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Assay Detail

CHEMBL5608637

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

Functional
Antagonist activity at CXCR4 (unknown origin) expressed in human HEK293T cells assessed as intracellular calcium flux by FLIPR assay
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HEK293T
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 and therapeutic perspectives of CXCR4 antagonists for disease therapy.
Yang J, Tian E, Chen L, Liu Z, Ren Y, Mao W, Zhang Y, Zhang J.
Eur J Med Chem (2024) 275 : 116594 -116594
PubMed 38879970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 17 8.65 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5612607 1 9.92
CHEMBL5612623 1 9.72
CHEMBL5611972 1 9.72
CHEMBL5613902 1 9.62
CHEMBL4074140 1 9.00
CHEMBL5614258 1 9.00
CHEMBL5613857 1 9.00
CHEMBL5613412 1 8.89
CHEMBL4168957 1 8.68
CHEMBL4162609 1 8.44
CHEMBL1381819 1 8.42
CHEMBL4172669 1 8.22
CHEMBL4778921 1 8.06
CHEMBL4075191 1 8.00
CHEMBL5613701 1 7.62
CHEMBL5612347 1 7.47
CHEMBL4299893 1 7.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5612607 EC50 = 0.12 nM 9.92
CHEMBL5612623 EC50 = 0.19 nM 9.72
CHEMBL5611972 EC50 = 0.19 nM 9.72
CHEMBL5613902 EC50 = 0.24 nM 9.62
CHEMBL4074140 EC50 = 1.0 nM 9.00
CHEMBL5614258 EC50 = 1.0 nM 9.00
CHEMBL5613857 EC50 = 1.0 nM 9.00
CHEMBL5613412 EC50 = 1.3 nM 8.89
CHEMBL4168957 EC50 = 2.1 nM 8.68
CHEMBL4162609 EC50 = 3.6 nM 8.44
CHEMBL1381819 EC50 = 3.8 nM 8.42
CHEMBL4172669 EC50 = 6.0 nM 8.22
CHEMBL4778921 EC50 = 8.8 nM 8.06
CHEMBL4075191 EC50 = 10.0 nM 8.00
CHEMBL5613701 EC50 = 24.0 nM 7.62
CHEMBL5612347 EC50 = 34.0 nM 7.47
CHEMBL4299893 EC50 = 54.0 nM 7.27