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Assay Detail

CHEMBL681444

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

Binding
Inhibition of GAR transformylase isolated from murine lymphoma cell line L5178Y
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Cell Type lymphoma
Confidence 9 — Direct single protein target
Curated By Expert

Target

Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3690)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

N10-substituted 5,8-dideazafolate inhibitors of glycinamide ribonucleotide transformylase.
Caperelli CA.
J Med Chem (1987) 30 : 1254 -1256
PubMed 3599031 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.17 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL22344 1 5.89
CHEMBL23977 DIDEAZAFOLATE 1 5.70
CHEMBL22798 1 5.52
CHEMBL22626 1 5.30
CHEMBL422395 1 5.22
CHEMBL23035 1 5.16
CHEMBL25108 1 5.10
CHEMBL25107 1 4.96
CHEMBL22668 1 4.75
CHEMBL282270 1 4.72
CHEMBL415251 1 4.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL22344 Ki = 1300.0 nM 5.89
CHEMBL23977 DIDEAZAFOLATE Ki = 2000.0 nM 5.70
CHEMBL22798 Ki = 3000.0 nM 5.52
CHEMBL22626 Ki = 5000.0 nM 5.30
CHEMBL422395 Ki = 6000.0 nM 5.22
CHEMBL23035 Ki = 7000.0 nM 5.16
CHEMBL25108 Ki = 8000.0 nM 5.10
CHEMBL25107 Ki = 11000.0 nM 4.96
CHEMBL22668 Ki = 18000.0 nM 4.75
CHEMBL282270 Ki = 19000.0 nM 4.72
CHEMBL415251 Ki = 32000.0 nM 4.50