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Assay Detail

CHEMBL891821

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Functional
Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay
14
Total Activities
14
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 Intermediate

Target

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

Publication

Synthesis of novel diarylpyrimidine analogues of TMC278 and their antiviral activity against HIV-1 wild-type and mutant strains.
Mordant C, Schmitt B, Pasquier E, Demestre C, Queguiner L, Masungi C, Peeters A, Smeulders L, Bettens E, Hertogs K, Heeres J, Lewi P, Guillemont J.
Eur J Med Chem (2007) 42 : 567 -579
PubMed 17223230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 8.31 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL242408 1 9.52
CHEMBL175691 RILPIVIRINE 4.0 1 9.30
CHEMBL242616 1 9.30
CHEMBL231281 1 9.15
CHEMBL242617 1 9.10
CHEMBL231582 1 9.00
CHEMBL242189 1 8.96
CHEMBL231482 1 8.92
CHEMBL231282 1 8.85
CHEMBL242407 1 8.41
CHEMBL223228 EFAVIRENZ 4.0 1 7.33
CHEMBL388225 1 7.01
CHEMBL57 NEVIRAPINE 4.0 1 6.08
CHEMBL593 DELAVIRDINE 4.0 1 5.34

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL242408 EC50 = 0.3 nM 9.52
CHEMBL175691 RILPIVIRINE EC50 = 0.5 nM 9.30
CHEMBL242616 EC50 = 0.5 nM 9.30
CHEMBL231281 EC50 = 0.7 nM 9.15
CHEMBL242617 EC50 = 0.8 nM 9.10
CHEMBL231582 EC50 = 1.0 nM 9.00
CHEMBL242189 EC50 = 1.1 nM 8.96
CHEMBL231482 EC50 = 1.2 nM 8.92
CHEMBL231282 EC50 = 1.4 nM 8.85
CHEMBL242407 EC50 = 3.9 nM 8.41
CHEMBL223228 EFAVIRENZ EC50 = 46.9 nM 7.33
CHEMBL388225 EC50 = 98.4 nM 7.01
CHEMBL57 NEVIRAPINE EC50 = 827.0 nM 6.08
CHEMBL593 DELAVIRDINE EC50 = 4560.0 nM 5.34