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Assay Detail

CHEMBL1000392

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

Binding
Inhibition of human recombinant GAR transformylase
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase.
DeMartino JK, Hwang I, Connelly S, Wilson IA, Boger DL.
J Med Chem (2008) 51 : 5441 -5448
PubMed 18686942 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 6.53 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL451819 1 7.85
CHEMBL451818 1 7.82
CHEMBL34412 LOMETREXOL 2.0 1 7.22
CHEMBL452322 1 6.75
CHEMBL453090 1 6.68
CHEMBL452324 1 6.07
CHEMBL452837 1 5.96
CHEMBL453089 1 5.96
CHEMBL508910 1 5.92
CHEMBL453348 1 5.85
CHEMBL13705 DIDEAZAACYCLOTETRAHYDROFOLIC ACID 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL451819 Ki = 14.0 nM 7.85
CHEMBL451818 Ki = 15.0 nM 7.82
CHEMBL34412 LOMETREXOL Ki = 60.0 nM 7.22
CHEMBL452322 Ki = 180.0 nM 6.75
CHEMBL453090 Ki = 210.0 nM 6.68
CHEMBL452324 Ki = 850.0 nM 6.07
CHEMBL452837 Ki = 1100.0 nM 5.96
CHEMBL453089 Ki = 1100.0 nM 5.96
CHEMBL508910 Ki = 1200.0 nM 5.92
CHEMBL453348 Ki = 1400.0 nM 5.85
CHEMBL13705 DIDEAZAACYCLOTETRAHYDROFOLIC ACID Ki = 1700.0 nM 5.77