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Assay Detail

CHEMBL712000

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

Functional
Inhibition of Efavirenz resistant HIV-1 (K103N-Y181C) induced cytopathicity in MT-4 cells.
18
Total Activities
18
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 Expert

Target

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

Publication

Simple, short peptide derivatives of a sulfonylindolecarboxamide (L-737,126) active in vitro against HIV-1 wild type and variants carrying non-nucleoside reverse transcriptase inhibitor resistance mutations.
Silvestri R, Artico M, De Martino G, La Regina G, Loddo R, La Colla M, Mura M, La Colla P.
J Med Chem (2004) 47 : 3892 -3896
PubMed 15239667 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 18 5.67 6.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL223228 EFAVIRENZ 4.0 1 6.82
CHEMBL85059 1 6.22
CHEMBL127012 1 6.16
CHEMBL126603 1 6.10
CHEMBL126278 1 5.92
CHEMBL127048 1 5.70
CHEMBL2370619 1 5.66
CHEMBL129797 1 5.55
CHEMBL2370614 1 5.46
CHEMBL129707 1 5.33
CHEMBL2370613 1 5.28
CHEMBL340564 1 5.22
CHEMBL283950 L-737126 1 5.10
CHEMBL443548 1 4.80
CHEMBL81097 1 -
CHEMBL129046 1 -
CHEMBL338559 1 -
CHEMBL57 NEVIRAPINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL223228 EFAVIRENZ EC50 = 150.0 nM 6.82
CHEMBL85059 EC50 = 600.0 nM 6.22
CHEMBL127012 EC50 = 700.0 nM 6.16
CHEMBL126603 EC50 = 800.0 nM 6.10
CHEMBL126278 EC50 = 1200.0 nM 5.92
CHEMBL127048 EC50 = 2000.0 nM 5.70
CHEMBL2370619 EC50 = 2200.0 nM 5.66
CHEMBL129797 EC50 = 2800.0 nM 5.55
CHEMBL2370614 EC50 = 3500.0 nM 5.46
CHEMBL129707 EC50 = 4700.0 nM 5.33
CHEMBL2370613 EC50 = 5300.0 nM 5.28
CHEMBL340564 EC50 = 6000.0 nM 5.22
CHEMBL283950 L-737126 EC50 = 8000.0 nM 5.10
CHEMBL443548 EC50 = 16000.0 nM 4.80
CHEMBL81097 EC50 >= 100000.0 nM -
CHEMBL129046 EC50 > 11000.0 nM -
CHEMBL338559 EC50 > 20000.0 nM -
CHEMBL57 NEVIRAPINE EC50 > 30000.0 nM -