Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4392471

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

Binding
Inhibition of HIV1 protease activity
13
Total Activities
13
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, Synthesis, and Pharmacokinetic Evaluation of Phosphate and Amino Acid Ester Prodrugs for Improving the Oral Bioavailability of the HIV-1 Protease Inhibitor Atazanavir.
A M Subbaiah M, Mandlekar S, Desikan S, Ramar T, Subramani L, Annadurai M, Desai SD, Sinha S, Jenkins SM, Krystal MR, Subramanian M, Sridhar S, Padmanabhan S, Bhutani P, Arla R, Singh S, Sinha J, Thakur M, Kadow JF, Meanwell NA.
J Med Chem (2019) 62 : 3553 -3574
PubMed 30938524 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 13 8.49 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1163 ATAZANAVIR 4.0 1 9.52
CHEMBL4300203 1 8.40
CHEMBL4522729 1 8.40
CHEMBL4437104 1 8.40
CHEMBL4474072 1 8.40
CHEMBL4460401 1 8.40
CHEMBL4554438 1 8.40
CHEMBL4447493 1 8.40
CHEMBL4463796 1 8.40
CHEMBL4525849 1 8.40
CHEMBL4542773 1 8.40
CHEMBL4573907 1 8.40
CHEMBL4574382 1 8.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1163 ATAZANAVIR IC50 = 0.3 nM 9.52
CHEMBL4300203 IC50 = 4.0 nM 8.40
CHEMBL4522729 IC50 = 4.0 nM 8.40
CHEMBL4437104 IC50 = 4.0 nM 8.40
CHEMBL4474072 IC50 = 4.0 nM 8.40
CHEMBL4460401 IC50 = 4.0 nM 8.40
CHEMBL4554438 IC50 = 4.0 nM 8.40
CHEMBL4447493 IC50 = 4.0 nM 8.40
CHEMBL4463796 IC50 = 4.0 nM 8.40
CHEMBL4525849 IC50 = 4.0 nM 8.40
CHEMBL4542773 IC50 = 4.0 nM 8.40
CHEMBL4573907 IC50 = 4.0 nM 8.40
CHEMBL4574382 IC50 = 4.0 nM 8.40