General
Preferred name
EFAVIRENZ
Synonyms
EFV ()
DMP 266 ()
Sustiva ()
Stocrin ()
L-743726 ()
Elavirenz ()
Sustiva, Stocrin, DMP-266, DMP 266 ()
(S)-6-Chloro-4-(cyclopropylethynyl)-4-(trifluoromethyl)-1,4-dihydro-2H-benzo[d][1,3]oxazin-2-one ()
Efavirenz component of atripla ()
NSC-742403 ()
Sustiva 600 ()
Efavirenz component of symfi ()
Efavirenz component of telura ()
DMP-266 ()
Viraday ()
Efavirenzum ()
(-)-efavirenz ()
Efavirenz teva ()
P&D ID
PD003010
CAS
154598-52-4
Tags
available
drug
Approved by
EMA
FDA
First approval
1998
Drug indication
Human immunodeficiency virus infection
HIV-1 infection
Drug Status
approved
investigational
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION Efavirenz is an antiviral drug that is used in the treatment of HIV. It is a synthetic non-nucleoside inhibitor (NNRTI) that binds to the HIV RNA-dependent DNA polymerase and thereby blocks viral DNA replication . (GtoPdb)
DESCRIPTION Efavirenz (DMP 266) is a potent inhibitor of the wild-type HIV-1 reverse transcriptase with a Ki of 2.93 nM and exhibits an IC95 of 1.5 nM for the inhibition of HIV-1 replicative spread in cell culture[1].
PRICE 38
DESCRIPTION Non-nucleoside reverse transcriptase inhibitors (NNRTIs) are highly specific and potent allosteric inhibitors of human immunodeficiency virus type 1 (HIV-1) reverse transcriptase. Efavirenz is an NNRTI that prevents RNA plus-strand initiation with an IC50 value of 17 nM. Efavirenz also inhibits the late stages of HIV-1 replication by interfering with HIV-1 Gag-Pol polyprotein processing. It has been used in combination therapy with drugs directed at the treatment of opportunistic infections such as HIV and cancer. (BOC Sciences Bioactive Compounds)
DESCRIPTION Efavirenz is a non-nucleoside reverse transcriptase inhibitor used to treat HIV infection or prevent the spread of HIV. (Enamine Bioactive Compounds)
DESCRIPTION Efavirenz (DMP 266) is a Human Immunodeficiency Virus 1 Non-Nucleoside Analog Reverse Transcriptase Inhibitor, acting as a Non-Nucleoside Reverse Transcriptase Inhibitor, Cytochrome P450 3A Inducer, Cytochrome P450 2B6 Inducer, Cytochrome P450 2C9 Inhibitor, Cytochrome P450 2C19 Inhibitor, and Cytochrome P450 3A4 Inhibitor, classified as a Non-Nucleoside Analog. (TargetMol Bioactive Compound Library)
Cell lines
4
Organisms
9
Compound Sets
25
Axon Medchem Screening Library
Cayman Chemical Bioactives
CeMM library of unique drugs (CLOUD)
ChEMBL Approved Drugs
ChEMBL Drugs
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
Enamine Bioactive Compounds
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
External IDs
47
Properties
(calculated by RDKit )
Molecular Weight
315.03
Hydrogen Bond Acceptors
2
Hydrogen Bond Donors
1
Rotatable Bonds
0
Ring Count
3
Aromatic Ring Count
1
cLogP
4.07
TPSA
38.33
Fraction CSP3
0.36
Chiral centers
1.0
Largest ring
6.0
QED
0.73
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target
Human immunodeficiency virus type 1 reverse transcriptase
Gag-Pol polyprotein
CYP1A2, CYP2B6, CYP2C19, CYP2C9, CYP2D6, CYP3A4
NNRT inhibitor
Reverse Transcriptase
Endogenous Metabolite
HIV
Parasite
HIV-1 RT
MOA
viral reverse transcriptase inhibitor
HIV Protease inhibitor
Indication
human immunodeficiency virus (HIV-1)
Pathway
Autophagy
Microbiology/virology
Proteases/Proteasome
Anti-infection
Metabolic Enzyme/Protease
Therapeutic Class
Anti-HIV Agents
Solubility
In Vitro:<br/>DMSO: ≥ 38 mg/mL (120.38 mM)
Source data