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Assay Detail

CHEMBL879331

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Binding
Inhibitory activity against HIV-1 protease expressed in Escherichia coli
12
Total Activities
12
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 Expert

Target

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

Publication

Design and fast synthesis of C-terminal duplicated potent C(2)-symmetric P1/P1'-modified HIV-1 protease inhibitors.
Alterman M, Andersson HO, Garg N, Ahlsén G, Lövgren S, Classon B, Danielson UH, Kvarnström I, Vrang L, Unge T, Samuelsson B, Hallberg A.
J Med Chem (1999) 42 : 3835 -3844
PubMed 10508432 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 9.23 10.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127045 1 10.05
CHEMBL124139 1 9.52
CHEMBL338428 1 9.52
CHEMBL123850 1 9.52
CHEMBL105459 1 9.40
CHEMBL340116 1 9.22
CHEMBL127524 1 9.22
CHEMBL125420 1 9.15
CHEMBL127214 1 8.92
CHEMBL333399 1 8.92
CHEMBL264815 1 8.85
CHEMBL441167 1 8.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127045 Ki = 0.09 nM 10.05
CHEMBL124139 Ki = 0.3 nM 9.52
CHEMBL338428 Ki = 0.3 nM 9.52
CHEMBL123850 Ki = 0.3 nM 9.52
CHEMBL105459 Ki = 0.4 nM 9.40
CHEMBL340116 Ki = 0.6 nM 9.22
CHEMBL127524 Ki = 0.6 nM 9.22
CHEMBL125420 Ki = 0.7 nM 9.15
CHEMBL127214 Ki = 1.2 nM 8.92
CHEMBL333399 Ki = 1.2 nM 8.92
CHEMBL264815 Ki = 1.4 nM 8.85
CHEMBL441167 Ki = 3.8 nM 8.42