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Assay Detail

CHEMBL1108000

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

Binding
Inhibition of anti-CXCR4 12G5 monoclonal antibody to CXCR4 in human SUP-T1 cells pretreated for 30 mins by flow cytometry
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type SUP-T1
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

Discovery of novel small molecule orally bioavailable C-X-C chemokine receptor 4 antagonists that are potent inhibitors of T-tropic (X4) HIV-1 replication.
Skerlj RT, Bridger GJ, Kaller A, McEachern EJ, Crawford JB, Zhou Y, Atsma B, Langille J, Nan S, Veale D, Wilson T, Harwig C, Hatse S, Princen K, De Clercq E, Schols D.
J Med Chem (2010) 53 : 3376 -3388
PubMed 20297846 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 6.02 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1093137 1 6.92
CHEMBL1089434 1 6.60
CHEMBL1090509 1 4.54

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1093137 IC50 = 120.0 nM 6.92
CHEMBL1089434 IC50 = 250.0 nM 6.60
CHEMBL1090509 IC50 = 29200.0 nM 4.54