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Assay Detail

CHEMBL769369

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Binding
Inhibition of HIV-1 Protease.
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

Discovery of a novel class of potent HIV-1 protease inhibitors containing the (R)-(hydroxyethyl)urea isostere.
Getman DP, DeCrescenzo GA, Heintz RM, Reed KL, Talley JJ, Bryant ML, Clare M, Houseman KA, Marr JJ, Mueller RA.
J Med Chem (1993) 36 : 288 -291
PubMed 8423599 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 6.83 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL99616 1 8.52
CHEMBL98002 1 8.52
CHEMBL317933 1 8.30
CHEMBL322241 TELINAVIR 2.0 1 8.22
CHEMBL100039 1 7.89
CHEMBL98302 1 7.72
CHEMBL329068 1 7.72
CHEMBL98150 1 7.54
CHEMBL99211 1 7.46
CHEMBL430674 1 6.98
CHEMBL100034 1 6.90
CHEMBL317077 1 6.58
CHEMBL98533 1 6.48
CHEMBL99934 1 6.29
CHEMBL99015 1 6.03
CHEMBL48996 1 5.72
CHEMBL607102 1 5.29
CHEMBL607101 1 5.19
CHEMBL99317 1 5.00
CHEMBL99268 1 4.27

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL99616 IC50 = 3.0 nM 8.52
CHEMBL98002 IC50 = 3.0 nM 8.52
CHEMBL317933 IC50 = 5.0 nM 8.30
CHEMBL322241 TELINAVIR IC50 = 6.0 nM 8.22
CHEMBL100039 IC50 = 13.0 nM 7.89
CHEMBL98302 IC50 = 19.0 nM 7.72
CHEMBL329068 IC50 = 19.0 nM 7.72
CHEMBL98150 IC50 = 29.0 nM 7.54
CHEMBL99211 IC50 = 35.0 nM 7.46
CHEMBL430674 IC50 = 105.0 nM 6.98
CHEMBL100034 IC50 = 126.0 nM 6.90
CHEMBL317077 IC50 = 260.0 nM 6.58
CHEMBL98533 IC50 = 330.0 nM 6.48
CHEMBL99934 IC50 = 518.0 nM 6.29
CHEMBL99015 IC50 = 940.0 nM 6.03
CHEMBL48996 IC50 = 1900.0 nM 5.72
CHEMBL607102 IC50 = 5100.0 nM 5.29
CHEMBL607101 IC50 = 6500.0 nM 5.19
CHEMBL99317 IC50 = 10000.0 nM 5.00
CHEMBL99268 IC50 = 54000.0 nM 4.27