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Assay Detail

CHEMBL925700

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

Binding
Inhibition of HIV1 protease
8
Total Activities
7
Compounds Tested
3
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

Protease (CHEMBL2366517)
Type SINGLE PROTEIN
Organism Human immunodeficiency virus 1

Publication

Darunavir, a conceptually new HIV-1 protease inhibitor for the treatment of drug-resistant HIV.
Ghosh AK, Dawson ZL, Mitsuya H.
Bioorg Med Chem (2007) 15 : 7576 -7580
PubMed 17900913 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 10.55 10.85
IC50 2 8.74 8.74
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL469086 1 10.85
CHEMBL1323 DARUNAVIR 4.0 1 10.80
CHEMBL254841 1 10.00
CHEMBL315403 1 8.74
CHEMBL254349 2 8.74
CHEMBL254419 1 -
CHEMBL168640 PPL-100 1.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL469086 Ki = 0.014 nM 10.85
CHEMBL1323 DARUNAVIR Ki = 0.016 nM 10.80
CHEMBL254841 Ki = 0.1 nM 10.00
CHEMBL315403 IC50 = 1.8 nM 8.74
CHEMBL254349 IC50 = 1.8 nM 8.74
CHEMBL254349 Ki = 0.0045 nM -
CHEMBL254419 Activity < 20.0 nM -
CHEMBL168640 PPL-100 Activity < 20.0 nM -