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Assay Detail

CHEMBL871864

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

Binding
Percent inhibition against 5-hydroxytryptamine 2C receptor at 1 uM
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

5-hydroxytryptamine receptor 2C (CHEMBL225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Minetti P, Tinti MO, Carminati P, Castorina M, Di Cesare MA, Di Serio S, Gallo G, Ghirardi O, Giorgi F, Giorgi L, Piersanti G, Bartoccini F, Tarzia G.
J Med Chem (2005) 48 : 6887 -6896
PubMed 16250647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 2 - -
IC50 2 8.65 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12314 MESULERGINE 2.0 1 8.72
CHEMBL51 KETANSERIN 3.0 1 8.57
CHEMBL197669 ST1535 1.0 1 -
CHEMBL196258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12314 MESULERGINE IC50 = 1.9 nM 8.72
CHEMBL51 KETANSERIN IC50 = 2.7 nM 8.57
CHEMBL197669 ST1535 Inhibition < 10.0 % -
CHEMBL196258 Inhibition < 10.0 % -