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Assay Detail

CHEMBL809138

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

Binding
Inhibitory activity against squalene hopene cyclase from Alicyclobacillus acidocaldarius expressed in Escherichia coli
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Alicyclobacillus acidocaldarius
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Squalene--hopene cyclase (CHEMBL3569)
Type SINGLE PROTEIN
Organism Alicyclobacillus acidocaldarius subsp. acidocaldarius (strain ATCC27009 / DSM 446 / 104-1A) (Bacillus acidocaldarius)

Publication

Farnesyloxycoumarins, a new class of squalene-hopene cyclase inhibitors.
Cravotto G, Balliano G, Robaldo B, Oliaro-Bosso S, Chimichi S, Boccalini M.
Bioorg Med Chem Lett (2004) 14 : 1931 -1934
PubMed 15050630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 4.64 5.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL367931 1 5.82
CHEMBL427120 1 5.60
CHEMBL177697 FARNESIFEROL C 1 5.16
CHEMBL178219 1 4.19
CHEMBL174435 1 4.17
CHEMBL156127 UMBELLIPRENIN 1 4.16
CHEMBL174839 FERULENOL 1 4.05
CHEMBL178379 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL367931 IC50 = 1500.0 nM 5.82
CHEMBL427120 IC50 = 2500.0 nM 5.60
CHEMBL177697 FARNESIFEROL C IC50 = 7000.0 nM 5.16
CHEMBL178219 IC50 = 65000.0 nM 4.19
CHEMBL174435 IC50 = 67000.0 nM 4.17
CHEMBL156127 UMBELLIPRENIN IC50 = 70000.0 nM 4.16
CHEMBL174839 FERULENOL IC50 = 90000.0 nM 4.05
CHEMBL178379 IC50 = 100000.0 nM 4.00