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Assay Detail

CHEMBL3385496

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Functional
Agonist activity at human GPR39 expressed in HEK293 cells by cAMP assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

G-protein coupled receptor 39 (CHEMBL3091266)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 2-Pyridylpyrimidines as the First Orally Bioavailable GPR39 Agonists.
Peukert S, Hughes R, Nunez J, He G, Yan Z, Jain R, Llamas L, Luchansky S, Carlson A, Liang G, Kunjathoor V, Pietropaolo M, Shapiro J, Castellana A, Wu X, Bose A.
ACS Med Chem Lett (2014) 5 : 1114 -1118
PubMed 25313322 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 9.42 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342358 1 10.22
CHEMBL3342376 1 9.74
CHEMBL3342379 1 9.46
CHEMBL3342377 1 9.26
CHEMBL1200679 ZINC CHLORIDE 4.0 1 8.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342358 EC50 = 0.06 nM 10.22
CHEMBL3342376 EC50 = 0.18 nM 9.74
CHEMBL3342379 EC50 = 0.35 nM 9.46
CHEMBL3342377 EC50 = 0.55 nM 9.26
CHEMBL1200679 ZINC CHLORIDE EC50 = 3.6 nM 8.44