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Assay Detail

CHEMBL5154014

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

Functional
Antiviral activity against HIV-1 Ba-L infected in human TZM-bl cells measured after 48 hrs incubation by luciferase based analysis
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type TZM-bl
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Structure-Based Design of Tropane Derivatives as a Novel Series of CCR5 Antagonists with Broad-Spectrum Anti-HIV-1 Activities and Improved Oral Bioavailability.
Xie X, Zheng YG, Chen H, Li J, Luo RH, Chen L, Zheng CB, Zhang S, Peng P, Ma D, Yang LM, Zheng YT, Liu H, Wang J.
J Med Chem (2022) 65 : 16526 -16540
PubMed 36472561 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 16 6.69 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5175220 1 8.00
CHEMBL5209067 1 7.96
CHEMBL256907 MARAVIROC 4.0 1 7.82
CHEMBL5171331 1 7.52
CHEMBL4240742 1 7.11
CHEMBL5177519 1 6.27
CHEMBL5180628 1 6.04
CHEMBL5178495 1 5.47
CHEMBL5205216 1 5.34
CHEMBL5197247 1 5.33
CHEMBL5184978 1 -
CHEMBL5205626 1 -
CHEMBL5208613 1 -
CHEMBL5169473 1 -
CHEMBL5194455 1 -
CHEMBL5171807 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5175220 EC50 = 10.0 nM 8.00
CHEMBL5209067 EC50 = 11.0 nM 7.96
CHEMBL256907 MARAVIROC EC50 = 15.0 nM 7.82
CHEMBL5171331 EC50 = 30.0 nM 7.52
CHEMBL4240742 EC50 = 78.0 nM 7.11
CHEMBL5177519 EC50 = 540.0 nM 6.27
CHEMBL5180628 EC50 = 910.0 nM 6.04
CHEMBL5178495 EC50 = 3390.0 nM 5.47
CHEMBL5205216 EC50 = 4540.0 nM 5.34
CHEMBL5197247 EC50 = 4630.0 nM 5.33
CHEMBL5184978 EC50 > 200000.0 nM -
CHEMBL5205626 EC50 > 50000.0 nM -
CHEMBL5208613 EC50 > 50000.0 nM -
CHEMBL5169473 EC50 > 200000.0 nM -
CHEMBL5194455 EC50 > 200000.0 nM -
CHEMBL5171807 EC50 > 200000.0 nM -