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Assay Detail

CHEMBL1110028

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

Binding
Inhibition of recombinant RGGT assessed as incorporation of [3H]GGPP into His-tagged canine rab1a after 20 mins
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
McKenna CE, Kashemirov BA, Błazewska KM, Mallard-Favier I, Stewart CA, Rojas J, Lundy MW, Ebetino FH, Baron RA, Dunford JE, Kirsten ML, Seabra MC, Bala JL, Marma MS, Rogers MJ, Coxon FP.
J Med Chem (2010) 53 : 3454 -3464
PubMed 20394422 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 5.20 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1099309 (2-HYDROXY-3-IMIDAZO[1,2-A]PYRIDIN-3-YL-2-PHOSPHONOPROPIONIC ACID (ENANTIONMERS) 1 5.89
CHEMBL397829 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1099309 (2-HYDROXY-3-IMIDAZO[1,2-A]PYRIDIN-3-YL-2-PHOSPHONOPROPIONIC ACID (ENANTIONMERS) IC50 = 1300.0 nM 5.89
CHEMBL397829 IC50 = 32000.0 nM 4.50