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Assay Detail

CHEMBL1034062

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
35
Total Activities
35
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 1.
Barber CG, Blakemore DC, Chiva JY, Eastwood RL, Middleton DS, Paradowski KA.
Bioorg Med Chem Lett (2009) 19 : 1075 -1079
PubMed 19171484 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 35 8.00 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL460845 1 10.30
CHEMBL457043 1 10.15
CHEMBL461687 1 9.80
CHEMBL256907 MARAVIROC 4.0 1 9.70
CHEMBL459384 1 9.47
CHEMBL456226 1 9.32
CHEMBL461690 1 9.03
CHEMBL457044 1 8.81
CHEMBL469724 1 8.70
CHEMBL457960 1 8.63
CHEMBL461689 1 8.50
CHEMBL459567 1 8.47
CHEMBL518640 1 8.44
CHEMBL458157 1 8.43
CHEMBL460628 1 8.32
CHEMBL518794 1 8.30
CHEMBL459571 1 8.12
CHEMBL514410 1 7.87
CHEMBL456019 1 7.85
CHEMBL456224 1 7.75
CHEMBL459599 1 7.67
CHEMBL460629 1 7.60
CHEMBL459378 1 7.47
CHEMBL469542 1 7.43
CHEMBL460630 1 7.32
CHEMBL518326 1 7.19
CHEMBL460008 1 7.13
CHEMBL459600 1 7.02
CHEMBL460217 1 6.42
CHEMBL459598 1 6.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL460845 IC50 = 0.05 nM 10.30
CHEMBL457043 IC50 = 0.07 nM 10.15
CHEMBL461687 IC50 = 0.16 nM 9.80
CHEMBL256907 MARAVIROC IC50 = 0.2 nM 9.70
CHEMBL459384 IC50 = 0.34 nM 9.47
CHEMBL456226 IC50 = 0.48 nM 9.32
CHEMBL461690 IC50 = 0.94 nM 9.03
CHEMBL457044 IC50 = 1.54 nM 8.81
CHEMBL469724 IC50 = 2.0 nM 8.70
CHEMBL457960 IC50 = 2.33 nM 8.63
CHEMBL461689 IC50 = 3.16 nM 8.50
CHEMBL459567 IC50 = 3.4 nM 8.47
CHEMBL518640 IC50 = 3.63 nM 8.44
CHEMBL458157 IC50 = 3.76 nM 8.43
CHEMBL460628 IC50 = 4.83 nM 8.32
CHEMBL518794 IC50 = 5.0 nM 8.30
CHEMBL459571 IC50 = 7.5 nM 8.12
CHEMBL514410 IC50 = 13.4 nM 7.87
CHEMBL456019 IC50 = 14.0 nM 7.85
CHEMBL456224 IC50 = 17.9 nM 7.75
CHEMBL459599 IC50 = 21.4 nM 7.67
CHEMBL460629 IC50 = 25.3 nM 7.60
CHEMBL459378 IC50 = 33.7 nM 7.47
CHEMBL469542 IC50 = 37.5 nM 7.43
CHEMBL460630 IC50 = 48.0 nM 7.32
CHEMBL518326 IC50 = 64.4 nM 7.19
CHEMBL460008 IC50 = 73.5 nM 7.13
CHEMBL459600 IC50 = 94.6 nM 7.02
CHEMBL460217 IC50 = 382.0 nM 6.42
CHEMBL459598 IC50 = 540.0 nM 6.27
CHEMBL516939 IC50 = 1849.0 nM 5.73
CHEMBL460009 IC50 = 2310.0 nM 5.64
CHEMBL461688 IC50 = 6430.0 nM 5.19
CHEMBL515193 IC50 = 0.003 nM -
CHEMBL456425 IC50 > 25000.0 nM -