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Assay Detail

CHEMBL815091

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

Functional
Concentration required to inhibit the entry of HIV-1 reporter virus (ADA) into U-87 cells by 50%
39
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type U-87MG ATCC
Confidence 1 — Organism
Curated By Expert

Target

U-87 MG (CHEMBL614247)
Type CELL-LINE
Organism Homo sapiens

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
IC50 39 8.43 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL105821 1 9.70
CHEMBL323172 1 9.30
CHEMBL109158 1 9.30
CHEMBL78535 ANCRIVIROC 2.0 1 9.22
CHEMBL105784 1 9.22
CHEMBL110757 1 9.05
CHEMBL107092 1 9.00
CHEMBL107154 1 9.00
CHEMBL320502 1 8.96
CHEMBL324643 1 8.96
CHEMBL324671 2 8.92
CHEMBL106533 1 8.89
CHEMBL443999 1 8.85
CHEMBL419735 1 8.85
CHEMBL317644 1 8.77
CHEMBL109008 1 8.77
CHEMBL318311 1 8.74
CHEMBL321413 1 8.68
CHEMBL112760 1 8.55
CHEMBL106767 1 8.40
CHEMBL106790 1 8.36
CHEMBL317476 1 8.30
CHEMBL106813 1 8.29
CHEMBL106098 1 8.25
CHEMBL418997 1 8.24
CHEMBL110730 1 8.19
CHEMBL106982 1 8.15
CHEMBL106406 1 8.05
CHEMBL331140 1 8.04
CHEMBL106468 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL105821 IC50 = 0.2 nM 9.70
CHEMBL323172 IC50 = 0.5 nM 9.30
CHEMBL109158 IC50 = 0.5 nM 9.30
CHEMBL105784 IC50 = 0.6 nM 9.22
CHEMBL78535 ANCRIVIROC IC50 = 0.6 nM 9.22
CHEMBL110757 IC50 = 0.9 nM 9.05
CHEMBL107092 IC50 = 1.0 nM 9.00
CHEMBL107154 IC50 = 1.0 nM 9.00
CHEMBL324643 IC50 = 1.1 nM 8.96
CHEMBL320502 IC50 = 1.1 nM 8.96
CHEMBL324671 IC50 = 1.2 nM 8.92
CHEMBL106533 IC50 = 1.3 nM 8.89
CHEMBL419735 IC50 = 1.4 nM 8.85
CHEMBL324671 IC50 = 1.4 nM 8.85
CHEMBL443999 IC50 = 1.4 nM 8.85
CHEMBL109008 IC50 = 1.7 nM 8.77
CHEMBL317644 IC50 = 1.7 nM 8.77
CHEMBL318311 IC50 = 1.8 nM 8.74
CHEMBL321413 IC50 = 2.1 nM 8.68
CHEMBL112760 IC50 = 2.8 nM 8.55
CHEMBL106767 IC50 = 4.0 nM 8.40
CHEMBL106790 IC50 = 4.4 nM 8.36
CHEMBL317476 IC50 = 5.0 nM 8.30
CHEMBL106813 IC50 = 5.1 nM 8.29
CHEMBL106098 IC50 = 5.6 nM 8.25
CHEMBL418997 IC50 = 5.7 nM 8.24
CHEMBL110730 IC50 = 6.4 nM 8.19
CHEMBL106982 IC50 = 7.0 nM 8.15
CHEMBL106406 IC50 = 9.0 nM 8.05
CHEMBL331140 IC50 = 9.2 nM 8.04
CHEMBL106468 IC50 = 10.0 nM 8.00
CHEMBL106247 IC50 = 10.0 nM 8.00
CHEMBL106209 IC50 = 12.0 nM 7.92
CHEMBL106299 IC50 = 23.0 nM 7.64
CHEMBL106369 IC50 = 26.0 nM 7.58
CHEMBL110786 IC50 = 38.0 nM 7.42
CHEMBL110809 IC50 = 41.0 nM 7.39
CHEMBL323454 IC50 = 76.0 nM 7.12
CHEMBL110185 IC50 = 1300.0 nM 5.89