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There are 11 purchasable compounds for target: ACAT-related gene product 1

Wt: 428.4
BDBM20716
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Wt: 394.4
BDBM27947
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Wt: 420.5
BDBM27950
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Wt: 319.1
BDBM50003723
Purchase
Wt: 501.3
BDBM50314752
Purchase
Wt: 419.3
BDBM50341762
Purchase
Wt: 396.4
BDBM50355142
Purchase
Wt: 396.4
BDBM50362681
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Wt: 350.4
BDBM50394726
Purchase
Wt: 367.4
BDBM50399710
Purchase
Wt: 420.3
BDBM50442833
Purchase
Wt: 498.6
BDBM50020053
Purchase

Activity Spreadsheet -- Enzyme Inhibition Constant Data from BindingDB

Found 33 hits for monomerid = 20716,27947,27950,50003723,50314752,50341762,50355142,50362681,50394726,50399710,50442833,50020053   
Target
(Institution)
LigandTarget
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM20716
PNG
((1R,2R)-2-[(4-{4-[(phenylcarbamoyl)amino]phenyl}ph...)
Show SMILES OC(=O)[C@@H]1CCC[C@H]1C(=O)c1ccc(cc1)-c1ccc(NC(=O)Nc2ccccc2)cc1
Show InChI InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1
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n/an/a 7n/an/an/an/a7.522



Abbott Laboratories



Assay Description
DGAT-1 activity was characterized by catalyzing the transfer of the radiolabeled decanoyl group onto the syn-3 position of didecanoyl glycerol. The r...


J Med Chem 51: 380-3 (2008)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50399710
PNG
(CHEMBL2178953)
Show SMILES Cc1nc(C)c(nc1C(N)=O)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C21H25N3O3/c1-12-19(24-20(21(22)27)13(2)23-12)17-9-7-16(8-10-17)15-5-3-14(4-6-15)11-18(25)26/h7-10,14-15H,3-6,11H2,1-2H3,(H2,22,27)(H,25,26)/t14-,15-
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n/an/a 70n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of DGAT1 in human liver microsomes


J Med Chem 55: 10610-29 (2012)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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n/an/a 15n/an/an/an/a7.422



AstraZeneca



Assay Description
The assay mixture contains test compound, membrane protein, and 1,2 dioleoyl-sn-glycerol in a 96-deep well plate. The reaction was started by adding ...


J Med Chem 52: 1558-68 (2009)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50314752
PNG
(CHEMBL1092385 | N-[2-({[1-Phenyl-3-(trifluoromethy...)
Show SMILES FC(F)(F)COc1ccc(cn1)C(=O)NCCNC(=O)c1cn(nc1C(F)(F)F)-c1ccccc1
Show InChI InChI=1S/C21H17F6N5O3/c22-20(23,24)12-35-16-7-6-13(10-30-16)18(33)28-8-9-29-19(34)15-11-32(14-4-2-1-3-5-14)31-17(15)21(25,26)27/h1-7,10-11H,8-9,12H2,(H,28,33)(H,29,34)
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n/an/a 22n/an/an/an/an/an/a



Takeda Pharmaceutical Company Ltd

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 expressed in baculovirus infected Sf9 cells using [14C]oleoyl-CoA after 15 mins by TLC analysis


Bioorg Med Chem 18: 2785-95 (2010)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50341762
PNG
(2-Phenyl-5-trifluoromethyloxazole-4-carboxylic Aci...)
Show SMILES COCCN(C)c1ccc(NC(=O)c2nc(oc2C(F)(F)F)-c2ccccc2)cc1
Show InChI InChI=1S/C21H20F3N3O3/c1-27(12-13-29-2)16-10-8-15(9-11-16)25-19(28)17-18(21(22,23)24)30-20(26-17)14-6-4-3-5-7-14/h3-11H,12-13H2,1-2H3,(H,25,28)
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n/an/an/an/a 1.80E+3n/an/an/an/a



Hoffmann-La Roche Inc.

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay


J Med Chem 54: 2433-46 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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n/an/an/an/a 1.44E+3n/an/an/an/a



Hoffmann-La Roche Inc.

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 expressed in CHO-K1 cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay


J Med Chem 54: 2433-46 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50341762
PNG
(2-Phenyl-5-trifluoromethyloxazole-4-carboxylic Aci...)
Show SMILES COCCN(C)c1ccc(NC(=O)c2nc(oc2C(F)(F)F)-c2ccccc2)cc1
Show InChI InChI=1S/C21H20F3N3O3/c1-27(12-13-29-2)16-10-8-15(9-11-16)25-19(28)17-18(21(22,23)24)30-20(26-17)14-6-4-3-5-7-14/h3-11H,12-13H2,1-2H3,(H,25,28)
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n/an/a 325n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 expressed in baculovirus infected insect cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay


J Med Chem 54: 2433-46 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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n/an/a 113n/an/an/an/an/an/a



Hoffmann-La Roche Inc.

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 expressed in baculovirus infected insect cells after 1 hr using palmitoyl-1-14C-coenzyme A by phospholipid flashplate assay


J Med Chem 54: 2433-46 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM20716
PNG
((1R,2R)-2-[(4-{4-[(phenylcarbamoyl)amino]phenyl}ph...)
Show SMILES OC(=O)[C@@H]1CCC[C@H]1C(=O)c1ccc(cc1)-c1ccc(NC(=O)Nc2ccccc2)cc1
Show InChI InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1
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n/an/a 20n/an/an/an/an/an/a



Piramal Life Sciences Limited

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 assessed as formation of [14C]-triglyceride using [14C]oleoyl-CoA by liquid scintillation counting


Bioorg Med Chem Lett 21: 5812-7 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM20716
PNG
((1R,2R)-2-[(4-{4-[(phenylcarbamoyl)amino]phenyl}ph...)
Show SMILES OC(=O)[C@@H]1CCC[C@H]1C(=O)c1ccc(cc1)-c1ccc(NC(=O)Nc2ccccc2)cc1
Show InChI InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1
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n/an/a 20n/an/an/an/an/an/a



Piramal Life Sciences Limited

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 expressed in Sf9 cells assessed as formation of didecanoylglycerol product after 1 hr using 14C-decanoyl-CoA by beta scinti...


Bioorg Med Chem Lett 21: 5812-7 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50355142
PNG
(CHEMBL1835919)
Show SMILES Nc1ncnc2OCCN(c3ccc(cc3)[C@H]3CC[C@H](CC(O)=O)CC3)C(=O)c12
Show InChI InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
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n/an/a 19n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1


Bioorg Med Chem Lett 21: 6122-5 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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n/an/a 72n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1


Bioorg Med Chem Lett 21: 6122-5 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50355142
PNG
(CHEMBL1835919)
Show SMILES Nc1ncnc2OCCN(c3ccc(cc3)[C@H]3CC[C@H](CC(O)=O)CC3)C(=O)c12
Show InChI InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
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n/an/a 16n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay


Bioorg Med Chem Lett 21: 6122-5 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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n/an/a 8n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of human DGAT-1-mediated triglyceride synthesis in the HT-29 cells by whole cell assay


Bioorg Med Chem Lett 21: 6122-5 (2011)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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TBA

Assay Description
Inhibition of full length human microsomal DGAT-1 expressed in baculovirus infected insect Sf9 cells using [14C]decanoylCoA as substrate after 1.5 hr...


Citation and Details
More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50355142
PNG
(CHEMBL1835919)
Show SMILES Nc1ncnc2OCCN(c3ccc(cc3)[C@H]3CC[C@H](CC(O)=O)CC3)C(=O)c12
Show InChI InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
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TBA

Assay Description
Inhibition of full length human microsomal DGAT-1 expressed in baculovirus infected insect Sf9 cells using [14C]decanoylCoA as substrate after 1.5 hr...


Citation and Details
More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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TBA

Assay Description
Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting


Citation and Details
More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50355142
PNG
(CHEMBL1835919)
Show SMILES Nc1ncnc2OCCN(c3ccc(cc3)[C@H]3CC[C@H](CC(O)=O)CC3)C(=O)c12
Show InChI InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
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TBA

Assay Description
Inhibition of DGAT1-mediated triglyceride synthesis in human HT-29 cells using [3H]glycerol as substrate after 6 hrs by beta counting


Citation and Details
More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50362681
PNG
(CHEMBL1305904)
Show SMILES CC(Sc1nnc(-c2ccc(NC(=O)c3ccccc3C)cc2)n1C)C(O)=O
Show InChI InChI=1S/C20H20N4O3S/c1-12-6-4-5-7-16(12)18(25)21-15-10-8-14(9-11-15)17-22-23-20(24(17)3)28-13(2)19(26)27/h4-11,13H,1-3H3,(H,21,25)(H,26,27)
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n/an/a 1.98E+3n/an/an/an/an/an/a



Prosidion Ltd

Curated by ChEMBL


Assay Description
Inhibition of human recombinant N-terminus FLAG-tagged DGAT1 expressed in baculovirus infected insect Sf9 cells assessed as triglyceride synthesis


Bioorg Med Chem Lett 22: 824-8 (2012)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50394726
PNG
(CHEMBL2165819)
Show SMILES Nc1c(cnc2ccnn12)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C20H22N4O2/c21-20-17(12-22-18-9-10-23-24(18)20)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-19(25)26/h5-10,12-14H,1-4,11,21H2,(H,25,26)/t13-,14-
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n/an/a 78n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 expressed in human HeLa cells assessed as reduction in triglyceride synthesis


J Med Chem 55: 1751-7 (2012)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50394726
PNG
(CHEMBL2165819)
Show SMILES Nc1c(cnc2ccnn12)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C20H22N4O2/c21-20-17(12-22-18-9-10-23-24(18)20)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-19(25)26/h5-10,12-14H,1-4,11,21H2,(H,25,26)/t13-,14-
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n/an/a 8n/an/an/an/an/an/a



Abbott Laboratories

Curated by ChEMBL


Assay Description
Inhibition of N-terminal His6-tagged human recombinant DGAT1 expressed in insect cell membrane using [1-14C]decanoyl-CoA substrate by phospholipid fl...


J Med Chem 55: 1751-7 (2012)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50399710
PNG
(CHEMBL2178953)
Show SMILES Cc1nc(C)c(nc1C(N)=O)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C21H25N3O3/c1-12-19(24-20(21(22)27)13(2)23-12)17-9-7-16(8-10-17)15-5-3-14(4-6-15)11-18(25)26/h7-10,14-15H,3-6,11H2,1-2H3,(H2,22,27)(H,25,26)/t14-,15-
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n/an/a 10n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of DGAT1 in human adipose tissue assessed as reduction in triacylglycerol synthesis


J Med Chem 55: 10610-29 (2012)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50442833
PNG
(CHEMBL2441213)
Show SMILES COCCN(C)c1ccc(NC(=O)c2oc(nc2C(F)(F)F)-c2ccccc2)cn1
Show InChI InChI=1S/C20H19F3N4O3/c1-27(10-11-29-2)15-9-8-14(12-24-15)25-18(28)16-17(20(21,22)23)26-19(30-16)13-6-4-3-5-7-13/h3-9,12H,10-11H2,1-2H3,(H,25,28)
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n/an/a 85n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Inhibition of human DGAT-1 expressed in insect Sf9 cell microsomes using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-CoA as substrate after 2 hrs


Bioorg Med Chem Lett 23: 6410-4 (2013)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50355142
PNG
(CHEMBL1835919)
Show SMILES Nc1ncnc2OCCN(c3ccc(cc3)[C@H]3CC[C@H](CC(O)=O)CC3)C(=O)c12
Show InChI InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
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n/an/a 8n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of DGAT-1-mediated triglyceride synthesis in human HT-29 cells using [3H]-glycerol as substrate incubated for 1 hr prior to substrate addi...


Bioorg Med Chem 21: 5081-97 (2013)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50355142
PNG
(CHEMBL1835919)
Show SMILES Nc1ncnc2OCCN(c3ccc(cc3)[C@H]3CC[C@H](CC(O)=O)CC3)C(=O)c12
Show InChI InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
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n/an/a 19n/an/an/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Inhibition of human full length DGAT-1 expressed in insect sf9 cells using [14C]decanoylCoA as substrate after 1.5 hrs by scintillation spectrometry


Bioorg Med Chem 21: 5081-97 (2013)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50355142
PNG
(CHEMBL1835919)
Show SMILES Nc1ncnc2OCCN(c3ccc(cc3)[C@H]3CC[C@H](CC(O)=O)CC3)C(=O)c12
Show InChI InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
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n/an/a 90n/an/an/an/an/an/a



Korea Research Institute of Chemical Technology

Curated by ChEMBL


Assay Description
Inhibition of recombinant human DGAT-1 expressed in Hep3B cell lysate using didecanoyl glycerol and [14C]decanoyl-CoA as substrate after 60 mins by l...


Bioorg Med Chem Lett 23: 4713-8 (2013)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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n/an/a 6n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human liver flag-tagged DGAT1 expressed in baculovirus infected insect cells after 2 hrs by SPA


J Med Chem 57: 3464-83 (2014)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50003723
PNG
(CHEMBL3235289)
Show SMILES CC1Oc2ncnc(N)c2N=C1c1ccc(Br)cc1
Show InChI InChI=1S/C13H11BrN4O/c1-7-10(8-2-4-9(14)5-3-8)18-11-12(15)16-6-17-13(11)19-7/h2-7H,1H3,(H2,15,16,17)
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n/an/a 390n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of human liver flag-tagged DGAT1 expressed in baculovirus infected insect cells after 2 hrs by SPA


J Med Chem 57: 3464-83 (2014)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27947
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C22H26N4O3/c1-22(2)19(26-18-20(23)24-12-25-21(18)29-22)16-9-7-15(8-10-16)14-5-3-13(4-6-14)11-17(27)28/h7-10,12-14H,3-6,11H2,1-2H3,(H,27,28)(H2,23,24,25)/t13-,14-
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n/an/a 4n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Inhibition of DGAT1 (unknown origin) by cell-based assay


J Med Chem 57: 3464-83 (2014)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50020053
PNG
(CHEMBL3287867)
Show SMILES CCC1CN(C(=O)Nc2ccccc2)c2ccc(cc2O1)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C31H34N2O4/c1-2-27-20-33(31(36)32-26-6-4-3-5-7-26)28-17-16-25(19-29(28)37-27)24-14-12-23(13-15-24)22-10-8-21(9-11-22)18-30(34)35/h3-7,12-17,19,21-22,27H,2,8-11,18,20H2,1H3,(H,32,36)(H,34,35)/t21-,22-,27?
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n/an/a 110n/an/an/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Inhibition of human DGAT1 expressed in Sf9 insect cells using 1,2-dioleoyl-sn-glycerol and [14C]-palmitoyl-CoA substrate by scintillation counting an...


ACS Med Chem Lett 5: 544-9 (2014)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50399710
PNG
(CHEMBL2178953)
Show SMILES Cc1nc(C)c(nc1C(N)=O)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C21H25N3O3/c1-12-19(24-20(21(22)27)13(2)23-12)17-9-7-16(8-10-17)15-5-3-14(4-6-15)11-18(25)26/h7-10,14-15H,3-6,11H2,1-2H3,(H2,22,27)(H,25,26)/t14-,15-
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n/an/a 80n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of human recombinant DGAT1 expressed in Sf9 cells by liquid scintillography


J Med Chem 55: 10610-29 (2012)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM50399710
PNG
(CHEMBL2178953)
Show SMILES Cc1nc(C)c(nc1C(N)=O)-c1ccc(cc1)[C@H]1CC[C@H](CC(O)=O)CC1
Show InChI InChI=1S/C21H25N3O3/c1-12-19(24-20(21(22)27)13(2)23-12)17-9-7-16(8-10-17)15-5-3-14(4-6-15)11-18(25)26/h7-10,14-15H,3-6,11H2,1-2H3,(H2,22,27)(H,25,26)/t14-,15-
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n/an/a 10n/an/an/an/an/an/a



AstraZeneca

Curated by ChEMBL


Assay Description
Inhibition of DGAT1 in human HuTu80 cells


J Med Chem 55: 10610-29 (2012)

More data for this
Ligand-Target Pair
Diacylglycerol O-acyltransferase 1


(Homo sapiens (human))
BDBM27950
PNG
(2-[4-(4-{4-amino-7,7-dimethyl-7H-pyrimido[4,5-b][1...)
Show SMILES CC1(C)Oc2ncnc(N)c2N=C1c1ccc(cc1)C12CCC(CC(O)=O)(CC1)CC2
Show InChI InChI=1S/C24H28N4O3/c1-22(2)19(28-18-20(25)26-14-27-21(18)31-22)15-3-5-16(6-4-15)24-10-7-23(8-11-24,9-12-24)13-17(29)30/h3-6,14H,7-13H2,1-2H3,(H,29,30)(H2,25,26,27)
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n/an/a 15n/an/an/an/a7.422



AstraZeneca



Assay Description
The assay mixture contains test compound, membrane protein, and 1,2 dioleoyl-sn-glycerol in a 96-deep well plate. The reaction was started by adding ...


J Med Chem 52: 1558-68 (2009)

More data for this
Ligand-Target Pair