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Assay Detail

CHEMBL3267242

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Functional
Agonist activity at mouse GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Mus musculus
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Glucose-dependent insulinotropic receptor (CHEMBL5263)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R.
Bioorg Med Chem Lett (2014) 24 : 2383 -2387
PubMed 24751443 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.34 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3260533 1 7.72
CHEMBL3260540 1 7.41
CHEMBL3260536 1 7.31
CHEMBL3260518 1 7.12
CHEMBL3260506 1 7.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3260533 EC50 = 19.0 nM 7.72
CHEMBL3260540 EC50 = 39.0 nM 7.41
CHEMBL3260536 EC50 = 49.0 nM 7.31
CHEMBL3260518 EC50 = 76.0 nM 7.12
CHEMBL3260506 EC50 = 76.0 nM 7.12