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Found 4 hits Enz. Inhib. hit(s) with Target = 'Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase' and Ligand = 'BDBM201278'   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kJ/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase


(Homo sapiens (Human))
BDBM201278
PNG
(US9187424, 42)
Show SMILES CCCCCc1ccc(cc1)C1(CC(=C(C#N)C(=O)N1)c1ccc(C)cc1)C(F)(F)F |t:14|
Show InChI InChI=1S/C25H25F3N2O/c1-3-4-5-6-18-9-13-20(14-10-18)24(25(26,27)28)15-21(22(16-29)23(31)30-24)19-11-7-17(2)8-12-19/h7-14H,3-6,15H2,1-2H3,(H,30,31)
PDB

UniProtKB/SwissProt

antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
US Patent
n/an/a 77n/an/an/an/a7.4n/a



Bristol-Myers Squibb Company

US Patent


Assay Description
The MGAT enzyme reactions were performed in CORNING Falcon 96-well Polypropylene plates, in a total volume of 60 uL of 50 mM Potassium Phosphate buff...


US Patent US9187424 (2015)


BindingDB Entry DOI: 10.7270/Q2FQ9VFG
More data for this
Ligand-Target Pair
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase


(Homo sapiens (Human))
BDBM201278
PNG
(US9187424, 42)
Show SMILES CCCCCc1ccc(cc1)C1(CC(=C(C#N)C(=O)N1)c1ccc(C)cc1)C(F)(F)F |t:14|
Show InChI InChI=1S/C25H25F3N2O/c1-3-4-5-6-18-9-13-20(14-10-18)24(25(26,27)28)15-21(22(16-29)23(31)30-24)19-11-7-17(2)8-12-19/h7-14H,3-6,15H2,1-2H3,(H,30,31)
PDB

UniProtKB/SwissProt

antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
Article
PubMed
n/an/a 77n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of human recombinant MGAT2 expressed in Sf9 cell membrane using 2-monooleglycerol and [H3]-oleoyl-CoA as substrates incubated for 20 mins ...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01356
BindingDB Entry DOI: 10.7270/Q2RF5ZVM
More data for this
Ligand-Target Pair
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase


(Mus musculus)
BDBM201278
PNG
(US9187424, 42)
Show SMILES CCCCCc1ccc(cc1)C1(CC(=C(C#N)C(=O)N1)c1ccc(C)cc1)C(F)(F)F |t:14|
Show InChI InChI=1S/C25H25F3N2O/c1-3-4-5-6-18-9-13-20(14-10-18)24(25(26,27)28)15-21(22(16-29)23(31)30-24)19-11-7-17(2)8-12-19/h7-14H,3-6,15H2,1-2H3,(H,30,31)
PDB

Reactome pathway
KEGG

UniProtKB/SwissProt

GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
Article
PubMed
n/an/a 275n/an/an/an/an/an/a


TBA

Assay Description
Inhibition of mouse recombinant MGAT2 expressed in Sf9 cell membrane using 2-oleoylglycerol and oleoyl-CoA as substrates incubated for 10 mins by LCM...


Citation and Details

Article DOI: 10.1021/acs.jmedchem.1c01356
BindingDB Entry DOI: 10.7270/Q2RF5ZVM
More data for this
Ligand-Target Pair
Alpha-1,6-mannosyl-glycoprotein 2-beta-N-acetylglucosaminyltransferase


(Homo sapiens (Human))
BDBM201278
PNG
(US9187424, 42)
Show SMILES CCCCCc1ccc(cc1)C1(CC(=C(C#N)C(=O)N1)c1ccc(C)cc1)C(F)(F)F |t:14|
Show InChI InChI=1S/C25H25F3N2O/c1-3-4-5-6-18-9-13-20(14-10-18)24(25(26,27)28)15-21(22(16-29)23(31)30-24)19-11-7-17(2)8-12-19/h7-14H,3-6,15H2,1-2H3,(H,30,31)
PDB

UniProtKB/SwissProt

antibodypedia
GoogleScholar
AffyNet 
PC cid
PC sid
UniChem
US Patent
n/an/a 403n/an/an/an/a7.425



Bristol-Myers Squibb Company

US Patent


Assay Description
MGAT2 enzyme was assayed using membranes isolated from Sf9 cells expressing the recombinant human MGAT2 cDNA with 2-monooleoylglycerol and [3H]-oleoy...


US Patent US9187424 (2015)


BindingDB Entry DOI: 10.7270/Q2FQ9VFG
More data for this
Ligand-Target Pair