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Assay Detail

CHEMBL5042907

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Functional
Antagonist activity at CCR5 (unknown origin) expressed in HOS cells co-expressing Gqi-5 assessed as inhibition CCL5-stimulated Ca2+ mobilization by calcium mobilization assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HOS
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
IC50 5 7.03 9.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL584744 1 9.11
CHEMBL5074744 1 7.24
CHEMBL5071060 1 6.90
CHEMBL5089300 1 6.01
CHEMBL5074037 1 5.90

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL584744 IC50 = 0.77 nM 9.11
CHEMBL5074744 IC50 = 57.5 nM 7.24
CHEMBL5071060 IC50 = 126.0 nM 6.90
CHEMBL5089300 IC50 = 965.0 nM 6.01
CHEMBL5074037 IC50 = 1260.0 nM 5.90