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Assay Detail

CHEMBL825072

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

Functional
Effective concentration of compound to inhibit human immunodeficiency virus HIV-1 wild type strain IIIB multiplication in MT-4 infected cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and evaluation of double-prodrugs against HIV. Conjugation of D4T with 6-benzyl-1-(ethoxymethyl)-5-isopropyluracil (MKC-442, emivirine)-type reverse transcriptase inhibitors via the SATE prodrug approach.
Petersen L, Jørgensen PT, Nielsen C, Hansen TH, Nielsen J, Pedersen EB.
J Med Chem (2005) 48 : 1211 -1220
PubMed 15715487 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 9 7.70 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL178880 1 8.52
CHEMBL178164 1 8.52
CHEMBL179744 1 8.30
CHEMBL180477 1 7.70
CHEMBL35033 EMIVIRINE 2.0 1 7.52
CHEMBL361382 1 7.52
CHEMBL434333 1 7.52
CHEMBL360887 1 7.40
CHEMBL991 STAVUDINE 4.0 1 6.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL178880 EC50 = 3.0 nM 8.52
CHEMBL178164 EC50 = 3.0 nM 8.52
CHEMBL179744 EC50 = 5.0 nM 8.30
CHEMBL180477 EC50 = 20.0 nM 7.70
CHEMBL35033 EMIVIRINE EC50 = 30.0 nM 7.52
CHEMBL361382 EC50 = 30.0 nM 7.52
CHEMBL434333 EC50 = 30.0 nM 7.52
CHEMBL360887 EC50 = 40.0 nM 7.40
CHEMBL991 STAVUDINE EC50 = 500.0 nM 6.30