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Assay Detail

CHEMBL1107397

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

Functional
Agonist activity at human GPR17 expressed in human 1321N1 cells assessed as induction of [35S]GTPgammaS binding after 30 mins by rapid filtration assay
6
Total Activities
6
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

Frontal affinity chromatography-mass spectrometry useful for characterization of new ligands for GPR17 receptor.
Calleri E, Ceruti S, Cristalli G, Martini C, Temporini C, Parravicini C, Volpini R, Daniele S, Caccialanza G, Lecca D, Lambertucci C, Trincavelli ML, Marucci G, Wainer IW, Ranghino G, Fantucci P, Abbracchio MP, Massolini G.
J Med Chem (2010) 53 : 3489 -3501
PubMed 20394377 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 6 8.00 10.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1097652 1 10.44
CHEMBL1096742 1 8.85
CHEMBL1098419 1 8.77
CHEMBL1098083 1 7.96
CHEMBL1094759 1 6.03
CHEMBL1096401 UDP TRISODIUM 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1097652 EC50 = 0.036 nM 10.44
CHEMBL1096742 EC50 = 1.4 nM 8.85
CHEMBL1098419 EC50 = 1.7 nM 8.77
CHEMBL1098083 EC50 = 11.0 nM 7.96
CHEMBL1094759 EC50 = 945.0 nM 6.03
CHEMBL1096401 UDP TRISODIUM EC50 = 1140.0 nM 5.94