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Assay Detail

CHEMBL5238916

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

Functional
Antiviral activity against wild type HIV-1 NLRepRlucP373S harboring R361K/V362I/L363M mutant infected in human MT2 cells assessed as inhibition of viral growth measured after 4 to 5 days by Dual luciferase reporter assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Synthesis, Structure-Activity Relationships, and <i>In Vivo</i> Evaluation of Novel C-17 Amine Derivatives Based on GSK3640254 as HIV-1 Maturation Inhibitors with Broad Spectrum Activity.
Hartz RA, Xu L, Sit SY, Chen J, Venables BL, Lin Z, Zhang S, Li Z, Parker D, Simmons TS, Jenkins S, Hanumegowda UM, Dicker I, Krystal M, Meanwell NA, Regueiro-Ren A.
J Med Chem (2022) 65 : 15935 -15966
PubMed 36441509 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 8.34 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5201510 FIPRAVIRIMAT 2.0 1 8.52
CHEMBL5285267 1 8.35
CHEMBL5268258 1 8.29
CHEMBL5272708 1 8.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5201510 FIPRAVIRIMAT EC50 = 3.0 nM 8.52
CHEMBL5285267 EC50 = 4.5 nM 8.35
CHEMBL5268258 EC50 = 5.1 nM 8.29
CHEMBL5272708 EC50 = 6.1 nM 8.21