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Assay Detail

CHEMBL4047805

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

Functional
Anti-viral activity against HIV-1 LAI infected in human MT2 cells assessed as reduction in p24 Gag protein production
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Design, synthesis, X-ray studies, and biological evaluation of novel macrocyclic HIV-1 protease inhibitors involving the P1'-P2' ligands.
Ghosh AK, Sean Fyvie W, Brindisi M, Steffey M, Agniswamy J, Wang YF, Aoki M, Amano M, Weber IT, Mitsuya H.
Bioorg Med Chem Lett (2017) 27 : 4925 -4931
PubMed 28958624 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 7.66 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067478 1 8.70
CHEMBL1323 DARUNAVIR 4.0 1 8.52
CHEMBL4076488 1 8.28
CHEMBL4096469 1 7.66
CHEMBL4083439 1 7.51
CHEMBL4095133 1 7.34
CHEMBL4079687 1 7.27
CHEMBL4091175 1 6.91
CHEMBL4070241 1 6.75
CHEMBL4073734 1 -
CHEMBL4096186 1 -
CHEMBL4068907 1 -
CHEMBL4074816 1 -
CHEMBL4095267 1 -
CHEMBL4080889 1 -
CHEMBL4100548 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067478 IC50 = 2.0 nM 8.70
CHEMBL1323 DARUNAVIR IC50 = 3.0 nM 8.52
CHEMBL4076488 IC50 = 5.3 nM 8.28
CHEMBL4096469 IC50 = 22.0 nM 7.66
CHEMBL4083439 IC50 = 31.0 nM 7.51
CHEMBL4095133 IC50 = 46.0 nM 7.34
CHEMBL4079687 IC50 = 54.0 nM 7.27
CHEMBL4091175 IC50 = 122.0 nM 6.91
CHEMBL4070241 IC50 = 176.0 nM 6.75
CHEMBL4073734 IC50 - -
CHEMBL4096186 IC50 > 1000.0 nM -
CHEMBL4068907 IC50 - -
CHEMBL4074816 IC50 - -
CHEMBL4095267 IC50 - -
CHEMBL4080889 IC50 > 1000.0 nM -
CHEMBL4100548 IC50 - -