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Assay Detail

CHEMBL815478

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

Binding
In Vitro inhibition of Thymidine Monophosphatase Kinase (TMPKh)
10
Total Activities
10
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

Thymidine kinase, cytosolic (CHEMBL2883)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3'-C-branched-chain-substituted nucleosides and nucleotides as potent inhibitors of Mycobacterium tuberculosis thymidine monophosphate kinase.
Vanheusden V, Munier-Lehmann H, Froeyen M, Dugué L, Heyerick A, De Keukeleire D, Pochet S, Busson R, Herdewijn P, Van Calenbergh S.
J Med Chem (2003) 46 : 3811 -3821
PubMed 12930144 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 4.65 5.33

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1161004 1 5.33
CHEMBL1160994 1 4.50
CHEMBL1160993 1 4.40
CHEMBL1161003 1 4.36
CHEMBL124682 1 -
CHEMBL124260 1 -
CHEMBL340604 1 -
CHEMBL1161001 1 -
CHEMBL127523 1 -
CHEMBL341264 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1161004 Ki = 4700.0 nM 5.33
CHEMBL1160994 Ki = 32000.0 nM 4.50
CHEMBL1160993 Ki = 40000.0 nM 4.40
CHEMBL1161003 Ki = 43500.0 nM 4.36
CHEMBL124682 Ki = 110000.0 nM -
CHEMBL124260 Ki = 420000.0 nM -
CHEMBL340604 Ki = 1040000.0 nM -
CHEMBL1161001 Ki = 280000.0 nM -
CHEMBL127523 Ki = 970000.0 nM -
CHEMBL341264 Ki = 220000.0 nM -