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Assay Detail

CHEMBL679699

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Binding
Inhibitory activity against farnesyltransferase (FT) using SPA assay
34
Total Activities
34
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

Potent inhibitors of protein farnesyltransferase: heteroarenes as cysteine replacements.
Shen W, Fakhoury S, Donner G, Henry K, Lee J, Zhang H, Cohen J, Warner R, Saeed B, Cherian S, Tahir S, Kovar P, Bauch J, Ng SC, Marsh K, Sham H, Rosenberg S.
Bioorg Med Chem Lett (1999) 9 : 703 -708
PubMed 10201832 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 34 8.83 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436440 1 9.92
CHEMBL163383 1 9.82
CHEMBL159400 1 9.70
CHEMBL159764 1 9.68
CHEMBL163102 1 9.54
CHEMBL433519 1 9.54
CHEMBL164480 1 9.52
CHEMBL347874 1 9.43
CHEMBL274122 1 9.40
CHEMBL54044 1 9.29
CHEMBL352208 1 9.27
CHEMBL159390 1 9.24
CHEMBL159324 1 9.23
CHEMBL349051 1 9.21
CHEMBL350180 1 9.20
CHEMBL162868 1 9.18
CHEMBL164366 1 9.10
CHEMBL163559 1 9.09
CHEMBL262187 1 9.04
CHEMBL164259 1 9.04
CHEMBL164537 1 8.85
CHEMBL423459 1 8.68
CHEMBL163331 1 8.62
CHEMBL350566 1 8.57
CHEMBL159326 1 8.54
CHEMBL164408 1 8.44
CHEMBL348838 1 8.33
CHEMBL351869 1 7.92
CHEMBL162842 1 7.82
CHEMBL159928 1 7.80

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436440 IC50 = 0.12 nM 9.92
CHEMBL163383 IC50 = 0.15 nM 9.82
CHEMBL159400 IC50 = 0.2 nM 9.70
CHEMBL159764 IC50 = 0.21 nM 9.68
CHEMBL163102 IC50 = 0.29 nM 9.54
CHEMBL433519 IC50 = 0.29 nM 9.54
CHEMBL164480 IC50 = 0.3 nM 9.52
CHEMBL347874 IC50 = 0.37 nM 9.43
CHEMBL274122 IC50 = 0.4 nM 9.40
CHEMBL54044 IC50 = 0.51 nM 9.29
CHEMBL352208 IC50 = 0.54 nM 9.27
CHEMBL159390 IC50 = 0.58 nM 9.24
CHEMBL159324 IC50 = 0.59 nM 9.23
CHEMBL349051 IC50 = 0.61 nM 9.21
CHEMBL350180 IC50 = 0.63 nM 9.20
CHEMBL162868 IC50 = 0.66 nM 9.18
CHEMBL164366 IC50 = 0.8 nM 9.10
CHEMBL163559 IC50 = 0.81 nM 9.09
CHEMBL262187 IC50 = 0.91 nM 9.04
CHEMBL164259 IC50 = 0.92 nM 9.04
CHEMBL164537 IC50 = 1.4 nM 8.85
CHEMBL423459 IC50 = 2.1 nM 8.68
CHEMBL163331 IC50 = 2.4 nM 8.62
CHEMBL350566 IC50 = 2.7 nM 8.57
CHEMBL159326 IC50 = 2.9 nM 8.54
CHEMBL164408 IC50 = 3.6 nM 8.44
CHEMBL348838 IC50 = 4.7 nM 8.33
CHEMBL351869 IC50 = 12.0 nM 7.92
CHEMBL162842 IC50 = 15.0 nM 7.82
CHEMBL159928 IC50 = 16.0 nM 7.80
CHEMBL163270 IC50 = 25.0 nM 7.60
CHEMBL163444 IC50 = 26.0 nM 7.58
CHEMBL161476 IC50 = 57.0 nM 7.24
CHEMBL162959 IC50 = 140.0 nM 6.85