Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL1772425

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

Functional
Agonist activity at mouse GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins by HTRF assay
40
Total Activities
36
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

Design of potent and selective GPR119 agonists for type II diabetes.
Szewczyk JW, Acton J, Adams AD, Chicchi G, Freeman S, Howard AD, Huang Y, Li C, Meinke PT, Mosely R, Murphy E, Samuel R, Santini C, Yang M, Zhang Y, Zhao K, Wood HB.
Bioorg Med Chem Lett (2011) 21 : 2665 -2669
PubMed 21273063 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 7.46 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1771098 3 9.40
CHEMBL1771104 1 9.10
CHEMBL1771103 1 8.70
CHEMBL1771082 1 8.70
CHEMBL1771081 1 8.70
CHEMBL1771102 1 8.40
CHEMBL1771100 1 8.40
CHEMBL1771101 1 8.22
CHEMBL1771092 1 8.10
CHEMBL1770161 1 8.10
CHEMBL1771097 2 8.05
CHEMBL1771094 1 8.00
CHEMBL1771079 1 7.96
CHEMBL1771093 1 7.96
CHEMBL1771099 2 7.75
CHEMBL1771080 1 7.51
CHEMBL1771068 1 7.44
CHEMBL1771091 1 7.39
CHEMBL1771086 1 7.35
CHEMBL1771096 1 7.19
CHEMBL1771090 1 7.14
CHEMBL1771095 1 7.09
CHEMBL1771088 1 6.88
CHEMBL1771070 1 6.88
CHEMBL1771078 1 6.85
CHEMBL1771073 1 6.78
CHEMBL1771089 1 6.69
CHEMBL1771084 1 6.62
CHEMBL1771071 1 6.47
CHEMBL1771076 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1771098 EC50 = 0.4 nM 9.40
CHEMBL1771104 EC50 = 0.8 nM 9.10
CHEMBL1771098 EC50 = 2.0 nM 8.70
CHEMBL1771082 EC50 = 2.0 nM 8.70
CHEMBL1771081 EC50 = 2.0 nM 8.70
CHEMBL1771103 EC50 = 2.0 nM 8.70
CHEMBL1771102 EC50 = 4.0 nM 8.40
CHEMBL1771100 EC50 = 4.0 nM 8.40
CHEMBL1771098 EC50 = 5.0 nM 8.30
CHEMBL1771101 EC50 = 6.0 nM 8.22
CHEMBL1770161 EC50 = 8.0 nM 8.10
CHEMBL1771092 EC50 = 8.0 nM 8.10
CHEMBL1771097 EC50 = 9.0 nM 8.05
CHEMBL1771094 EC50 = 10.0 nM 8.00
CHEMBL1771079 EC50 = 11.0 nM 7.96
CHEMBL1771093 EC50 = 11.0 nM 7.96
CHEMBL1771099 EC50 = 18.0 nM 7.75
CHEMBL1771097 EC50 = 23.0 nM 7.64
CHEMBL1771080 EC50 = 31.0 nM 7.51
CHEMBL1771068 EC50 = 36.0 nM 7.44
CHEMBL1771099 EC50 = 36.0 nM 7.44
CHEMBL1771091 EC50 = 41.0 nM 7.39
CHEMBL1771086 EC50 = 45.0 nM 7.35
CHEMBL1771096 EC50 = 64.0 nM 7.19
CHEMBL1771090 EC50 = 73.0 nM 7.14
CHEMBL1771095 EC50 = 82.0 nM 7.09
CHEMBL1771088 EC50 = 131.0 nM 6.88
CHEMBL1771070 EC50 = 132.0 nM 6.88
CHEMBL1771078 EC50 = 142.0 nM 6.85
CHEMBL1771073 EC50 = 165.0 nM 6.78
CHEMBL1771089 EC50 = 206.0 nM 6.69
CHEMBL1771084 EC50 = 239.0 nM 6.62
CHEMBL1771071 EC50 = 341.0 nM 6.47
CHEMBL1771076 EC50 = 379.0 nM 6.42
CHEMBL1771072 EC50 = 513.0 nM 6.29
CHEMBL1771077 EC50 = 523.0 nM 6.28
CHEMBL1771083 EC50 = 682.0 nM 6.17
CHEMBL1771085 EC50 = 887.0 nM 6.05
CHEMBL1771067 EC50 = 1900.0 nM 5.72
CHEMBL1771075 EC50 = 2500.0 nM 5.60