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Assay Detail

CHEMBL5361971

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

Functional
Antagonist activity at CCR5 (unknown origin) expressed in HEK293 cells co-expressing Galpha16 assessed as intracellular calcium change incubated for 60 mins by Fluo-4 AM calcium flux based FLIPR assay
6
Total Activities
6
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-C chemokine receptor type 5 (CHEMBL274)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Multitargeted drug design strategy for discovery of short-peptide-based HIV-1 entry inhibitors with high potency.
Wang C, Wang H, Wang X, Sun L, Wang Q, Li Q, Liang R, Dou D, Yu F, Lu L, Jiang S.
Eur J Med Chem (2023) 252 : 115294 -115294
PubMed 36944281 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 8.58 9.12

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5413158 1 9.12
CHEMBL207004 1 9.08
CHEMBL5438380 1 8.97
CHEMBL5410204 1 7.99
CHEMBL5414303 1 7.72
CHEMBL5415654 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5413158 IC50 = 0.75 nM 9.12
CHEMBL207004 IC50 = 0.83 nM 9.08
CHEMBL5438380 IC50 = 1.08 nM 8.97
CHEMBL5410204 IC50 = 10.27 nM 7.99
CHEMBL5414303 IC50 = 19.17 nM 7.72
CHEMBL5415654 IC50 > 10000.0 nM -