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Assay Detail

CHEMBL895981

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

Binding
Inhibition of Wild type HIV1 Protease by FRET based assay
20
Total Activities
20
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 Autocuration

Target

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

Publication

Design and synthesis of HIV-1 protease inhibitors incorporating oxazolidinones as P2/P2' ligands in pseudosymmetric dipeptide isosteres.
Reddy GS, Ali A, Nalam MN, Anjum SG, Cao H, Nathans RS, Schiffer CA, Rana TM.
J Med Chem (2007) 50 : 4316 -4328
PubMed 17696512 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 20 7.57 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL388680 1 9.07
CHEMBL388901 1 9.01
CHEMBL245221 1 8.69
CHEMBL245003 1 8.67
CHEMBL437356 1 8.58
CHEMBL230771 1 8.46
CHEMBL395064 1 8.15
CHEMBL388689 1 8.14
CHEMBL243053 1 8.09
CHEMBL395065 1 7.97
CHEMBL397231 1 7.67
CHEMBL243054 1 7.46
CHEMBL388688 1 7.40
CHEMBL397462 1 7.39
CHEMBL245002 1 6.88
CHEMBL243868 1 6.52
CHEMBL397461 1 6.18
CHEMBL244764 1 5.96
CHEMBL244758 1 5.75
CHEMBL267966 1 5.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL388680 Ki = 0.85 nM 9.07
CHEMBL388901 Ki = 0.98 nM 9.01
CHEMBL245221 Ki = 2.04 nM 8.69
CHEMBL245003 Ki = 2.13 nM 8.67
CHEMBL437356 Ki = 2.62 nM 8.58
CHEMBL230771 Ki = 3.51 nM 8.46
CHEMBL395064 Ki = 7.0 nM 8.15
CHEMBL388689 Ki = 7.28 nM 8.14
CHEMBL243053 Ki = 8.05 nM 8.09
CHEMBL395065 Ki = 10.6 nM 7.97
CHEMBL397231 Ki = 21.63 nM 7.67
CHEMBL243054 Ki = 35.11 nM 7.46
CHEMBL388688 Ki = 39.87 nM 7.40
CHEMBL397462 Ki = 41.09 nM 7.39
CHEMBL245002 Ki = 131.4 nM 6.88
CHEMBL243868 Ki = 300.0 nM 6.52
CHEMBL397461 Ki = 657.0 nM 6.18
CHEMBL244764 Ki = 1090.0 nM 5.96
CHEMBL244758 Ki = 1800.0 nM 5.75
CHEMBL267966 Ki = 4731.0 nM 5.33