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Assay Detail

CHEMBL3583503

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

Binding
Inhibition of [125I]SDF-1alpha binding to CXCR4 (unknown origin) expressed in HEK293 cell membranes incubated for 1 hr by radioligand displacement assay
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-X-C chemokine receptor type 4 (CHEMBL2107)
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
IC50 26 5.36 5.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436283 1 5.92
CHEMBL3581262 1 5.66
CHEMBL3581269 1 5.34
CHEMBL3581263 1 5.22
CHEMBL3581261 1 4.64
CHEMBL3581264 1 -
CHEMBL3581265 1 -
CHEMBL3581266 1 -
CHEMBL3581267 1 -
CHEMBL3581268 1 -
CHEMBL3581270 1 -
CHEMBL3581271 1 -
CHEMBL3581272 1 -
CHEMBL3581273 1 -
CHEMBL3581274 1 -
CHEMBL3581275 1 -
CHEMBL3581276 1 -
CHEMBL3581277 1 -
CHEMBL3581278 1 -
CHEMBL3581279 1 -
CHEMBL3581280 1 -
CHEMBL3581281 1 -
CHEMBL3581282 1 -
CHEMBL3581283 1 -
CHEMBL3581284 1 -
CHEMBL3581285 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436283 IC50 = 1200.0 nM 5.92
CHEMBL3581262 IC50 = 2200.0 nM 5.66
CHEMBL3581269 IC50 = 4600.0 nM 5.34
CHEMBL3581263 IC50 = 6000.0 nM 5.22
CHEMBL3581261 IC50 = 23000.0 nM 4.64
CHEMBL3581264 IC50 > 30000.0 nM -
CHEMBL3581265 IC50 > 30000.0 nM -
CHEMBL3581266 IC50 > 30000.0 nM -
CHEMBL3581267 IC50 > 30000.0 nM -
CHEMBL3581268 IC50 > 30000.0 nM -
CHEMBL3581270 IC50 > 30000.0 nM -
CHEMBL3581271 IC50 > 30000.0 nM -
CHEMBL3581272 IC50 > 30000.0 nM -
CHEMBL3581273 IC50 > 30000.0 nM -
CHEMBL3581274 IC50 > 30000.0 nM -
CHEMBL3581275 IC50 > 30000.0 nM -
CHEMBL3581276 IC50 > 30000.0 nM -
CHEMBL3581277 IC50 > 30000.0 nM -
CHEMBL3581278 IC50 > 30000.0 nM -
CHEMBL3581279 IC50 > 30000.0 nM -
CHEMBL3581280 IC50 > 30000.0 nM -
CHEMBL3581281 IC50 > 30000.0 nM -
CHEMBL3581282 IC50 > 30000.0 nM -
CHEMBL3581283 IC50 > 30000.0 nM -
CHEMBL3581284 IC50 > 30000.0 nM -
CHEMBL3581285 IC50 > 30000.0 nM -