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Assay Detail

CHEMBL654654

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

Binding
Displacement inhibition of 125-I labeled MIP-alpha from CCR5 receptor expressed on CHO cell membranes
25
Total Activities
25
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

1,3,4 Trisubstituted pyrrolidine CCR5 receptor antagonists bearing 4-aminoheterocycle substituted piperidine side chains.
Willoughby CA, Rosauer KG, Hale JJ, Budhu RJ, Mills SG, Chapman KT, MacCoss M, Malkowitz L, Springer MS, Gould SL, DeMartino JA, Siciliano SJ, Cascieri MA, Carella A, Carver G, Holmes K, Schleif WA, Danzeisen R, Hazuda D, Kessler J, Lineberger J, Miller M, Emini EA.
Bioorg Med Chem Lett (2003) 13 : 427 -431
PubMed 12565944 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 8.38 9.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL344261 1 9.40
CHEMBL344641 1 9.30
CHEMBL328297 1 9.10
CHEMBL275998 1 9.10
CHEMBL137327 1 8.96
CHEMBL342842 1 8.92
CHEMBL343745 1 8.92
CHEMBL343366 1 8.82
CHEMBL138437 1 8.80
CHEMBL335562 1 8.77
CHEMBL428104 1 8.74
CHEMBL343160 1 8.41
CHEMBL137728 1 8.30
CHEMBL137419 1 8.22
CHEMBL137038 1 8.18
CHEMBL137524 1 8.05
CHEMBL136977 1 8.05
CHEMBL138645 1 8.00
CHEMBL135432 1 7.92
CHEMBL137072 1 7.92
CHEMBL138282 1 7.85
CHEMBL137272 1 7.68
CHEMBL137206 1 7.64
CHEMBL137154 1 7.38
CHEMBL137650 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL344261 IC50 = 0.4 nM 9.40
CHEMBL344641 IC50 = 0.5 nM 9.30
CHEMBL328297 IC50 = 0.8 nM 9.10
CHEMBL275998 IC50 = 0.8 nM 9.10
CHEMBL137327 IC50 = 1.1 nM 8.96
CHEMBL342842 IC50 = 1.2 nM 8.92
CHEMBL343745 IC50 = 1.2 nM 8.92
CHEMBL343366 IC50 = 1.5 nM 8.82
CHEMBL138437 IC50 = 1.6 nM 8.80
CHEMBL335562 IC50 = 1.7 nM 8.77
CHEMBL428104 IC50 = 1.8 nM 8.74
CHEMBL343160 IC50 = 3.9 nM 8.41
CHEMBL137728 IC50 = 5.0 nM 8.30
CHEMBL137419 IC50 = 6.0 nM 8.22
CHEMBL137038 IC50 = 6.6 nM 8.18
CHEMBL137524 IC50 = 9.0 nM 8.05
CHEMBL136977 IC50 = 9.0 nM 8.05
CHEMBL138645 IC50 = 10.0 nM 8.00
CHEMBL135432 IC50 = 12.0 nM 7.92
CHEMBL137072 IC50 = 12.0 nM 7.92
CHEMBL138282 IC50 = 14.0 nM 7.85
CHEMBL137272 IC50 = 21.0 nM 7.68
CHEMBL137206 IC50 = 23.0 nM 7.64
CHEMBL137154 IC50 = 42.0 nM 7.38
CHEMBL137650 IC50 = 66.0 nM 7.18