Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL5048366

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

Binding
Inhibition of human FPPS expressed in Escherichia coli BL21 (DE3) preincubated for 10 mins in presence compound relative to control
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Farnesyl pyrophosphate synthase (CHEMBL1782)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and Evaluation of Structurally Diverse C-2-Substituted Thienopyrimidine-Based Inhibitors of the Human Geranylgeranyl Pyrophosphate Synthase.
Lee HF, Lacbay CM, Boutin R, Matralis AN, Park J, Waller DD, Guan TL, Sebag M, Tsantrizos YS.
J Med Chem (2022) 65 : 2471 -2496
PubMed 35077178 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 6.43 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL434024 1 8.40
CHEMBL5088349 1 6.34
CHEMBL2347859 1 6.26
CHEMBL5082193 1 6.14
CHEMBL4577077 1 5.89
CHEMBL4465832 1 5.52
CHEMBL5080121 1 -
CHEMBL5089506 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL434024 IC50 = 4.0 nM 8.40
CHEMBL5088349 IC50 = 460.0 nM 6.34
CHEMBL2347859 IC50 = 550.0 nM 6.26
CHEMBL5082193 IC50 = 730.0 nM 6.14
CHEMBL4577077 IC50 = 1300.0 nM 5.89
CHEMBL4465832 IC50 = 3000.0 nM 5.52
CHEMBL5080121 IC50 - -
CHEMBL5089506 IC50 - -