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Assay Detail

CHEMBL864674

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Binding
Inhibitory activity against farnesyltransferase quantified by SPA assay
44
Total Activities
42
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

Guiding farnesyltransferase inhibitors from an ECLiPS library to the catalytic zinc.
Huang CY, Stauffer TM, Strickland CL, Reader JC, Huang H, Li G, Cooper AB, Doll RJ, Ganguly AK, Baldwin JJ, Rokosz LL.
Bioorg Med Chem Lett (2006) 16 : 507 -511
PubMed 16289818 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 7.72 8.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL381360 3 8.82
CHEMBL372343 1 8.26
CHEMBL202272 1 8.24
CHEMBL378816 1 8.15
CHEMBL201844 1 8.15
CHEMBL369933 1 8.14
CHEMBL371962 1 8.14
CHEMBL201043 1 8.10
CHEMBL408569 1 8.10
CHEMBL201817 1 8.10
CHEMBL370411 1 8.10
CHEMBL381736 1 8.08
CHEMBL372350 1 8.04
CHEMBL199921 1 8.04
CHEMBL372415 1 8.00
CHEMBL427191 1 7.96
CHEMBL425931 1 7.92
CHEMBL201888 1 7.92
CHEMBL201956 1 7.92
CHEMBL201903 1 7.89
CHEMBL382285 1 7.89
CHEMBL383764 1 7.85
CHEMBL372163 1 7.85
CHEMBL202547 1 7.82
CHEMBL202825 1 7.77
CHEMBL201044 1 7.75
CHEMBL369994 1 7.72
CHEMBL202493 1 7.70
CHEMBL201693 1 7.70
CHEMBL382367 1 7.68

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL381360 IC50 = 1.5 nM 8.82
CHEMBL381360 IC50 = 2.0 nM 8.70
CHEMBL381360 IC50 = 4.5 nM 8.35
CHEMBL372343 IC50 = 5.5 nM 8.26
CHEMBL202272 IC50 = 5.7 nM 8.24
CHEMBL378816 IC50 = 7.0 nM 8.15
CHEMBL201844 IC50 = 7.0 nM 8.15
CHEMBL369933 IC50 = 7.3 nM 8.14
CHEMBL371962 IC50 = 7.3 nM 8.14
CHEMBL201817 IC50 = 7.9 nM 8.10
CHEMBL408569 IC50 = 8.0 nM 8.10
CHEMBL201043 IC50 = 8.0 nM 8.10
CHEMBL370411 IC50 = 8.0 nM 8.10
CHEMBL381736 IC50 = 8.4 nM 8.08
CHEMBL199921 IC50 = 9.1 nM 8.04
CHEMBL372350 IC50 = 9.1 nM 8.04
CHEMBL372415 IC50 = 10.0 nM 8.00
CHEMBL427191 IC50 = 11.0 nM 7.96
CHEMBL201956 IC50 = 12.0 nM 7.92
CHEMBL201888 IC50 = 12.0 nM 7.92
CHEMBL425931 IC50 = 12.0 nM 7.92
CHEMBL201903 IC50 = 13.0 nM 7.89
CHEMBL382285 IC50 = 13.0 nM 7.89
CHEMBL383764 IC50 = 14.0 nM 7.85
CHEMBL372163 IC50 = 14.0 nM 7.85
CHEMBL202547 IC50 = 15.0 nM 7.82
CHEMBL202825 IC50 = 17.0 nM 7.77
CHEMBL201044 IC50 = 18.0 nM 7.75
CHEMBL369994 IC50 = 19.0 nM 7.72
CHEMBL202493 IC50 = 20.0 nM 7.70
CHEMBL201693 IC50 = 20.0 nM 7.70
CHEMBL382367 IC50 = 21.0 nM 7.68
CHEMBL201176 IC50 = 22.0 nM 7.66
CHEMBL372162 IC50 = 26.0 nM 7.58
CHEMBL202232 IC50 = 45.0 nM 7.35
CHEMBL201729 IC50 = 47.0 nM 7.33
CHEMBL202381 IC50 = 51.0 nM 7.29
CHEMBL267033 IC50 = 61.0 nM 7.21
CHEMBL383236 IC50 = 80.0 nM 7.10
CHEMBL201904 IC50 = 190.0 nM 6.72
CHEMBL370621 IC50 = 490.0 nM 6.31
CHEMBL202334 IC50 = 560.0 nM 6.25
CHEMBL382506 IC50 = 760.0 nM 6.12
CHEMBL201891 IC50 = 1800.0 nM 5.75