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Assay Detail

CHEMBL682228

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Binding
In vitro inhibitory activity against farnesyltransferase (FT)
ChEMBL ↗
44
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

Pyridone-containing farnesyltransferase inhibitors: synthesis and biological evaluation.
Hasvold LA, Wang W, Gwaltney SL, Rockway TW, Nelson LT, Mantei RA, Fakhoury SA, Sullivan GM, Li Q, Lin NH, Wang L, Zhang H, Cohen J, Gu WZ, Marsh K, Bauch J, Rosenberg S, Sham HL.
Bioorg Med Chem Lett (2003) 13 : 4001 -4005
PubMed 14592494 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 44 8.93 10.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128501 — — 1 10.44
CHEMBL128454 — — 1 9.44
CHEMBL128834 — — 1 9.39
CHEMBL130185 — — 1 9.38
CHEMBL336168 — — 1 9.38
CHEMBL335180 — — 1 9.38
CHEMBL128309 — — 1 9.36
CHEMBL131081 — — 1 9.34
CHEMBL131612 — — 1 9.31
CHEMBL128760 — — 1 9.30
CHEMBL424448 — — 1 9.29
CHEMBL336497 — — 1 9.17
CHEMBL131170 — — 1 9.16
CHEMBL131609 — — 1 9.15
CHEMBL128282 — — 1 9.14
CHEMBL127898 — — 1 9.14
CHEMBL43631 — — 1 9.14
CHEMBL128571 — — 1 9.12
CHEMBL130062 — — 1 9.11
CHEMBL129685 — — 1 9.09
CHEMBL338349 — — 1 9.08
CHEMBL128116 — — 1 9.07
CHEMBL339758 — — 1 9.05
CHEMBL130723 — — 1 9.01
CHEMBL132283 — — 1 9.00
CHEMBL132337 — — 1 8.96
CHEMBL29982 — — 1 8.96
CHEMBL128371 — — 1 8.89
CHEMBL339801 — — 1 8.89
CHEMBL128267 — — 1 8.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128501 — IC50 = 0.036 nM 10.44
CHEMBL128454 — IC50 = 0.36 nM 9.44
CHEMBL128834 — IC50 = 0.41 nM 9.39
CHEMBL130185 — IC50 = 0.42 nM 9.38
CHEMBL336168 — IC50 = 0.42 nM 9.38
CHEMBL335180 — IC50 = 0.42 nM 9.38
CHEMBL128309 — IC50 = 0.44 nM 9.36
CHEMBL131081 — IC50 = 0.46 nM 9.34
CHEMBL131612 — IC50 = 0.49 nM 9.31
CHEMBL128760 — IC50 = 0.5 nM 9.30
CHEMBL424448 — IC50 = 0.51 nM 9.29
CHEMBL336497 — IC50 = 0.67 nM 9.17
CHEMBL131170 — IC50 = 0.69 nM 9.16
CHEMBL131609 — IC50 = 0.7 nM 9.15
CHEMBL43631 — IC50 = 0.73 nM 9.14
CHEMBL128282 — IC50 = 0.73 nM 9.14
CHEMBL127898 — IC50 = 0.73 nM 9.14
CHEMBL128571 — IC50 = 0.75 nM 9.12
CHEMBL130062 — IC50 = 0.77 nM 9.11
CHEMBL129685 — IC50 = 0.81 nM 9.09
CHEMBL338349 — IC50 = 0.84 nM 9.08
CHEMBL128116 — IC50 = 0.85 nM 9.07
CHEMBL339758 — IC50 = 0.89 nM 9.05
CHEMBL130723 — IC50 = 0.97 nM 9.01
CHEMBL132283 — IC50 = 1.0 nM 9.00
CHEMBL132337 — IC50 = 1.1 nM 8.96
CHEMBL29982 — IC50 = 1.1 nM 8.96
CHEMBL128371 — IC50 = 1.3 nM 8.89
CHEMBL339801 — IC50 = 1.3 nM 8.89
CHEMBL128267 — IC50 = 1.5 nM 8.82
CHEMBL128897 — IC50 = 1.6 nM 8.80
CHEMBL336569 — IC50 = 1.8 nM 8.74
CHEMBL128572 — IC50 = 1.9 nM 8.72
CHEMBL129578 — IC50 = 2.0 nM 8.70
CHEMBL131000 — IC50 = 2.1 nM 8.68
CHEMBL334490 — IC50 = 2.7 nM 8.57
CHEMBL128018 — IC50 = 3.9 nM 8.41
CHEMBL131116 — IC50 = 5.3 nM 8.28
CHEMBL334651 — IC50 = 5.5 nM 8.26
CHEMBL131108 — IC50 = 6.1 nM 8.21
CHEMBL274954 — IC50 = 6.3 nM 8.20
CHEMBL338695 — IC50 = 6.5 nM 8.19
CHEMBL128573 — IC50 = 9.9 nM 8.00
CHEMBL131165 — IC50 = 71.0 nM 7.15