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Assay Detail

CHEMBL683536

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

Binding
In vitro inhibitory activity against Geranylgeranyl transferase type I
41
Total Activities
41
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Geranylgeranyl transferase type I (CHEMBL2095164)
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 41 5.91 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL128371 1 7.52
CHEMBL132283 1 7.03
CHEMBL128018 1 6.96
CHEMBL129578 1 6.92
CHEMBL128454 1 6.82
CHEMBL338695 1 6.80
CHEMBL130062 1 6.72
CHEMBL339758 1 6.66
CHEMBL335180 1 6.54
CHEMBL339801 1 6.21
CHEMBL128116 1 6.09
CHEMBL130723 1 6.05
CHEMBL336168 1 5.98
CHEMBL127898 1 5.85
CHEMBL336569 1 5.82
CHEMBL336497 1 5.82
CHEMBL131081 1 5.77
CHEMBL131609 1 5.75
CHEMBL132337 1 5.72
CHEMBL128760 1 5.70
CHEMBL131612 1 5.64
CHEMBL131108 1 5.60
CHEMBL128309 1 5.57
CHEMBL128897 1 5.54
CHEMBL128501 1 5.52
CHEMBL128834 1 5.50
CHEMBL130185 1 5.48
CHEMBL128282 1 5.48
CHEMBL424448 1 5.47
CHEMBL274954 1 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL128371 IC50 = 30.0 nM 7.52
CHEMBL132283 IC50 = 94.0 nM 7.03
CHEMBL128018 IC50 = 110.0 nM 6.96
CHEMBL129578 IC50 = 120.0 nM 6.92
CHEMBL128454 IC50 = 150.0 nM 6.82
CHEMBL338695 IC50 = 160.0 nM 6.80
CHEMBL130062 IC50 = 190.0 nM 6.72
CHEMBL339758 IC50 = 220.0 nM 6.66
CHEMBL335180 IC50 = 290.0 nM 6.54
CHEMBL339801 IC50 = 610.0 nM 6.21
CHEMBL128116 IC50 = 820.0 nM 6.09
CHEMBL130723 IC50 = 890.0 nM 6.05
CHEMBL336168 IC50 = 1045.0 nM 5.98
CHEMBL127898 IC50 = 1400.0 nM 5.85
CHEMBL336497 IC50 = 1500.0 nM 5.82
CHEMBL336569 IC50 = 1500.0 nM 5.82
CHEMBL131081 IC50 = 1700.0 nM 5.77
CHEMBL131609 IC50 = 1800.0 nM 5.75
CHEMBL132337 IC50 = 1900.0 nM 5.72
CHEMBL128760 IC50 = 2000.0 nM 5.70
CHEMBL131612 IC50 = 2300.0 nM 5.64
CHEMBL131108 IC50 = 2500.0 nM 5.60
CHEMBL128309 IC50 = 2700.0 nM 5.57
CHEMBL128897 IC50 = 2900.0 nM 5.54
CHEMBL128501 IC50 = 3000.0 nM 5.52
CHEMBL128834 IC50 = 3200.0 nM 5.50
CHEMBL130185 IC50 = 3300.0 nM 5.48
CHEMBL128282 IC50 = 3300.0 nM 5.48
CHEMBL424448 IC50 = 3400.0 nM 5.47
CHEMBL274954 IC50 = 3400.0 nM 5.47
CHEMBL334651 IC50 = 4300.0 nM 5.37
CHEMBL128267 IC50 = 5500.0 nM 5.26
CHEMBL131170 IC50 = 6200.0 nM 5.21
CHEMBL129685 IC50 = 7500.0 nM 5.12
CHEMBL338349 IC50 = 12000.0 nM 4.92
CHEMBL334490 IC50 = 15000.0 nM 4.82
CHEMBL131000 IC50 > 10000.0 nM -
CHEMBL131116 IC50 > 900.0 nM -
CHEMBL128572 IC50 > 10000.0 nM -
CHEMBL128571 IC50 > 1000.0 nM -
CHEMBL128573 IC50 > 10000.0 nM -