBL155232 IC50 = 13.0 nM 7.89
CHEMBL157570 IC50 = 15.0 nM 7.82
CHEMBL155434 IC50 = 15.0 nM 7.82
CHEMBL153911 IC50 = 18.0 nM 7.75
CHEMBL443816 IC50 = 20.0 nM 7.70
CHEMBL345575 IC50 = 29.0 nM 7.54
CHEMBL345846 IC50 = 30.0 nM 7.52
CHEMBL154138 IC50 = 32.0 nM 7.50
CHEMBL347625 IC50 = 35.0 nM 7.46
CHEMBL347003 IC50 = 38.0 nM 7.42
CHEMBL347798 IC50 = 38.0 nM 7.42
CHEMBL155381 IC50 = 42.0 nM 7.38
CHEMBL157908 IC50 = 43.0 nM 7.37
CHEMBL348576 IC50 = 43.0 nM 7.37
CHEMBL348110 IC50 = 58.0 nM 7.24
CHEMBL158245 IC50 = 62.0 nM 7.21
CHEMBL415739 IC50 = 74.0 nM 7.13
CHEMBL434857 IC50 = 82.0 nM 7.09
CHEMBL157803 IC50 = 84.0 nM 7.08
CHEMBL433885 IC50 = 86.0 nM 7.07
CHEMBL41934 IC50 = 90.0 nM 7.05
CHEMBL440365 IC50 = 100.0 nM 7.00
CHEMBL348370 IC50 = 105.0 nM 6.98
CHEMBL346039 IC50 = 116.0 nM 6.94
CHEMBL154417 IC50 = 124.0 nM 6.91
CHEMBL156431 IC50 = 150.0 nM 6.82
CHEMBL156989 IC50 = 155.0 nM 6.81
CHEMBL347031 IC50 = 170.0 nM 6.77
CHEMBL156462 IC50 = 199.0 nM 6.70
CHEMBL158324 IC50 = 230.0 nM 6.64
CHEMBL348280 IC50 = 240.0 nM 6.62
CHEMBL155766 IC50 = 260.0 nM 6.58
CHEMBL346806 IC50 = 310.0 nM 6.51
CHEMBL346484 IC50 = 320.0 nM 6.50
CHEMBL338697 IC50 = 800.0 nM 6.10
CHEMBL338697 IC50 = 800.0 nM 6.10
CHEMBL154303 IC50 = 2600.0 nM 5.58
CHEMBL154710 IC50 = 15800.0 nM 4.80
CHEMBL1172 DESLORATADINE IC50 > 65000.0 nM -
CHEMBL358448 IC50 < 110.0 nM -