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Assay Detail

CHEMBL873990

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

Binding
In Vitro inhibition of Thymidine Monophosphatase Kinase of Mycobacterium tuberculosis (TMPKm)
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mycobacterium tuberculosis
Confidence 9 — Direct single protein target
Curated By Expert

Target

Thymidylate kinase (CHEMBL2361)
Type SINGLE PROTEIN
Organism Mycobacterium tuberculosis

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 18 4.61 5.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL257695 AZIDOTHYMIDINE MONOPHOSPHATE 1 5.00
CHEMBL1161004 1 4.98
CHEMBL1160994 1 4.92
CHEMBL1160993 1 4.82
CHEMBL52609 DOXRIBTIMINE 2.0 1 4.57
CHEMBL1160596 1 4.57
CHEMBL129 ZIDOVUDINE 4.0 1 4.55
CHEMBL1161003 1 4.54
CHEMBL340604 1 4.40
CHEMBL124260 1 4.39
CHEMBL127523 1 4.35
CHEMBL341264 1 4.24
CHEMBL124814 1 -
CHEMBL124682 1 -
CHEMBL1161002 1 -
CHEMBL1160597 1 -
CHEMBL1161001 1 -
CHEMBL123912 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL257695 AZIDOTHYMIDINE MONOPHOSPHATE Ki = 10000.0 nM 5.00
CHEMBL1161004 Ki = 10500.0 nM 4.98
CHEMBL1160994 Ki = 12000.0 nM 4.92
CHEMBL1160993 Ki = 15000.0 nM 4.82
CHEMBL52609 DOXRIBTIMINE Ki = 27000.0 nM 4.57
CHEMBL1160596 Ki = 27000.0 nM 4.57
CHEMBL129 ZIDOVUDINE Ki = 28000.0 nM 4.55
CHEMBL1161003 Ki = 29000.0 nM 4.54
CHEMBL340604 Ki = 40000.0 nM 4.40
CHEMBL124260 Ki = 41000.0 nM 4.39
CHEMBL127523 Ki = 45000.0 nM 4.35
CHEMBL341264 Ki = 57000.0 nM 4.24
CHEMBL124814 Ki = 156000.0 nM -
CHEMBL124682 Ki = 393000.0 nM -
CHEMBL1161002 Ki = 116000.0 nM -
CHEMBL1160597 Ki = 235000.0 nM -
CHEMBL1161001 Ki = 315000.0 nM -
CHEMBL123912 Ki = 770000.0 nM -