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Assay Detail

CHEMBL817302

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

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Thymidylate synthase (CHEMBL1952)
Type SINGLE PROTEIN
Organism Homo sapiens

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 6.82 8.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL25889 1 8.07
CHEMBL422395 1 7.92
CHEMBL417222 1 7.89
CHEMBL275685 1 7.51
CHEMBL301256 1 7.51
CHEMBL291548 1 7.30
CHEMBL56662 1 7.19
CHEMBL299928 1 7.16
CHEMBL301423 1 6.41
CHEMBL301844 1 6.11
CHEMBL57002 1 6.08
CHEMBL57333 1 5.66
CHEMBL56992 1 5.52
CHEMBL353700 1 5.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL25889 Ki = 8.5 nM 8.07
CHEMBL422395 Ki = 12.0 nM 7.92
CHEMBL417222 Ki = 13.0 nM 7.89
CHEMBL275685 Ki = 31.0 nM 7.51
CHEMBL301256 Ki = 31.0 nM 7.51
CHEMBL291548 Ki = 50.0 nM 7.30
CHEMBL56662 Ki = 64.0 nM 7.19
CHEMBL299928 Ki = 69.0 nM 7.16
CHEMBL301423 Ki = 390.0 nM 6.41
CHEMBL301844 Ki = 770.0 nM 6.11
CHEMBL57002 Ki = 840.0 nM 6.08
CHEMBL57333 Ki = 2200.0 nM 5.66
CHEMBL56992 Ki = 3000.0 nM 5.52
CHEMBL353700 Ki = 7700.0 nM 5.11