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Assay Detail

CHEMBL2168515

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

Functional
Antiviral activity against R5 tropic HIV1 Ba-L infected human PBMC assessed as inhibition of viral replication by p-24 antigen specific ELISA
18
Total Activities
18
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Confidence 1 — Organism
Curated By Autocuration

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Mitigating hERG Inhibition: Design of Orally Bioavailable CCR5 Antagonists as Potent Inhibitors of R5 HIV-1 Replication.
Skerlj R, Bridger G, Zhou Y, Bourque E, McEachern E, Danthi S, Langille J, Harwig C, Veale D, Carpenter B, Ba T, Bey M, Baird I, Wilson T, Metz M, MacFarland R, Mosi R, Bodart V, Wong R, Fricker S, Huskens D, Schols D.
ACS Med Chem Lett (2012) 3 : 216 -221
PubMed 24900457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.68 8.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164202 1 8.80
CHEMBL2164207 1 8.72
CHEMBL2164210 1 8.54
CHEMBL2164208 1 8.32
CHEMBL2164212 1 8.16
CHEMBL2164209 1 8.14
CHEMBL2164206 1 7.83
CHEMBL2164203 1 7.81
CHEMBL2164201 1 7.79
CHEMBL2164220 1 7.77
CHEMBL2164211 1 7.67
CHEMBL2164215 1 7.65
CHEMBL2164217 1 7.46
CHEMBL2164219 1 7.42
CHEMBL2164213 1 7.18
CHEMBL2164218 1 6.86
CHEMBL2164205 1 6.46
CHEMBL1926888 1 5.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164202 IC50 = 1.6 nM 8.80
CHEMBL2164207 IC50 = 1.9 nM 8.72
CHEMBL2164210 IC50 = 2.9 nM 8.54
CHEMBL2164208 IC50 = 4.8 nM 8.32
CHEMBL2164212 IC50 = 6.9 nM 8.16
CHEMBL2164209 IC50 = 7.3 nM 8.14
CHEMBL2164206 IC50 = 14.8 nM 7.83
CHEMBL2164203 IC50 = 15.5 nM 7.81
CHEMBL2164201 IC50 = 16.1 nM 7.79
CHEMBL2164220 IC50 = 17.1 nM 7.77
CHEMBL2164211 IC50 = 21.3 nM 7.67
CHEMBL2164215 IC50 = 22.5 nM 7.65
CHEMBL2164217 IC50 = 34.4 nM 7.46
CHEMBL2164219 IC50 = 38.0 nM 7.42
CHEMBL2164213 IC50 = 65.9 nM 7.18
CHEMBL2164218 IC50 = 138.0 nM 6.86
CHEMBL2164205 IC50 = 344.0 nM 6.46
CHEMBL1926888 IC50 = 1832.0 nM 5.74