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Assay Detail

CHEMBL811641

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

Binding
Affinity towards RFC (Reduced folate carrier) measured by the inhibition of [3H]MTX uptake
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Thymidylate synthase (CHEMBL5328)
Type SINGLE PROTEIN
Organism Lactobacillus casei

Publication

Design and synthesis of Cyclopenta[g]quinazoline-based antifolates as inhibitors of thymidylate synthase and potential antitumor agents(,).
Bavetsias V, Marriott JH, Melin C, Kimbell R, Matusiak ZS, Boyle FT, Jackman AL.
J Med Chem (2000) 43 : 1910 -1926
PubMed 10821704 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 4.66 5.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL55437 1 5.22
CHEMBL59261 1 4.85
CHEMBL57269 1 4.40
CHEMBL299273 1 4.16
CHEMBL293148 1 -
CHEMBL301895 1 -
CHEMBL61300 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL55437 Ki = 6000.0 nM 5.22
CHEMBL59261 Ki = 14000.0 nM 4.85
CHEMBL57269 Ki = 40000.0 nM 4.40
CHEMBL299273 Ki = 69000.0 nM 4.16
CHEMBL293148 Ki = 150000.0 nM -
CHEMBL301895 Ki = 200000.0 nM -
CHEMBL61300 Ki = 106000.0 nM -