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Assay Detail

CHEMBL1037784

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

Functional
Antiviral activity against indinavir-resistant HIV1 harboring L10R/M46I/L63P/V82T/I84V mutant protease infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type MT4
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Small-sized human immunodeficiency virus type-1 protease inhibitors containing allophenylnorstatine to explore the S2' pocket.
Hidaka K, Kimura T, Abdel-Rahman HM, Nguyen JT, McDaniel KF, Kohlbrenner WE, Molla A, Adachi M, Tamada T, Kuroki R, Katsuki N, Tanaka Y, Matsumoto H, Wang J, Hayashi Y, Kempf DJ, Kiso Y.
J Med Chem (2009) 52 : 7604 -7617
PubMed 19954246 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 15 6.22 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL300891 1 7.00
CHEMBL584761 1 6.81
CHEMBL584342 1 6.80
CHEMBL577569 1 6.76
CHEMBL729 LOPINAVIR 4.0 1 6.42
CHEMBL575276 1 6.39
CHEMBL584969 1 6.38
CHEMBL574652 1 6.33
CHEMBL584763 1 6.25
CHEMBL466535 1 5.85
CHEMBL576364 1 5.76
CHEMBL575717 1 5.71
CHEMBL573747 1 5.69
CHEMBL573061 1 5.66
CHEMBL575916 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL300891 EC50 = 100.0 nM 7.00
CHEMBL584761 EC50 = 155.0 nM 6.81
CHEMBL584342 EC50 = 157.0 nM 6.80
CHEMBL577569 EC50 = 173.0 nM 6.76
CHEMBL729 LOPINAVIR EC50 = 385.0 nM 6.42
CHEMBL575276 EC50 = 409.0 nM 6.39
CHEMBL584969 EC50 = 416.0 nM 6.38
CHEMBL574652 EC50 = 470.0 nM 6.33
CHEMBL584763 EC50 = 568.0 nM 6.25
CHEMBL466535 EC50 = 1420.0 nM 5.85
CHEMBL576364 EC50 = 1730.0 nM 5.76
CHEMBL575717 EC50 = 1930.0 nM 5.71
CHEMBL573747 EC50 = 2030.0 nM 5.69
CHEMBL573061 EC50 = 2200.0 nM 5.66
CHEMBL575916 EC50 = 3010.0 nM 5.52