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Assay Detail

CHEMBL3745283

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

Functional
Antiviral activity against HIV-1 X4 expressing reverse transcriptase K103N mutant infected in human CD4+ T cells for 3 days by FACS analysis
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Human immunodeficiency virus 1
Cell Type T-cell
Confidence 1 — Organism
Curated By Autocuration

Target

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

Publication

Potent Inhibitors Active against HIV Reverse Transcriptase with K101P, a Mutation Conferring Rilpivirine Resistance.
Gray WT, Frey KM, Laskey SB, Mislak AC, Spasov KA, Lee WG, Bollini M, Siliciano RF, Jorgensen WL, Anderson KS.
ACS Med Chem Lett (2015) 6 : 1075 -1079
PubMed 26487915 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 7.37 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3342974 1 8.52
CHEMBL175691 RILPIVIRINE 4.0 1 7.89
CHEMBL3342966 1 7.30
CHEMBL1923492 1 7.05
CHEMBL223228 EFAVIRENZ 4.0 1 6.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3342974 EC50 = 3.0 nM 8.52
CHEMBL175691 RILPIVIRINE EC50 = 13.0 nM 7.89
CHEMBL3342966 EC50 = 50.0 nM 7.30
CHEMBL1923492 EC50 = 89.0 nM 7.05
CHEMBL223228 EFAVIRENZ EC50 = 836.0 nM 6.08