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Assay Detail

CHEMBL1019461

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

Binding
Antagonist activity at human recombinant CCR5 expressed in human HeLa-P4 cells assessed as inhibition of human HeLa-P4 cells binding to HIV1 gp160 expressing CHO cells by cell-cell fusion assay
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

1-Amido-1-phenyl-3-piperidinylbutanes--CCR5 antagonists for the treatment of HIV: part 2.
Barber CG, Blakemore DC, Chiva JY, Eastwood RL, Middleton DS, Paradowski KA.
Bioorg Med Chem Lett (2009) 19 : 1499 -1503
PubMed 19185490 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 23 8.11 9.86

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL473558 1 9.86
CHEMBL256907 MARAVIROC 4.0 1 9.70
CHEMBL489513 1 9.42
CHEMBL491319 1 9.32
CHEMBL473759 1 9.29
CHEMBL522259 1 9.08
CHEMBL491679 1 8.89
CHEMBL3085107 1 8.85
CHEMBL474154 1 8.51
CHEMBL515261 1 8.50
CHEMBL472953 1 8.41
CHEMBL523267 1 8.31
CHEMBL491153 1 8.21
CHEMBL491154 1 7.54
CHEMBL491320 1 7.30
CHEMBL473353 1 7.28
CHEMBL489324 1 7.21
CHEMBL473352 1 7.07
CHEMBL473348 1 7.05
CHEMBL514000 1 6.79
CHEMBL489323 1 6.75
CHEMBL489512 1 6.73
CHEMBL491328 1 6.50

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL473558 IC50 = 0.137 nM 9.86
CHEMBL256907 MARAVIROC IC50 = 0.2 nM 9.70
CHEMBL489513 IC50 = 0.38 nM 9.42
CHEMBL491319 IC50 = 0.48 nM 9.32
CHEMBL473759 IC50 = 0.513 nM 9.29
CHEMBL522259 IC50 = 0.84 nM 9.08
CHEMBL491679 IC50 = 1.3 nM 8.89
CHEMBL3085107 IC50 = 1.4 nM 8.85
CHEMBL474154 IC50 = 3.11 nM 8.51
CHEMBL515261 IC50 = 3.16 nM 8.50
CHEMBL472953 IC50 = 3.93 nM 8.41
CHEMBL523267 IC50 = 4.87 nM 8.31
CHEMBL491153 IC50 = 6.12 nM 8.21
CHEMBL491154 IC50 = 28.7 nM 7.54
CHEMBL491320 IC50 = 49.9 nM 7.30
CHEMBL473353 IC50 = 52.8 nM 7.28
CHEMBL489324 IC50 = 62.0 nM 7.21
CHEMBL473352 IC50 = 85.3 nM 7.07
CHEMBL473348 IC50 = 89.2 nM 7.05
CHEMBL514000 IC50 = 164.0 nM 6.79
CHEMBL489323 IC50 = 176.0 nM 6.75
CHEMBL489512 IC50 = 187.0 nM 6.73
CHEMBL491328 IC50 = 315.0 nM 6.50