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Assay Detail

CHEMBL4223433

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

Binding
Binding affinity to CA-SP1 P373S/V370A double mutant in HIV-1 subtype B NL4-3 infected in human MT2 cells assessed as inhibition of viral maturation by measuring virus yield after 4 to 5 days in presence of 10% FBS/27 mg/ml HSA/40% human serum by luciferase reporter gene assay
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Human immunodeficiency virus 1
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Gag-Pol polyprotein (CHEMBL3638360)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus type 1 group M subtype B (isolate HXB2)(HIV-1)

Publication

The design, synthesis and structure-activity relationships associated with C28 amine-based betulinic acid derivatives as inhibitors of HIV-1 maturation.
Chen Y, Sit SY, Chen J, Swidorski JJ, Liu Z, Sin N, Venables BL, Parker DD, Nowicka-Sans B, Lin Z, Li Z, Terry BJ, Protack T, Rahematpura S, Hanumegowda U, Jenkins S, Krystal M, Dicker ID, Meanwell NA, Regueiro-Ren A.
Bioorg Med Chem Lett (2018) 28 : 1550 -1557
PubMed 29631960 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 1 7.82 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3827026 1 7.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3827026 EC50 = 15.0 nM 7.82