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Assay Detail

CHEMBL3583508

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

Binding
Agonist activity at CXCR7 D275N mutant (unknown origin) expressed in HEK293E cells co-transfected with receptor-eYFP construct and beta-arrestin2-Rluc assessed as induction of receptor-mediated beta-arrestin recruitment by BRET assay
4
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293E
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Atypical chemokine receptor 3 (CHEMBL2010631)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Development of novel CXC chemokine receptor 7 (CXCR7) ligands: selectivity switch from CXCR4 antagonists with a cyclic pentapeptide scaffold.
Oishi S, Kuroyanagi T, Kubo T, Montpas N, Yoshikawa Y, Misu R, Kobayashi Y, Ohno H, Heveker N, Furuya T, Fujii N.
J Med Chem (2015) 58 : 5218 -5225
PubMed 26042340 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 6.00 6.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3581276 2 6.20
CHEMBL3581264 2 5.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3581276 EC50 = 630.96 nM 6.20
CHEMBL3581276 EC50 = 650.0 nM 6.19
CHEMBL3581264 EC50 = 1500.0 nM 5.82
CHEMBL3581264 EC50 = 1584.89 nM 5.80