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Assay Detail

CHEMBL3224412

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Binding
Competitive reversible inhibition of Strepotomyces coelicolor type 2 dehydroquinase expressed in Escherichia coli BL21 (DE3) cells assessed as enone-carboxylate chromophore of 3-dehydroshikimate formation using 3-dehydroquinate as substrate preincubated with enzyme for 3 mins prior to substrate addition by UV spectrophotometric assay
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Streptomyces coelicolor
Cell Type BL21-DE3
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

3-dehydroquinate dehydratase (CHEMBL5276)
Type SINGLE PROTEIN
Organism Streptomyces coelicolor (strain ATCC BAA-471 / A3(2) / M145)

Publication

Rapid assembly of potent type II dehydroquinase inhibitors viaClick chemistry
Tran AT, Cergol KM, Britton WJ, Imran Bokhari SA, Ibrahim M, Lapthorn AJ, Payne RJ
Medchemcomm (2010) 1 : 271 -275
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.25 8.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1823559 1 8.24
CHEMBL3221803 1 8.24
CHEMBL3221799 1 7.54
CHEMBL3221802 1 7.32
CHEMBL3221805 1 7.14
CHEMBL3221800 1 7.11
CHEMBL3221804 1 6.66
CHEMBL3221801 1 5.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1823559 Ki = 5.7 nM 8.24
CHEMBL3221803 Ki = 5.7 nM 8.24
CHEMBL3221799 Ki = 29.0 nM 7.54
CHEMBL3221802 Ki = 48.0 nM 7.32
CHEMBL3221805 Ki = 73.0 nM 7.14
CHEMBL3221800 Ki = 78.0 nM 7.11
CHEMBL3221804 Ki = 217.0 nM 6.66
CHEMBL3221801 Ki = 1720.0 nM 5.76