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Assay Detail

CHEMBL1026417

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

Functional
Antiviral activity against multidrug-resistant HIV1 with protease L10I, V11I, T12E, I15V, L19I, R41K, M46L, L63P, A71T, V82A, L90M mutation in phytohemagglutininin-activated PBMC assessed as inhibition of p24G protein production
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Flexible cyclic ethers/polyethers as novel P2-ligands for HIV-1 protease inhibitors: design, synthesis, biological evaluation, and protein-ligand X-ray studies.
Ghosh AK, Gemma S, Baldridge A, Wang YF, Kovalevsky AY, Koh Y, Weber IT, Mitsuya H.
J Med Chem (2008) 51 : 6021 -6033
PubMed 18783203 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 6.82 8.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1323 DARUNAVIR 4.0 1 8.15
CHEMBL5483011 INDINAVIR 3.0 1 6.54
CHEMBL523528 1 6.52
CHEMBL116 AMPRENAVIR 4.0 1 6.47
CHEMBL492254 1 6.44
CHEMBL163 RITONAVIR 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1323 DARUNAVIR IC50 = 7.0 nM 8.15
CHEMBL5483011 INDINAVIR IC50 = 290.0 nM 6.54
CHEMBL523528 IC50 = 300.0 nM 6.52
CHEMBL116 AMPRENAVIR IC50 = 340.0 nM 6.47
CHEMBL492254 IC50 = 360.0 nM 6.44
CHEMBL163 RITONAVIR IC50 > 1000.0 nM -