Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL649944

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

Binding
Inhibition of RANTES binding to C-C chemokine receptor type 5
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Discovery of 4-[(Z)-(4-bromophenyl)- (ethoxyimino)methyl]-1'-[(2,4-dimethyl-3- pyridinyl)carbonyl]-4'-methyl-1,4'- bipiperidine N-oxide (SCH 351125): an orally bioavailable human CCR5 antagonist for the treatment of HIV infection.
Palani A, Shapiro S, Clader JW, Greenlee WJ, Cox K, Strizki J, Endres M, Baroudy BM.
J Med Chem (2001) 44 : 3339 -3342
PubMed 11585437 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 8.14 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL109051 1 9.00
CHEMBL323172 1 8.96
CHEMBL105821 1 8.96
CHEMBL324643 1 8.74
CHEMBL112686 1 8.70
CHEMBL78535 ANCRIVIROC 2.0 1 8.68
CHEMBL105784 1 8.47
CHEMBL109158 1 8.35
CHEMBL292625 1 8.15
CHEMBL2111747 1 7.96
CHEMBL106098 1 7.75
CHEMBL106767 1 7.75
CHEMBL112760 1 7.60
CHEMBL108569 1 7.54
CHEMBL331140 1 7.32
CHEMBL106209 1 7.27
CHEMBL106247 1 7.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL109051 Ki = 1.0 nM 9.00
CHEMBL323172 Ki = 1.1 nM 8.96
CHEMBL105821 Ki = 1.1 nM 8.96
CHEMBL324643 Ki = 1.8 nM 8.74
CHEMBL112686 Ki = 2.0 nM 8.70
CHEMBL78535 ANCRIVIROC Ki = 2.1 nM 8.68
CHEMBL105784 Ki = 3.4 nM 8.47
CHEMBL109158 Ki = 4.5 nM 8.35
CHEMBL292625 Ki = 7.0 nM 8.15
CHEMBL2111747 Ki = 11.0 nM 7.96
CHEMBL106098 Ki = 18.0 nM 7.75
CHEMBL106767 Ki = 18.0 nM 7.75
CHEMBL112760 Ki = 25.0 nM 7.60
CHEMBL108569 Ki = 29.0 nM 7.54
CHEMBL331140 Ki = 48.0 nM 7.32
CHEMBL106209 Ki = 54.0 nM 7.27
CHEMBL106247 Ki = 66.0 nM 7.18