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Assay Detail

CHEMBL661336

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

Binding
Inhibition of RANTES binding to Chemokine receptor type 5 receptor from NIH 3T3 cells
58
Total Activities
57
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type NIH3T3
Confidence 8 — Homologous single protein target
Curated By Expert

Target

C-C chemokine receptor type 5 (CHEMBL3676)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Synthesis, SAR, and biological evaluation of oximino-piperidino-piperidine amides. 1. Orally bioavailable CCR5 receptor antagonists with potent anti-HIV activity.
Palani A, Shapiro S, Josien H, Bara T, Clader JW, Greenlee WJ, Cox K, Strizki JM, Baroudy BM.
J Med Chem (2002) 45 : 3143 -3160
PubMed 12086500 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 58 7.66 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105821 1 8.96
CHEMBL323172 1 8.96
CHEMBL324643 1 8.70
CHEMBL324671 2 8.70
CHEMBL78535 ANCRIVIROC 2.0 1 8.68
CHEMBL321413 1 8.52
CHEMBL105784 1 8.47
CHEMBL106533 1 8.42
CHEMBL109008 1 8.40
CHEMBL318311 1 8.36
CHEMBL109158 1 8.35
CHEMBL320502 1 8.28
CHEMBL419735 1 8.25
CHEMBL110757 1 8.15
CHEMBL106813 1 8.12
CHEMBL107154 1 8.10
CHEMBL418997 1 8.05
CHEMBL107363 1 7.92
CHEMBL317644 1 7.80
CHEMBL106767 1 7.75
CHEMBL106098 1 7.72
CHEMBL106558 1 7.70
CHEMBL106099 1 7.62
CHEMBL107092 1 7.60
CHEMBL112760 1 7.60
CHEMBL443999 1 7.58
CHEMBL108569 1 7.54
CHEMBL107999 1 7.52
CHEMBL432636 1 7.52
CHEMBL105779 1 7.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105821 Ki = 1.1 nM 8.96
CHEMBL323172 Ki = 1.1 nM 8.96
CHEMBL324671 Ki = 2.0 nM 8.70
CHEMBL324643 Ki = 2.0 nM 8.70
CHEMBL78535 ANCRIVIROC Ki = 2.1 nM 8.68
CHEMBL321413 Ki = 3.0 nM 8.52
CHEMBL105784 Ki = 3.4 nM 8.47
CHEMBL106533 Ki = 3.8 nM 8.42
CHEMBL109008 Ki = 4.0 nM 8.40
CHEMBL318311 Ki = 4.4 nM 8.36
CHEMBL109158 Ki = 4.5 nM 8.35
CHEMBL320502 Ki = 5.3 nM 8.28
CHEMBL419735 Ki = 5.6 nM 8.25
CHEMBL110757 Ki = 7.0 nM 8.15
CHEMBL106813 Ki = 7.6 nM 8.12
CHEMBL107154 Ki = 8.0 nM 8.10
CHEMBL418997 Ki = 9.0 nM 8.05
CHEMBL324671 Ki = 11.0 nM 7.96
CHEMBL107363 Ki = 12.0 nM 7.92
CHEMBL317644 Ki = 16.0 nM 7.80
CHEMBL106767 Ki = 18.0 nM 7.75
CHEMBL106098 Ki = 19.0 nM 7.72
CHEMBL106558 Ki = 20.0 nM 7.70
CHEMBL106099 Ki = 24.0 nM 7.62
CHEMBL112760 Ki = 25.0 nM 7.60
CHEMBL107092 Ki = 25.0 nM 7.60
CHEMBL443999 Ki = 26.0 nM 7.58
CHEMBL108569 Ki = 29.0 nM 7.54
CHEMBL107999 Ki = 30.0 nM 7.52
CHEMBL432636 Ki = 30.0 nM 7.52
CHEMBL105779 Ki = 33.0 nM 7.48
CHEMBL106790 Ki = 33.0 nM 7.48
CHEMBL106406 Ki = 33.0 nM 7.48
CHEMBL106982 Ki = 33.0 nM 7.48
CHEMBL110730 Ki = 43.0 nM 7.37
CHEMBL331140 Ki = 48.0 nM 7.32
CHEMBL106209 Ki = 54.0 nM 7.27
CHEMBL317476 Ki = 55.0 nM 7.26
CHEMBL106247 Ki = 58.0 nM 7.24
CHEMBL106507 Ki = 62.0 nM 7.21
CHEMBL110871 Ki = 62.0 nM 7.21
CHEMBL110809 Ki = 67.0 nM 7.17
CHEMBL106299 Ki = 68.0 nM 7.17
CHEMBL106468 Ki = 78.0 nM 7.11
CHEMBL110463 Ki = 86.0 nM 7.07
CHEMBL110786 Ki = 113.0 nM 6.95
CHEMBL106369 Ki = 155.0 nM 6.81
CHEMBL323454 Ki = 190.0 nM 6.72
CHEMBL110270 Ki = 282.0 nM 6.55
CHEMBL106264 Ki = 363.0 nM 6.44