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Assay Detail

CHEMBL654655

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

Binding
Ability to displace [125I]-labeled MIP-1alpha from the C-C chemokine receptor type 5 expressed on CHO cell membranes
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

CCR5 antagonists: bicyclic isoxazolidines as conformationally constrained N-1-substituted pyrrolidines.
Lynch CL, Gentry AL, Hale JJ, Mills SG, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Doss G, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.
Bioorg Med Chem Lett (2002) 12 : 677 -679
PubMed 11844699 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.99 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL157491 1 9.89
CHEMBL328260 1 9.10
CHEMBL435259 1 8.60
CHEMBL423427 1 8.30
CHEMBL161093 1 8.30
CHEMBL158754 1 8.22
CHEMBL159018 1 8.10
CHEMBL350763 1 7.96
CHEMBL157983 1 7.85
CHEMBL159097 1 7.57
CHEMBL161594 1 7.52
CHEMBL539943 1 7.48
CHEMBL350027 1 7.37
CHEMBL158438 1 7.34
CHEMBL436245 1 7.16
CHEMBL161480 1 7.07
CHEMBL351973 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL157491 IC50 = 0.13 nM 9.89
CHEMBL328260 IC50 = 0.8 nM 9.10
CHEMBL435259 IC50 = 2.5 nM 8.60
CHEMBL423427 IC50 = 5.0 nM 8.30
CHEMBL161093 IC50 = 5.0 nM 8.30
CHEMBL158754 IC50 = 6.0 nM 8.22
CHEMBL159018 IC50 = 8.0 nM 8.10
CHEMBL350763 IC50 = 11.0 nM 7.96
CHEMBL157983 IC50 = 14.0 nM 7.85
CHEMBL159097 IC50 = 27.0 nM 7.57
CHEMBL161594 IC50 = 30.0 nM 7.52
CHEMBL539943 IC50 = 33.0 nM 7.48
CHEMBL350027 IC50 = 43.0 nM 7.37
CHEMBL158438 IC50 = 46.0 nM 7.34
CHEMBL436245 IC50 = 69.0 nM 7.16
CHEMBL161480 IC50 = 86.0 nM 7.07
CHEMBL351973 IC50 ~ 27.0 nM -