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Assay Detail

CHEMBL691398

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

Binding
In vitro inhibition HIV-1 IIIB protease.
18
Total Activities
18
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

Design, synthesis, and activity of conformationally-constrained macrocyclic peptide-based inhibitors of HIV protease
Smith RA, Coles PJ, Chen JJ, Robinson VJ, MacDonald I, Carriere J, Krantz A
Bioorg Med Chem Lett (1994) 4 : 2217 -2222
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 18 7.76 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL114 SAQUINAVIR 4.0 1 9.70
CHEMBL72386 1 9.05
CHEMBL68313 1 9.00
CHEMBL433309 1 8.82
CHEMBL72474 1 8.52
CHEMBL431387 1 8.47
CHEMBL305466 1 8.26
CHEMBL305463 1 8.22
CHEMBL306727 1 8.14
CHEMBL306897 1 8.10
CHEMBL70787 1 8.00
CHEMBL431754 1 7.89
CHEMBL305063 1 7.60
CHEMBL430984 1 7.06
CHEMBL305289 1 6.40
CHEMBL302486 1 6.35
CHEMBL304369 1 6.05
CHEMBL305290 1 4.05

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL114 SAQUINAVIR IC50 = 0.2 nM 9.70
CHEMBL72386 IC50 = 0.9 nM 9.05
CHEMBL68313 IC50 = 1.0 nM 9.00
CHEMBL433309 IC50 = 1.5 nM 8.82
CHEMBL72474 IC50 = 3.0 nM 8.52
CHEMBL431387 IC50 = 3.4 nM 8.47
CHEMBL305466 IC50 = 5.5 nM 8.26
CHEMBL305463 IC50 = 6.0 nM 8.22
CHEMBL306727 IC50 = 7.3 nM 8.14
CHEMBL306897 IC50 = 8.0 nM 8.10
CHEMBL70787 IC50 = 10.0 nM 8.00
CHEMBL431754 IC50 = 13.0 nM 7.89
CHEMBL305063 IC50 = 25.0 nM 7.60
CHEMBL430984 IC50 = 88.0 nM 7.06
CHEMBL305289 IC50 = 400.0 nM 6.40
CHEMBL302486 IC50 = 450.0 nM 6.35
CHEMBL304369 IC50 = 900.0 nM 6.05
CHEMBL305290 IC50 = 90000.0 nM 4.05