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Assay Detail

CHEMBL1107398

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

Functional
Antagonist activity at human GPR17 expressed in human 1321N1 cells assessed as inhibition of UDP-glucose-induced [35S]GTPgammaS binding after 30 mins by rapid filtration assay
4
Total Activities
4
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
IC50 4 7.16 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1097279 CANGRELOR TETRASODIUM 4.0 1 9.15
CHEMBL1094109 1 6.95
CHEMBL1096400 1 6.29
CHEMBL1094760 1 6.24

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1097279 CANGRELOR TETRASODIUM IC50 = 0.7 nM 9.15
CHEMBL1094109 IC50 = 112.0 nM 6.95
CHEMBL1096400 IC50 = 508.0 nM 6.29
CHEMBL1094760 IC50 = 582.0 nM 6.24