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Assay Detail

CHEMBL847432

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Binding
Inhibitory activity against eubacterial tRNA guanine transglycosylase (TGT) from Zymomonas mobilis
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Zymomonas mobilis
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Queuine tRNA-ribosyltransferase (CHEMBL2987)
Type SINGLE PROTEIN
Organism Zymomonas mobilis (strain ATCC 31821 / ZM4 / CP4)

Publication

Virtual screening for submicromolar leads of tRNA-guanine transglycosylase based on a new unexpected binding mode detected by crystal structure analysis.
Brenk R, Naerum L, Grädler U, Gerber HD, Garcia GA, Reuter K, Stubbs MT, Klebe G.
J Med Chem (2003) 46 : 1133 -1143
PubMed 12646024 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 5.37 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL14926 1 7.00
CHEMBL14913 1 6.60
CHEMBL418720 1 6.52
CHEMBL278009 PTERINE 1 6.22
CHEMBL276808 1 5.57
CHEMBL277561 1 5.42
CHEMBL277134 1 5.33
CHEMBL278733 1 5.30
CHEMBL14996 1 5.09
CHEMBL14882 1 5.08
CHEMBL442329 1 4.44
CHEMBL14940 1 4.43
CHEMBL277783 1 4.14
CHEMBL280051 1 4.08
CHEMBL15221 1 -
CHEMBL15047 1 -
CHEMBL275408 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL14926 Ki = 100.0 nM 7.00
CHEMBL14913 Ki = 250.0 nM 6.60
CHEMBL418720 Ki = 300.0 nM 6.52
CHEMBL278009 PTERINE Ki = 600.0 nM 6.22
CHEMBL276808 Ki = 2700.0 nM 5.57
CHEMBL277561 Ki = 3800.0 nM 5.42
CHEMBL277134 Ki = 4700.0 nM 5.33
CHEMBL278733 Ki = 5000.0 nM 5.30
CHEMBL14996 Ki = 8100.0 nM 5.09
CHEMBL14882 Ki = 8300.0 nM 5.08
CHEMBL442329 Ki = 36000.0 nM 4.44
CHEMBL14940 Ki = 37000.0 nM 4.43
CHEMBL277783 Ki = 72000.0 nM 4.14
CHEMBL280051 Ki = 83000.0 nM 4.08
CHEMBL15221 Ki = 156000.0 nM -
CHEMBL15047 Ki = 200000.0 nM -
CHEMBL275408 Ki = 249000.0 nM -