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Assay Detail

CHEMBL734264

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Binding
Competitive inhibition against rat mitochondrial thymidine kinase
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Thymidine kinase 2 (CHEMBL5489)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Species- or isozyme-specific enzyme inhibitors. 5. Differential effects of thymidine substituents on affinity for rat thymidine kinase isozymes.
Hampton A, Chawla RR, Kappler F.
J Med Chem (1982) 25 : 644 -649
PubMed 7097717 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 4.50 5.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3143486 1 5.10
CHEMBL2111285 1 4.96
CHEMBL22539 1 4.21
CHEMBL3143491 1 4.14
CHEMBL3143492 1 4.11
CHEMBL157402 1 -
CHEMBL991 STAVUDINE 4.0 1 -
CHEMBL319447 1 -
CHEMBL103356 3-AMINO- 3-DEOXYTHYMIDINE 1 -
CHEMBL156488 1 -
CHEMBL444314 1 -
CHEMBL66115 DOXECITINE 2.0 1 -
CHEMBL3143490 1 -
CHEMBL373855 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3143486 Ki = 8000.0 nM 5.10
CHEMBL2111285 Ki = 11000.0 nM 4.96
CHEMBL22539 Ki = 62000.0 nM 4.21
CHEMBL3143491 Ki = 72000.0 nM 4.14
CHEMBL3143492 Ki = 77000.0 nM 4.11
CHEMBL157402 Ki = 960000.0 nM -
CHEMBL991 STAVUDINE Ki = 3250000.0 nM -
CHEMBL319447 Ki = 4600000.0 nM -
CHEMBL103356 3-AMINO- 3-DEOXYTHYMIDINE Ki = 2600000.0 nM -
CHEMBL156488 Ki = 1440000.0 nM -
CHEMBL444314 Ki = 880000.0 nM -
CHEMBL66115 DOXECITINE Ki = 320000.0 nM -
CHEMBL3143490 Ki = 1100000.0 nM -
CHEMBL373855 Ki = 250000.0 nM -