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Assay Detail

CHEMBL1245770

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

Functional
Antagonist activity at human CXCR4 expressed in HEK293 cells assessed as inhibition of SDF1-induced response treated 30 mins before agonist challenge by FLIPR assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Blockade of X4-tropic HIV-1 cellular entry by GSK812397, a potent noncompetitive CXCR4 receptor antagonist.
Jenkinson S, Thomson M, McCoy D, Edelstein M, Danehower S, Lawrence W, Wheelan P, Spaltenstein A, Gudmundsson K.
Antimicrob Agents Chemother (2010) 54 : 817 -824
PubMed 19949058 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.06 9.06

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1242210 1 9.06

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1242210 IC50 = 0.87 nM 9.06