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Assay Detail

CHEMBL3096580

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

Functional
Agonist activity at recombinant human GPR39 expressed in CHO-K1 cells assessed as increase of Zn2+-induced cAMP production preincubated for 30 mins measured after 60 mins
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Chemical Probe Identification Platform for Orphan GPCRs Using Focused Compound Screening: GPR39 as a Case Example.
Boehm M, Hepworth D, Loria PM, Norquay LD, Filipski KJ, Chin JE, Cameron KO, Brenner M, Bonnette P, Cabral S, Conn E, Ebner DC, Gautreau D, Hadcock J, Lee EC, Mathiowetz AM, Morin M, Rogers L, Smith A, VanVolkenburg M, Carpino PA.
ACS Med Chem Lett (2013) 4 : 1079 -1084
PubMed 24900608 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 5.72 6.51

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092411 1 6.51
CHEMBL3092410 1 6.08
CHEMBL3092412 1 5.35
CHEMBL3092413 1 4.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092411 EC50 = 310.0 nM 6.51
CHEMBL3092410 EC50 = 840.0 nM 6.08
CHEMBL3092412 EC50 = 4500.0 nM 5.35
CHEMBL3092413 EC50 = 12000.0 nM 4.92