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Assay Detail

CHEMBL678807

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

Binding
In vitro inhibition of hog liver GAR transformylase with (6R)-10-formyl-FH4 as cofactor
13
Total Activities
13
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Sus scrofa
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Trifunctional purine biosynthetic protein adenosine-3 (CHEMBL3972)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological activity of open-chain analogues of 5,6,7,8-tetrahydrofolic acid--potential antitumor agents.
Bigham EC, Hodson SJ, Mallory WR, Wilson D, Duch DS, Smith GK, Ferone R.
J Med Chem (1992) 35 : 1399 -1410
PubMed 1573633 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 5.33 6.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL170101 1 6.66
CHEMBL13705 DIDEAZAACYCLOTETRAHYDROFOLIC ACID 1 5.80
CHEMBL30842 1 5.58
CHEMBL13659 1 5.52
CHEMBL31176 1 5.51
CHEMBL285232 1 5.46
CHEMBL31609 1 5.28
CHEMBL30301 1 5.21
CHEMBL417304 1 5.18
CHEMBL30364 1 4.74
CHEMBL29713 1 4.73
CHEMBL31027 1 4.28
CHEMBL31107 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL170101 IC50 = 220.0 nM 6.66
CHEMBL13705 DIDEAZAACYCLOTETRAHYDROFOLIC ACID IC50 = 1600.0 nM 5.80
CHEMBL30842 IC50 = 2600.0 nM 5.58
CHEMBL13659 IC50 = 3000.0 nM 5.52
CHEMBL31176 IC50 = 3100.0 nM 5.51
CHEMBL285232 IC50 = 3500.0 nM 5.46
CHEMBL31609 IC50 = 5300.0 nM 5.28
CHEMBL30301 IC50 = 6100.0 nM 5.21
CHEMBL417304 IC50 = 6600.0 nM 5.18
CHEMBL30364 IC50 = 18200.0 nM 4.74
CHEMBL29713 IC50 = 18700.0 nM 4.73
CHEMBL31027 IC50 = 52000.0 nM 4.28
CHEMBL31107 IC50 > 100000.0 nM -