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Assay Detail

CHEMBL4189597

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

Binding
Inhibition of HIV1 NL4-3 protease assessed as decrease in viral replication in human MT2 cells after 4 days by luciferase reporter gene assay
3
Total Activities
3
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 Intermediate

Target

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

Publication

Coupling of an Acyl Migration Prodrug Strategy with Bio-activation To Improve Oral Delivery of the HIV-1 Protease Inhibitor Atazanavir.
Subbaiah MAM, Meanwell NA, Kadow JF, Subramani L, Annadurai M, Ramar T, Desai SD, Sinha S, Subramanian M, Mandlekar S, Sridhar S, Padmanabhan S, Bhutani P, Arla R, Jenkins SM, Krystal MR, Wang C, Sarabu R.
J Med Chem (2018) 61 : 4176 -4188
PubMed 29693401 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 8.72 9.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1163 ATAZANAVIR 4.0 1 9.15
CHEMBL4208792 1 8.74
CHEMBL4216648 1 8.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1163 ATAZANAVIR EC50 = 0.7 nM 9.15
CHEMBL4208792 EC50 = 1.8 nM 8.74
CHEMBL4216648 EC50 = 5.3 nM 8.28