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Assay Detail

CHEMBL1947458

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

Binding
Reversible inhibition of Clostridium perfringens ATCC 10543 sialidase Nan1 c-terminal catalytic domain using 4-methylumbelliferyl-alpha-D-N-acetylneuraminic acid sodium salt hydrate as substrate compound pre-incubated prior to substrate addition by fluorimetric analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Selective and slow-binding inhibition of shikonin derivatives isolated from Lithospermum erythrorhizon on glycosyl hydrolase 33 and 34 sialidases.
Kim JY, Jeong HJ, Park JY, Kim YM, Park SJ, Cho JK, Park KH, Ryu YB, Lee WS.
Bioorg Med Chem (2012) 20 : 1740 -1748
PubMed 22300884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 5.99 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1944654 SHIKONOFURAN E 1 7.30
CHEMBL1946217 SHIKONOFURAN C 1 6.82
CHEMBL1946216 SHIKONOFURAN D 1 6.68
CHEMBL9416 ISOBUTYLSHIKONIN 1 6.58
CHEMBL403516 ACETYLSHIKONIN 1 6.00
CHEMBL267024 DIMETHYLACRYLSHIKONIN 1 5.76
CHEMBL397309 BETA-HYDROXYISOVALERYLSHIKONIN 1 5.65
CHEMBL486627 DEOXYSHIKONIN 1 4.92
CHEMBL9470 SHIKONIN 1 4.23

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1944654 SHIKONOFURAN E Ki = 50.0 nM 7.30
CHEMBL1946217 SHIKONOFURAN C Ki = 150.0 nM 6.82
CHEMBL1946216 SHIKONOFURAN D Ki = 210.0 nM 6.68
CHEMBL9416 ISOBUTYLSHIKONIN Ki = 260.0 nM 6.58
CHEMBL403516 ACETYLSHIKONIN Ki = 1010.0 nM 6.00
CHEMBL267024 DIMETHYLACRYLSHIKONIN Ki = 1750.0 nM 5.76
CHEMBL397309 BETA-HYDROXYISOVALERYLSHIKONIN Ki = 2240.0 nM 5.65
CHEMBL486627 DEOXYSHIKONIN Ki = 11900.0 nM 4.92
CHEMBL9470 SHIKONIN Ki = 58800.0 nM 4.23