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Assay Detail

CHEMBL5345477

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

Binding
Competitive binding affinity to HIV-1 NL4.3 hexameric capsid protein assessed as inhibition of CPSF6 binding to capsid protein by SPR analysis
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Structural capsid protein (CHEMBL2366504)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Discovery, Crystallographic Studies, and Mechanistic Investigations of Novel Phenylalanine Derivatives Bearing a Quinazolin-4-one Scaffold as Potent HIV Capsid Modulators.
Xu S, Sun L, Barnett M, Zhang X, Ding D, Gattu A, Shi D, Taka JRH, Shen W, Jiang X, Cocklin S, De Clercq E, Pannecouque C, Goldstone DC, Liu X, Dick A, Zhan P.
J Med Chem (2023) 66 : 16303 -16329
PubMed 38054267 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 7.03 7.58

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4788393 1 7.58
CHEMBL5422125 1 6.79
CHEMBL5419397 1 6.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4788393 IC50 = 26.6 nM 7.58
CHEMBL5422125 IC50 = 163.3 nM 6.79
CHEMBL5419397 IC50 = 189.2 nM 6.72