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Assay Detail

CHEMBL814568

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Binding
Inhibition of Thymidylate synthase of Escherichia coli (Ki)
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Escherichia coli
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Thymidylate synthase (CHEMBL6137)
Type SINGLE PROTEIN
Organism Escherichia coli

Publication

Design of enzyme inhibitors using iterative protein crystallographic analysis.
Appelt K, Bacquet RJ, Bartlett CA, Booth CL, Freer ST, Fuhry MA, Gehring MR, Herrmann SM, Howland EF, Janson CA.
J Med Chem (1991) 34 : 1925 -1934
PubMed 2066965 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 6.53 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL422395 1 8.52
CHEMBL25889 1 8.32
CHEMBL417222 1 7.60
CHEMBL291548 1 7.43
CHEMBL301256 1 7.37
CHEMBL56662 1 6.85
CHEMBL299928 1 6.82
CHEMBL301423 1 6.35
CHEMBL275685 1 5.82
CHEMBL57333 1 5.40
CHEMBL353700 1 5.31
CHEMBL57002 1 4.68
CHEMBL56992 1 4.42
CHEMBL301844 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL422395 Ki = 3.0 nM 8.52
CHEMBL25889 Ki = 4.8 nM 8.32
CHEMBL417222 Ki = 25.0 nM 7.60
CHEMBL291548 Ki = 37.0 nM 7.43
CHEMBL301256 Ki = 43.0 nM 7.37
CHEMBL56662 Ki = 140.0 nM 6.85
CHEMBL299928 Ki = 150.0 nM 6.82
CHEMBL301423 Ki = 450.0 nM 6.35
CHEMBL275685 Ki = 1500.0 nM 5.82
CHEMBL57333 Ki = 4000.0 nM 5.40
CHEMBL353700 Ki = 4900.0 nM 5.31
CHEMBL57002 Ki = 21000.0 nM 4.68
CHEMBL56992 Ki = 38000.0 nM 4.42
CHEMBL301844 Ki > 1000.0 nM -