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Assay Detail

CHEMBL867569

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

Binding
Inhibitory activity against HIV1 protease expressed in Escherichia coli in a fluorometric assay
10
Total Activities
10
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

A new class of HIV-1 protease inhibitors containing a tertiary alcohol in the transition-state mimicking scaffold.
Ekegren JK, Unge T, Safa MZ, Wallberg H, Samuelsson B, Hallberg A.
J Med Chem (2005) 48 : 8098 -8102
PubMed 16335934 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.46 8.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL197500 1 8.62
CHEMBL436755 1 8.22
CHEMBL197165 1 8.05
CHEMBL438804 1 7.77
CHEMBL372806 1 7.75
CHEMBL370132 1 7.66
CHEMBL370127 1 7.64
CHEMBL369929 1 7.20
CHEMBL198534 1 6.06
CHEMBL198645 1 5.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL197500 Ki = 2.4 nM 8.62
CHEMBL436755 Ki = 6.0 nM 8.22
CHEMBL197165 Ki = 9.0 nM 8.05
CHEMBL438804 Ki = 17.0 nM 7.77
CHEMBL372806 Ki = 18.0 nM 7.75
CHEMBL370132 Ki = 22.0 nM 7.66
CHEMBL370127 Ki = 23.0 nM 7.64
CHEMBL369929 Ki = 63.0 nM 7.20
CHEMBL198534 Ki = 870.0 nM 6.06
CHEMBL198645 Ki = 2200.0 nM 5.66