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Assay Detail

CHEMBL5042909

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

Binding
Inhibition of CCR5-mediated HIV-1 Bal entry in human GHOST CCR5 cells assessed as decrease in viral reverse transcriptase activity by measuring [3H]thymidine triphosphate incorporation measured after 60 to 90 mins by scintillation counting analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type GHOST CCR5
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

C-C chemokine receptor type 5 (CHEMBL274)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design and Development of Chemical Probes Targeting Putative MOR-CCR5 Heterodimers to Inhibit Opioid Exacerbated HIV-1 Infectivity.
Huang B, Wang H, Zheng Y, Li M, Kang G, Barreto-de-Souza V, Nassehi N, Knapp PE, Selley DE, Hauser KF, Zhang Y.
J Med Chem (2021) 64 : 7702 -7723
PubMed 34027668 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 7.39 7.75

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL584744 1 7.75
CHEMBL5074744 1 7.03
CHEMBL5071060 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL584744 EC50 = 18.0 nM 7.75
CHEMBL5074744 EC50 = 93.0 nM 7.03
CHEMBL5071060 EC50 > 100000.0 nM -