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Assay Detail

CHEMBL615270

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

Binding
Initial dissociation constant towards human 5'-methylthioadenosine phosphorylase
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

S-methyl-5'-thioadenosine phosphorylase (CHEMBL4941)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Targeting the polyamine pathway with transition-state analogue inhibitors of 5'-methylthioadenosine phosphorylase.
Evans GB, Furneaux RH, Schramm VL, Singh V, Tyler PC.
J Med Chem (2004) 47 : 3275 -3281
PubMed 15163207 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 7.83 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL552894 1 9.24
CHEMBL542449 1 8.86
CHEMBL545042 1 8.44
CHEMBL544806 1 8.40
CHEMBL544110 1 8.36
CHEMBL545740 1 8.19
CHEMBL553982 1 8.19
CHEMBL554965 1 8.04
CHEMBL542694 1 7.70
CHEMBL554642 1 7.58
CHEMBL554322 1 7.58
CHEMBL542452 1 7.36
CHEMBL542697 1 7.25
CHEMBL553375 1 7.05
CHEMBL544574 1 6.87
CHEMBL545273 1 6.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL552894 Ki = 0.576 nM 9.24
CHEMBL542449 Ki = 1.39 nM 8.86
CHEMBL545042 Ki = 3.6 nM 8.44
CHEMBL544806 Ki = 4.0 nM 8.40
CHEMBL544110 Ki = 4.4 nM 8.36
CHEMBL545740 Ki = 6.4 nM 8.19
CHEMBL553982 Ki = 6.4 nM 8.19
CHEMBL554965 Ki = 9.2 nM 8.04
CHEMBL542694 Ki = 20.0 nM 7.70
CHEMBL554642 Ki = 26.0 nM 7.58
CHEMBL554322 Ki = 26.0 nM 7.58
CHEMBL542452 Ki = 44.0 nM 7.36
CHEMBL542697 Ki = 56.0 nM 7.25
CHEMBL553375 Ki = 90.0 nM 7.05
CHEMBL544574 Ki = 134.0 nM 6.87
CHEMBL545273 Ki = 720.0 nM 6.14