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Assay Detail

CHEMBL665164

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

Binding
Ability to displace [125I]- labeled MIP-1alpha from CCR5 receptor expressed on CHO cell membrane
ChEMBL ↗
25
Total Activities
24
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: modifications of the arylpropylpiperidine side chains.
Lynch CL, Willoughby CA, Hale JJ, Holson EJ, Budhu RJ, Gentry AL, Rosauer KG, Caldwell CG, Chen P, Mills SG, MacCoss M, Berk S, Chen L, Chapman KT, 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 : 119 -123
PubMed 12467630 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 25 9.01 10.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL21106 — — 1 10.22
CHEMBL20896 — — 1 10.00
CHEMBL20345 — — 1 10.00
CHEMBL21147 — — 1 9.70
CHEMBL20622 — — 1 9.70
CHEMBL20988 — — 1 9.52
CHEMBL282921 — — 1 9.52
CHEMBL21117 — — 1 9.52
CHEMBL278117 — — 2 9.40
CHEMBL20453 — — 1 9.40
CHEMBL278085 — — 1 9.30
CHEMBL20831 — — 1 9.30
CHEMBL281176 — — 1 9.10
CHEMBL281607 — — 1 9.10
CHEMBL20602 — — 1 9.05
CHEMBL280344 — — 1 8.96
CHEMBL283788 — — 1 8.82
CHEMBL21167 — — 1 8.80
CHEMBL20598 — — 1 8.80
CHEMBL278383 — — 1 8.43
CHEMBL417825 — — 1 8.32
CHEMBL20818 — — 1 7.72
CHEMBL284010 — — 1 7.29
CHEMBL21058 — — 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL21106 — IC50 = 0.06 nM 10.22
CHEMBL20896 — IC50 = 0.1 nM 10.00
CHEMBL20345 — IC50 = 0.1 nM 10.00
CHEMBL21147 — IC50 = 0.2 nM 9.70
CHEMBL20622 — IC50 = 0.2 nM 9.70
CHEMBL20988 — IC50 = 0.3 nM 9.52
CHEMBL21117 — IC50 = 0.3 nM 9.52
CHEMBL282921 — IC50 = 0.3 nM 9.52
CHEMBL20453 — IC50 = 0.4 nM 9.40
CHEMBL278117 — IC50 = 0.4 nM 9.40
CHEMBL278085 — IC50 = 0.5 nM 9.30
CHEMBL20831 — IC50 = 0.5 nM 9.30
CHEMBL278117 — IC50 = 0.5 nM 9.30
CHEMBL281176 — IC50 = 0.8 nM 9.10
CHEMBL281607 — IC50 = 0.8 nM 9.10
CHEMBL20602 — IC50 = 0.9 nM 9.05
CHEMBL280344 — IC50 = 1.1 nM 8.96
CHEMBL283788 — IC50 = 1.5 nM 8.82
CHEMBL21167 — IC50 = 1.6 nM 8.80
CHEMBL20598 — IC50 = 1.6 nM 8.80
CHEMBL278383 — IC50 = 3.7 nM 8.43
CHEMBL417825 — IC50 = 4.8 nM 8.32
CHEMBL20818 — IC50 = 19.0 nM 7.72
CHEMBL284010 — IC50 = 51.0 nM 7.29
CHEMBL21058 — IC50 = 1000.0 nM 6.00