BDBM2483 (4S)-6-chloro-4-(2-cyclopropylethynyl)-4-(trifluoromethyl)-2,4-dihydro-1H-3,1-benzoxazin-2-one::CHEMBL223228::DMP-266::EFV::Efavirenz::Efavirenz (EFV)::L-743,726::Sustiva

SMILES c1cc2c(cc1Cl)[C@@](OC(=O)N2)(C#CC3CC3)C(F)(F)F

InChI Key InChIKey=XPOQHMRABVBWPR-UHFFFAOYSA-N

Data  29 KI  177 IC50  3 Kd  33 EC50  1 ITC

PDB links: 11 PDB IDs match this monomer.

  Tab Delimited (TSV)   2D SDfile   Computed 3D by Vconf -m prep SDfile
Find this compound or compounds like it in BindingDB:
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Similarity at least:  must be >=0.5
Exact match

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 247 hits for monomerid = 2483   

TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 47nMpH: 8.2 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 38nMpH: 8.2 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/28/2004
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 48nMpH: 8.2 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 48nMpH: 8.2 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/28/2004
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 48nMpH: 8.2 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 48nMpH: 8.2 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
1/4/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 33nMpH: 7.8 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/6/2004
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027,K690N]/[588-1147,K690N](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 3.40E+3nMpH: 7.8 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/6/2004
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1127,Y768C]/[588-1147,Y768C](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 85nMpH: 7.8 T: 2°CAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/6/2004
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 4nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/28/2004
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1127,Y768C]/[588-1147,Y768C](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 6nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/28/2004
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027,K690N]/[588-1147,K690N](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 61nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
12/28/2004
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 6.90nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/7/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027,K690N]/[588-1147,K690N](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 21nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/7/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1127,Y768C]/[588-1147,Y768C](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 4nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/7/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027]/[588-1147](Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 6.90nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027,K690N]/[588-1147,K690N](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 21nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1127,Y768C]/[588-1147,Y768C](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 4nMAssay Description:The IC50 of reverse transcriptase is the concentration that inhibits 50% of recombinant HIV-1 RT RNA-directed DNA polymerase activity in vitro.More data for this Ligand-Target Pair
In Depth
Date in BDB:
7/19/2005
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 14nMpH: 7.8 T: 2°CAssay Description:The inhibition of the RNA-dependent DNA polymerase activity of the HIV-1 reverse transcriptase enzyme was measured using a primer extension assay. Th...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1027,K691N]/[588-1147,K690N](Human immunodeficiency virus type 1)
Pfizer

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 364nMpH: 7.8 T: 2°CAssay Description:The inhibition of the RNA-dependent DNA polymerase activity of the HIV-1 reverse transcriptase enzyme was measured using a primer extension assay. Th...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [588-1127,Y768C]/[588-1147,Y768C](Human immunodeficiency virus type 1)
Sapienza University of Rome

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 40nMpH: 7.8 T: 2°CAssay Description:The inhibition of the RNA-dependent DNA polymerase activity of the HIV-1 reverse transcriptase enzyme was measured using a primer extension assay. Th...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [600-1028,Y780C]/[600-1151,Y780C](Human immunodeficiency virus type 1)
Rutgers University

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataAssay Description:To assess the effect of inhibitors, RT RNH activity was measured using a FRET-based microplate fluorescence assay. Briefly, the RNA-DNA hybrid duplex...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [600-1028,Y787L]/[600-1151,Y787L](Human immunodeficiency virus type 1)
Rutgers University

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataAssay Description:To assess the effect of inhibitors, RT RNH activity was measured using a FRET-based microplate fluorescence assay. Briefly, the RNA-DNA hybrid duplex...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [600-1028,V705A,Y780C,C879S]/[600-1151,V705A,Y780C,C879S](Human immunodeficiency virus type 1)
Rutgers University

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataAssay Description:To assess the effect of inhibitors, RT RNH activity was measured using a FRET-based microplate fluorescence assay. Briefly, the RNA-DNA hybrid duplex...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein [600-1028,L699I,K702N,C879S]/[600-1151,L699I,K702N,C879S](Human immunodeficiency virus type 1)
Rutgers University

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataAssay Description:To assess the effect of inhibitors, RT RNH activity was measured using a FRET-based microplate fluorescence assay. Briefly, the RNA-DNA hybrid duplex...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataAssay Description:To assess the effect of inhibitors, RT RNH activity was measured using a FRET-based microplate fluorescence assay. Briefly, the RNA-DNA hybrid duplex...More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/10/2009
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase protein(Human immunodeficiency virus type 1)
Birla Institute of Technology

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 25nMAssay Description:The reaction mixture was set with template primer complex, RT enzyme and dNTPs in a lysis buffer with or without inhibitors. The reaction mixture was...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/17/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein(HIV-1)
University of Siena

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 20nMpH: 8.1 T: 2°CAssay Description:RNA-dependent DNA polymerase (RDDP) activity was measured as described[J. Microbiol. 2015, 53:288-293] in Tris HCl buffer (25 mL, 60 mm, pH 8.1) cont...More data for this Ligand-Target Pair
In Depth
Date in BDB:
8/3/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein(HIV-1)
Birla Institute of Technology

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 25nMAssay Description:The reaction mixture was set with template primer complex, RT enzyme and dNTPs in a lysis buffer with or without inhibitors. The reaction mixture was...More data for this Ligand-Target Pair
In Depth
Date in BDB:
9/14/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein(HIV-1)
Birla Institute of Technology

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 25nMpH: 8.1Assay Description:The RNA-dependent DNA polymerase (RDDP) activity associated with HIV-1 RT was measured by use of the Invitrogen EnzCheck Reverse Transcriptase Assay ...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein(HIV-1)
Birla Institute of Technology

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 5.00E+4nMpH: 7.8Assay Description:The RNase H activity associated with HIV-1 RT was measured in a 100 mL reactionvolume containing Tris HCl (pH 7.8, 50 mm), MgCl2 (6 mm), dithiothreit...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/24/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetGag-Pol polyprotein(HIV-1)
Birla Institute of Technology

LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 48nMAssay Description:The reaction mixture was set with template primer complex, RT enzyme and dNTPs in a lysis buffer with or without inhibitors. The reaction mixture was...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/20/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 20nMAssay Description:Inhibition of HIV1 reverse transcriptase assessed as reduction in biotin-dUTP incorporation using poly(rA)-oligo(dT) as template/primer and digoxigen...More data for this Ligand-Target Pair
In Depth
Date in BDB:
3/8/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 80nMAssay Description:Inhibition of wild type HIV1 reverse transcriptase assessed as reduction in enzyme activityMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 2.00E+4nMAssay Description:Inhibition of wild type HIV1 reverse transcriptase K103N mutant assessed as reduction in enzyme activityMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 400nMAssay Description:Inhibition of wild type HIV1 reverse transcriptase Y181I/Y181C mutant assessed as reduction in enzyme activityMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 120nMAssay Description:Inhibition of wild type HIV1 reverse transcriptase L100I mutant assessed as reduction in enzyme activityMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 400nMAssay Description:Inhibition of wild type HIV1 reverse transcriptase Y181I mutant assessed as reduction in enzyme activityMore data for this Ligand-Target Pair
In Depth
Date in BDB:
3/13/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 24nMAssay Description:Inhibition of wild type HIV1 p66/p51 reverse transcriptase by spectrofluorometryMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 22nMAssay Description:Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 pre-incubated with compound before enzyme addition using poly(rA) template and...More data for this Ligand-Target Pair
In Depth
Date in BDB:
4/7/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 280nMAssay Description:Inhibition of HIV1 reverse transcriptase Lys103Asn mutant-associated RNA-dependent DNA polymerase activity after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 12nMAssay Description:Inhibition of HIV1 reverse transcriptase-associated RNA-dependent DNA polymerase activity after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 680nMAssay Description:Inhibition of HIV1 reverse transcriptase Tyr181Cys mutant-associated RNA-dependent DNA polymerase activity after 30 minsMore data for this Ligand-Target Pair
In Depth
Date in BDB:
4/23/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 44nMAssay Description:Inhibition of HIV1 recombinant wild type reverse transcriptase p66/p51 assessed as reduction in biotin-labeled dUTP incorporation into DNA using poly...More data for this Ligand-Target Pair
In Depth
Date in BDB:
5/7/2016
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase(Human immunodeficiency virus type 1)
Shandong University

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 38nMAssay Description:Inhibition of HIV1 reverse transcriptaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
5/29/2017
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase/RNaseH(Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 47nMAssay Description:The compound was evaluated for the inhibition of HIV-1 reverse transcriptaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/1/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase/RNaseH(Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 47nMAssay Description:Tested for inhibitory concentration against HIV-1 non-nucleoside reverse transcriptaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/4/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase/RNaseH(Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 47nMAssay Description:Inhibition of the NNRTI HIV-1 enzyme by 50% using enzyme assay.More data for this Ligand-Target Pair
In Depth
Date in BDB:
10/4/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase/RNaseH(Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 47nMAssay Description:Inhibitory activity against HIV-1 reverse transcriptaseMore data for this Ligand-Target Pair
In Depth
Date in BDB:
10/4/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
TargetReverse transcriptase/RNaseH(Human immunodeficiency virus type 1)
Dupont Pharmaceuticals

Curated by ChEMBL
LigandPNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
Affinity DataIC50: 0.75nMAssay Description:Inhibitory concentration against wild-type reverse transcriptase of HIV-1More data for this Ligand-Target Pair
In Depth
Date in BDB:
11/30/2012
Entry Details Article
PubMedPDB3D3D Structure (crystal)
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Activity Spreadsheet -- ITC Data from BindingDB

Found 1 hit for monomerid = 2483   

CellReverse transcriptase (HIV-1 RT)(1-350)(Human immunodeficiency virus type 1)
Chulalongkorn University

SyringePNGBDBM2483(Sustiva | DMP-266 | (4S)-6-chloro-4-(2-cyclopropyl...)
ITC DataΔG°: -37.7kcal/mole −TΔS°: 19.7kcal/mole ΔH°: -57.3kcal/mole
T: 25.00°C