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Assay Detail

CHEMBL832846

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

Binding
Inhibition of bovine geranylgeranyl transferase
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Geranylgeranyl transferase type I (CHEMBL2096987)
Type PROTEIN COMPLEX
Organism Bos taurus

Publication

Design, synthesis, and activity of achiral analogs of 2-quinolones and indoles as non-thiol farnesyltransferase inhibitors.
Li Q, Woods KW, Wang W, Lin NH, Claiborne A, Gu WZ, Cohen J, Stoll VS, Hutchins C, Frost D, Rosenberg SH, Sham HL.
Bioorg Med Chem Lett (2005) 15 : 2033 -2039
PubMed 15808463 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 5.93 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440564 1 6.96
CHEMBL380554 1 6.85
CHEMBL194073 1 6.57
CHEMBL193340 1 6.28
CHEMBL289228 TIPIFARNIB 3.0 1 5.96
CHEMBL194072 1 5.40
CHEMBL371818 1 4.77
CHEMBL194041 1 4.66
CHEMBL194172 1 -
CHEMBL365362 1 -
CHEMBL194143 1 -
CHEMBL195553 1 -
CHEMBL364067 1 -
CHEMBL298734 LONAFARNIB 4.0 1 -
CHEMBL373267 1 -
CHEMBL194382 1 -
CHEMBL193881 1 -
CHEMBL195730 1 -
CHEMBL370049 1 -
CHEMBL195843 1 -
CHEMBL425561 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440564 IC50 = 110.0 nM 6.96
CHEMBL380554 IC50 = 140.0 nM 6.85
CHEMBL194073 IC50 = 270.0 nM 6.57
CHEMBL193340 IC50 = 520.0 nM 6.28
CHEMBL289228 TIPIFARNIB IC50 = 1100.0 nM 5.96
CHEMBL194072 IC50 = 4000.0 nM 5.40
CHEMBL371818 IC50 = 17000.0 nM 4.77
CHEMBL194041 IC50 = 22000.0 nM 4.66
CHEMBL194172 IC50 < 10000.0 nM -
CHEMBL365362 IC50 > 10000.0 nM -
CHEMBL194143 IC50 > 10000.0 nM -
CHEMBL195553 IC50 - nM -
CHEMBL364067 IC50 - nM -
CHEMBL298734 LONAFARNIB IC50 > 10000.0 nM -
CHEMBL373267 IC50 > 10000.0 nM -
CHEMBL194382 IC50 - nM -
CHEMBL193881 IC50 - nM -
CHEMBL195730 IC50 - nM -
CHEMBL370049 IC50 - nM -
CHEMBL195843 IC50 - nM -
CHEMBL425561 IC50 > 1000.0 nM -