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Assay Detail

CHEMBL926964

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Functional
Antiviral activity against HIV1 LAI in MT2 cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT2
Confidence 1 — Organism
Curated By Intermediate

Target

Human immunodeficiency virus 1 (CHEMBL378)
Type ORGANISM
Organism Human immunodeficiency virus 1

Publication

Potent inhibition of HIV-1 replication by novel non-peptidyl small molecule inhibitors of protease dimerization.
Koh Y, Matsumi S, Das D, Amano M, Davis DA, Li J, Leschenko S, Baldridge A, Shioda T, Yarchoan R, Ghosh AK, Mitsuya H.
J Biol Chem (2007) 282 : 28709 -28720
PubMed 17635930 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.45 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL206031 BRECANAVIR 2.0 1 9.70
CHEMBL469086 1 9.52
CHEMBL178593 1 9.40
CHEMBL254349 1 8.85
CHEMBL1323 DARUNAVIR 4.0 1 8.47
CHEMBL403306 1 8.30
CHEMBL222559 TIPRANAVIR 4.0 1 7.00
CHEMBL256107 1 6.32

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL206031 BRECANAVIR IC50 = 0.2 nM 9.70
CHEMBL469086 IC50 = 0.3 nM 9.52
CHEMBL178593 IC50 = 0.4 nM 9.40
CHEMBL254349 IC50 = 1.4 nM 8.85
CHEMBL1323 DARUNAVIR IC50 = 3.4 nM 8.47
CHEMBL403306 IC50 = 5.0 nM 8.30
CHEMBL222559 TIPRANAVIR IC50 = 100.0 nM 7.00
CHEMBL256107 IC50 = 480.0 nM 6.32