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Assay Detail

CHEMBL1107772

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

Binding
Displacement of [128I]-RANTES from CCR5 receptor receptors expressed in CHO cells
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Evaluation of a 4-aminopiperidine replacement in several series of CCR5 antagonists.
Lemoine RC, Petersen AC, Setti L, Chen L, Wanner J, Jekle A, Heilek G, deRosier A, Ji C, Rotstein DM.
Bioorg Med Chem Lett (2010) 20 : 1830 -1833
PubMed 20176481 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 7.53 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1078231 1 8.40
CHEMBL1077358 1 7.85
CHEMBL1077359 1 7.82
CHEMBL1077364 1 7.64
CHEMBL1077360 1 7.60
CHEMBL1077365 1 7.57
CHEMBL1077363 1 7.47
CHEMBL1077362 1 7.36
CHEMBL1077355 1 7.35
CHEMBL1077361 1 7.21
CHEMBL1077353 1 7.04
CHEMBL1077354 1 7.01
CHEMBL1077350 1 -
CHEMBL1077351 1 -
CHEMBL1077352 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1078231 IC50 = 4.0 nM 8.40
CHEMBL1077358 IC50 = 14.0 nM 7.85
CHEMBL1077359 IC50 = 15.0 nM 7.82
CHEMBL1077364 IC50 = 23.0 nM 7.64
CHEMBL1077360 IC50 = 25.0 nM 7.60
CHEMBL1077365 IC50 = 27.0 nM 7.57
CHEMBL1077363 IC50 = 34.0 nM 7.47
CHEMBL1077362 IC50 = 44.0 nM 7.36
CHEMBL1077355 IC50 = 45.0 nM 7.35
CHEMBL1077361 IC50 = 61.0 nM 7.21
CHEMBL1077353 IC50 = 92.0 nM 7.04
CHEMBL1077354 IC50 = 98.0 nM 7.01
CHEMBL1077350 IC50 > 500.0 nM -
CHEMBL1077351 IC50 > 500.0 nM -
CHEMBL1077352 IC50 > 500.0 nM -