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Assay Detail

CHEMBL3879920

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

Functional
Agonist activity at recombinant human GPR17 short isoform transfected in human 1321N1 cells assessed as mobilization of intracellular Ca2+ after 20 mins by oregon green 488 BAPTA-1/AM dye-based fluorescence assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type 1321-N1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Uracil nucleotide/cysteinyl leukotriene receptor (CHEMBL1075162)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

GPR 17 agonists and screening assay
(2013)

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.65 6.71

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3132880 1 6.71
CHEMBL3132887 1 6.15
CHEMBL3968577 1 6.14
CHEMBL31344 1 6.09
CHEMBL3915176 1 5.52
CHEMBL3132885 1 5.50
CHEMBL295718 1 5.43
CHEMBL3132881 1 5.32
CHEMBL3921330 1 5.28
CHEMBL53914 1 5.13
CHEMBL3897541 1 4.86

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3132880 EC50 = 194.98 nM 6.71
CHEMBL3132887 EC50 = 707.95 nM 6.15
CHEMBL3968577 EC50 = 724.44 nM 6.14
CHEMBL31344 EC50 = 812.83 nM 6.09
CHEMBL3915176 EC50 = 3019.95 nM 5.52
CHEMBL3132885 EC50 = 3162.28 nM 5.50
CHEMBL295718 EC50 = 3715.35 nM 5.43
CHEMBL3132881 EC50 = 4786.3 nM 5.32
CHEMBL3921330 EC50 = 5248.07 nM 5.28
CHEMBL53914 EC50 = 7413.1 nM 5.13
CHEMBL3897541 EC50 = 13803.84 nM 4.86