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Assay Detail

CHEMBL844165

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Binding
Time-independent inhibition of thymidylate synthase from FdUrd-resistant L1210 cells
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type L1210
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Thymidylate synthase (CHEMBL3160)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

5-Substituted N(4)-hydroxy-2'-deoxycytidines and their 5'-monophosphates: synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity.
Felczak K, Miazga A, Poznański J, Bretner M, Kulikowski T, Dzik JM, Gołos B, Zieliński Z, Cieśla J, Rode W.
J Med Chem (2000) 43 : 4647 -4656
PubMed 11101356 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.74 7.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL886 5-FLUORODEOXYURIDYLATE 1 7.52
CHEMBL1236538 1 6.82
CHEMBL1160593 1 6.34
CHEMBL1160818 1 6.05
CHEMBL1161226 1 5.85
CHEMBL1161224 1 5.66
CHEMBL1161225 1 5.24
CHEMBL1160594 1 5.16
CHEMBL1161232 1 5.08
CHEMBL1161227 1 5.03
CHEMBL1161231 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL886 5-FLUORODEOXYURIDYLATE Ki = 30.0 nM 7.52
CHEMBL1236538 Ki = 150.0 nM 6.82
CHEMBL1160593 Ki = 460.0 nM 6.34
CHEMBL1160818 Ki = 900.0 nM 6.05
CHEMBL1161226 Ki = 1400.0 nM 5.85
CHEMBL1161224 Ki = 2180.0 nM 5.66
CHEMBL1161225 Ki = 5700.0 nM 5.24
CHEMBL1160594 Ki = 6990.0 nM 5.16
CHEMBL1161232 Ki = 8400.0 nM 5.08
CHEMBL1161227 Ki = 9300.0 nM 5.03
CHEMBL1161231 Ki = 36600.0 nM 4.44