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Assay Detail

CHEMBL2318302

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

Binding
Inhibition of HIV-1 protease R8Q mutant using Abz-Thr-Ile-Nle-p-nitro-Phe-Gln-Arg-NH2 as substrate incubated for 5 mins prior to substrate addition measured for 5 mins by fluorescence assay
1
Total Activities
1
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

Human immunodeficiency virus type 1 protease (CHEMBL243)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Novel P2 tris-tetrahydrofuran group in antiviral compound 1 (GRL-0519) fills the S2 binding pocket of selected mutants of HIV-1 protease.
Zhang H, Wang YF, Shen CH, Agniswamy J, Rao KV, Xu CX, Ghosh AK, Harrison RW, Weber IT.
J Med Chem (2013) 56 : 1074 -1083
PubMed 23298236 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 1 8.92 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1232930 1 8.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1232930 Ki = 1.2 nM 8.92