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Compile Data Set for Download or QSAR

Found 1735 hits of ec50 for UniProtKB: Q8TDV5   
Target/Host
(Institution)		LigandTarget/Host
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
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50232631
PNG
(CHEMBL4104464)
Show SMILES Fc1cc(OCC[C@@H]2C[C@@H]2C2CCN(CC2)c2ncc(Cl)cn2)ccc1CC(=O)N1CCC1 |r|
Show InChI InChI=1S/C25H30ClFN4O2/c26-20-15-28-25(29-16-20)31-9-4-17(5-10-31)22-12-18(22)6-11-33-21-3-2-19(23(27)14-21)13-24(32)30-7-1-8-30/h2-3,14-18,22H,1,4-13H2/t18-,22-/m1/s1
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n/an/an/an/a 0.200n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay

Bioorg Med Chem Lett 27: 1124-1128 (2017)


Article DOI: 10.1016/j.bmcl.2017.01.091
BindingDB Entry DOI: 10.7270/Q2XK8HSD
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50232621
PNG
(CHEMBL4093284)
Show SMILES COCc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1cc(F)c(CC(=O)N2CCC2)c(F)c1 |r|
Show InChI InChI=1S/C27H34F2N4O3/c1-35-17-18-15-30-27(31-16-18)33-8-3-19(4-9-33)22-11-20(22)5-10-36-21-12-24(28)23(25(29)13-21)14-26(34)32-6-2-7-32/h12-13,15-16,19-20,22H,2-11,14,17H2,1H3/t20-,22-/m1/s1
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n/an/an/an/a 0.200n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay

Bioorg Med Chem Lett 27: 1124-1128 (2017)


Article DOI: 10.1016/j.bmcl.2017.01.091
BindingDB Entry DOI: 10.7270/Q2XK8HSD
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50342703
PNG
(CHEMBL1771104 | rac-4-(3-(2-(3-(1-(5-chloropyrimid...)
Show SMILES Fc1cc(OCCCC2CC2CCCC2CCN(CC2)c2ncc(Cl)cn2)ccc1C(=O)NC1CC1
Show InChI InChI=1S/C28H36ClFN4O2/c29-22-17-31-28(32-18-22)34-12-10-19(11-13-34)3-1-4-20-15-21(20)5-2-14-36-24-8-9-25(26(30)16-24)27(35)33-23-6-7-23/h8-9,16-21,23H,1-7,10-15H2,(H,33,35)
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n/an/an/an/a 0.200n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins ...

Bioorg Med Chem Lett 21: 2665-9 (2011)


Article DOI: 10.1016/j.bmcl.2010.12.086
BindingDB Entry DOI: 10.7270/Q2M61KJV
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50342697
PNG
((+)-trans-4-(2-(2-(1-(5-chloropyrimidin-2-yl)piper...)
Show SMILES Fc1cc(OCCC2CC2C2CCN(CC2)c2ncc(Cl)cn2)ccc1C(=O)NC1CC1
Show InChI InChI=1S/C24H28ClFN4O2/c25-17-13-27-24(28-14-17)30-8-5-15(6-9-30)21-11-16(21)7-10-32-19-3-4-20(22(26)12-19)23(31)29-18-1-2-18/h3-4,12-16,18,21H,1-2,5-11H2,(H,29,31)
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n/an/an/an/a 0.300n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins ...

Bioorg Med Chem Lett 21: 2665-9 (2011)


Article DOI: 10.1016/j.bmcl.2010.12.086
BindingDB Entry DOI: 10.7270/Q2M61KJV
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50342697
PNG
((+)-trans-4-(2-(2-(1-(5-chloropyrimidin-2-yl)piper...)
Show SMILES Fc1cc(OCCC2CC2C2CCN(CC2)c2ncc(Cl)cn2)ccc1C(=O)NC1CC1
Show InChI InChI=1S/C24H28ClFN4O2/c25-17-13-27-24(28-14-17)30-8-5-15(6-9-30)21-11-16(21)7-10-32-19-3-4-20(22(26)12-19)23(31)29-18-1-2-18/h3-4,12-16,18,21H,1-2,5-11H2,(H,29,31)
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n/an/an/an/a 0.300n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins ...

Bioorg Med Chem Lett 21: 2665-9 (2011)


Article DOI: 10.1016/j.bmcl.2010.12.086
BindingDB Entry DOI: 10.7270/Q2M61KJV
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50232627
PNG
(CHEMBL4098051)
Show SMILES CCc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(CC(=O)N2CCC2)c(F)c1 |r|
Show InChI InChI=1S/C27H35FN4O2/c1-2-19-17-29-27(30-18-19)32-11-6-20(7-12-32)24-14-21(24)8-13-34-23-5-4-22(25(28)16-23)15-26(33)31-9-3-10-31/h4-5,16-18,20-21,24H,2-3,6-15H2,1H3/t21-,24-/m1/s1
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n/an/an/an/a 0.400n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay

Bioorg Med Chem Lett 27: 1124-1128 (2017)


Article DOI: 10.1016/j.bmcl.2017.01.091
BindingDB Entry DOI: 10.7270/Q2XK8HSD
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50343443
PNG
(CHEMBL1773283 | tert-butyl 4-(1-(2-fluoro-4-(methy...)
Show SMILES CC(C)(C)OC(=O)N1CCC(CC1)Sc1ncnc2n(ncc12)-c1ccc(cc1F)S(C)(=O)=O
Show InChI InChI=1S/C22H26FN5O4S2/c1-22(2,3)32-21(29)27-9-7-14(8-10-27)33-20-16-12-26-28(19(16)24-13-25-20)18-6-5-15(11-17(18)23)34(4,30)31/h5-6,11-14H,7-10H2,1-4H3
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n/an/an/an/a 0.5n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 by melanophore assay

Bioorg Med Chem Lett 21: 3134-41 (2011)


Article DOI: 10.1016/j.bmcl.2011.03.007
BindingDB Entry DOI: 10.7270/Q24T6JQF
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50036640
PNG
(CHEMBL3354778)
Show SMILES CCOC(=O)[C@@]1(Cc2ccccc2)CCc2cnc3c(cnn3c12)-c1ccc(cc1)C(F)(F)F |r|
Show InChI InChI=1S/C26H22F3N3O2/c1-2-34-24(33)25(14-17-6-4-3-5-7-17)13-12-19-15-30-23-21(16-31-32(23)22(19)25)18-8-10-20(11-9-18)26(27,28)29/h3-11,15-16H,2,12-14H2,1H3/t25-/m1/s1
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n/an/an/an/a 0.5n/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method

Bioorg Med Chem Lett 24: 5478-83 (2015)


Article DOI: 10.1016/j.bmcl.2014.10.010
BindingDB Entry DOI: 10.7270/Q29C7019
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50343444
PNG
(CHEMBL1773292 | tert-butyl 4-(9-(2-fluoro-4-(methy...)
Show SMILES CC(C)(C)OC(=O)N1CCC(CC1)Oc1ncnc2n(-c3ccc(cc3F)S(C)(=O)=O)c(=O)[nH]c12 |(25.19,-11.96,;25.19,-13.5,;23.86,-14.27,;23.85,-12.72,;26.53,-14.27,;26.52,-15.81,;25.19,-16.58,;27.86,-16.58,;29.19,-15.81,;30.52,-16.58,;30.52,-18.12,;29.19,-18.9,;27.86,-18.12,;31.86,-18.88,;31.86,-20.42,;30.53,-21.19,;30.53,-22.74,;31.87,-23.51,;33.2,-22.74,;34.67,-23.22,;35.15,-24.68,;34.11,-25.82,;34.59,-27.29,;36.1,-27.61,;37.13,-26.45,;36.65,-24.99,;37.67,-23.85,;36.57,-29.07,;35.55,-30.22,;38.06,-28.66,;37.66,-30.15,;35.58,-21.96,;37.12,-21.96,;34.67,-20.71,;33.2,-21.19,)|
Show InChI InChI=1S/C22H26FN5O6S/c1-22(2,3)34-21(30)27-9-7-13(8-10-27)33-19-17-18(24-12-25-19)28(20(29)26-17)16-6-5-14(11-15(16)23)35(4,31)32/h5-6,11-13H,7-10H2,1-4H3,(H,26,29)
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n/an/an/an/a 0.600n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 by melanophore assay

Bioorg Med Chem Lett 21: 3134-41 (2011)


Article DOI: 10.1016/j.bmcl.2011.03.007
BindingDB Entry DOI: 10.7270/Q24T6JQF
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50204219
PNG
(CHEMBL3893596)
Show SMILES CC(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(C2)Oc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |r,@@:12,THB:14:12:6:8.9|
Show InChI InChI=1S/C22H26FN5O7S/c1-12(2)34-22(29)27-13-4-5-14(27)9-15(8-13)35-21-19(28(30)31)20(24-11-25-21)26-18-7-6-16(10-17(18)23)36(3,32)33/h6-7,10-15H,4-5,8-9H2,1-3H3,(H,24,25,26)/t13-,14-/m1/s1
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n/an/an/an/a 0.600n/an/an/an/a



Jiangxi University of Traditional Chinese Medicine

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay

Bioorg Med Chem 25: 254-260 (2017)


Article DOI: 10.1016/j.bmc.2016.10.030
BindingDB Entry DOI: 10.7270/Q2Z321MK
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50244791
PNG
((2-Fluoro-4-methanesulfonyl-phenyl)-{6-[4-(3-isopr...)
Show SMILES CC(C)c1nc([o+][n-]1)C1CCN(CC1)c1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O
Show InChI InChI=1S/C21H24FN7O5S/c1-12(2)18-26-21(34-27-18)13-6-8-28(9-7-13)20-17(29(30)31)19(23-11-24-20)25-16-5-4-14(10-15(16)22)35(3,32)33/h4-5,10-13H,6-9H2,1-3H3,(H,23,24,25)
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n/an/an/an/a 0.650n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 by melanophore assay

Bioorg Med Chem Lett 21: 3134-41 (2011)


Article DOI: 10.1016/j.bmcl.2011.03.007
BindingDB Entry DOI: 10.7270/Q24T6JQF
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50244791
PNG
((2-Fluoro-4-methanesulfonyl-phenyl)-{6-[4-(3-isopr...)
Show SMILES CC(C)c1nc([o+][n-]1)C1CCN(CC1)c1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O
Show InChI InChI=1S/C21H24FN7O5S/c1-12(2)18-26-21(34-27-18)13-6-8-28(9-7-13)20-17(29(30)31)19(23-11-24-20)25-16-5-4-14(10-15(16)22)35(3,32)33/h4-5,10-13H,6-9H2,1-3H3,(H,23,24,25)
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n/an/an/an/a 0.680n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at CPR119 (unknown origin) transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation

J Med Chem 51: 5172-5 (2008)


Article DOI: 10.1021/jm8006867
BindingDB Entry DOI: 10.7270/Q2KW5FVB
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50343445
PNG
(CHEMBL1773293 | tert-butyl 4-(3-(4-(methylsulfonyl...)
Show SMILES CC(C)(C)OC(=O)N1CCC(CC1)Oc1ncnc2c(noc12)-c1ccc(cc1)S(C)(=O)=O
Show InChI InChI=1S/C22H26N4O6S/c1-22(2,3)31-21(27)26-11-9-15(10-12-26)30-20-19-18(23-13-24-20)17(25-32-19)14-5-7-16(8-6-14)33(4,28)29/h5-8,13,15H,9-12H2,1-4H3
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n/an/an/an/a 0.700n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 by melanophore assay

Bioorg Med Chem Lett 21: 3134-41 (2011)


Article DOI: 10.1016/j.bmcl.2011.03.007
BindingDB Entry DOI: 10.7270/Q24T6JQF
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50232629
PNG
(CHEMBL4077033)
Show SMILES COCc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(CC(=O)N2CCC2)c(F)c1 |r|
Show InChI InChI=1S/C27H35FN4O3/c1-34-18-19-16-29-27(30-17-19)32-10-5-20(6-11-32)24-13-21(24)7-12-35-23-4-3-22(25(28)15-23)14-26(33)31-8-2-9-31/h3-4,15-17,20-21,24H,2,5-14,18H2,1H3/t21-,24-/m1/s1
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n/an/an/an/a 0.700n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay

Bioorg Med Chem Lett 27: 1124-1128 (2017)


Article DOI: 10.1016/j.bmcl.2017.01.091
BindingDB Entry DOI: 10.7270/Q2XK8HSD
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50232622
PNG
(CHEMBL4060838)
Show SMILES Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(CC(=O)N2CCC2)cc1 |r|
Show InChI InChI=1S/C25H31ClN4O2/c26-21-16-27-25(28-17-21)30-11-6-19(7-12-30)23-15-20(23)8-13-32-22-4-2-18(3-5-22)14-24(31)29-9-1-10-29/h2-5,16-17,19-20,23H,1,6-15H2/t20-,23-/m1/s1
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n/an/an/an/a 0.800n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay

Bioorg Med Chem Lett 27: 1124-1128 (2017)


Article DOI: 10.1016/j.bmcl.2017.01.091
BindingDB Entry DOI: 10.7270/Q2XK8HSD
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50122947
PNG
(CHEMBL3622182)
Show SMILES CCS(=O)(=O)c1ccc(COC[C@@H]2C[C@@H]2C2CCN(CC2)c2nc(no2)C(C)C)c(F)c1 |r|
Show InChI InChI=1S/C23H32FN3O4S/c1-4-32(28,29)19-6-5-17(21(24)12-19)13-30-14-18-11-20(18)16-7-9-27(10-8-16)23-25-22(15(2)3)26-31-23/h5-6,12,15-16,18,20H,4,7-11,13-14H2,1-3H3/t18-,20+/m0/s1
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n/an/an/an/a 0.800n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells by cAMP assay

ACS Med Chem Lett 6: 936-41 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00207
BindingDB Entry DOI: 10.7270/Q2BK1F5K
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50232625
PNG
(CHEMBL4080222)
Show SMILES OC1CN(C1)C(=O)Cc1ccc(OCC[C@@H]2C[C@@H]2C2CCN(CC2)c2ncc(Cl)cn2)cc1F |r|
Show InChI InChI=1S/C25H30ClFN4O3/c26-19-12-28-25(29-13-19)30-6-3-16(4-7-30)22-9-17(22)5-8-34-21-2-1-18(23(27)11-21)10-24(33)31-14-20(32)15-31/h1-2,11-13,16-17,20,22,32H,3-10,14-15H2/t17-,22-/m1/s1
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n/an/an/an/a 0.800n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay

Bioorg Med Chem Lett 27: 1124-1128 (2017)


Article DOI: 10.1016/j.bmcl.2017.01.091
BindingDB Entry DOI: 10.7270/Q2XK8HSD
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50343446
PNG
(CHEMBL1775178 | tert-butyl 4-(1-(2-fluoro-4-(methy...)
Show SMILES CC(C)(C)OC(=O)N1CCC(CC1)Oc1ncnc2n(ncc12)-c1ccc(cc1F)S(C)(=O)=O
Show InChI InChI=1S/C22H26FN5O5S/c1-22(2,3)33-21(29)27-9-7-14(8-10-27)32-20-16-12-26-28(19(16)24-13-25-20)18-6-5-15(11-17(18)23)34(4,30)31/h5-6,11-14H,7-10H2,1-4H3
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n/an/an/an/a 0.900n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 by melanophore assay

Bioorg Med Chem Lett 21: 3134-41 (2011)


Article DOI: 10.1016/j.bmcl.2011.03.007
BindingDB Entry DOI: 10.7270/Q24T6JQF
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50036636
PNG
(CHEMBL3354774)
Show SMILES CCOC(=O)[C@](C)(Cc1ccccc1)c1c(C)cnc2c(cnn12)-c1ccc(cc1)C(F)(F)F |r|
Show InChI InChI=1S/C26H24F3N3O2/c1-4-34-24(33)25(3,14-18-8-6-5-7-9-18)22-17(2)15-30-23-21(16-31-32(22)23)19-10-12-20(13-11-19)26(27,28)29/h5-13,15-16H,4,14H2,1-3H3/t25-/m1/s1
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n/an/an/an/a 1n/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method

Bioorg Med Chem Lett 24: 5478-83 (2015)


Article DOI: 10.1016/j.bmcl.2014.10.010
BindingDB Entry DOI: 10.7270/Q29C7019
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50013912
PNG
(CHEMBL3260536)
Show SMILES COCCN(C)C(=O)C(C)(Cc1ccccc1)c1ccnc2c(cnn12)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C27H27F3N4O2/c1-26(17-19-7-5-4-6-8-19,25(35)33(2)15-16-36-3)23-13-14-31-24-22(18-32-34(23)24)20-9-11-21(12-10-20)27(28,29)30/h4-14,18H,15-17H2,1-3H3
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n/an/an/an/a 1n/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 overexpressed in CHO cells assessed as stimulation of cAMP production by HTRF assay

Bioorg Med Chem Lett 24: 2383-7 (2014)


Article DOI: 10.1016/j.bmcl.2014.03.023
BindingDB Entry DOI: 10.7270/Q2KP83P1
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50342680
PNG
(CHEMBL1771081 | tert-butyl 1'-(2-cyano-6-methylpyr...)
Show SMILES Cc1cc(nc(n1)C#N)N1CCC(CC1)C1CCN(CC1)C(=O)OC(C)(C)C
Show InChI InChI=1S/C21H31N5O2/c1-15-13-19(24-18(14-22)23-15)25-9-5-16(6-10-25)17-7-11-26(12-8-17)20(27)28-21(2,3)4/h13,16-17H,5-12H2,1-4H3
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n/an/an/an/a 1n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins ...

Bioorg Med Chem Lett 21: 2665-9 (2011)


Article DOI: 10.1016/j.bmcl.2010.12.086
BindingDB Entry DOI: 10.7270/Q2M61KJV
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50122756
PNG
(CHEMBL3622179)
Show SMILES COCc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1COCc1ccc(c(F)c1)-n1cnnn1 |r|
Show InChI InChI=1S/C23H28FN7O2/c1-32-12-17-10-25-23(26-11-17)30-6-4-18(5-7-30)20-9-19(20)14-33-13-16-2-3-22(21(24)8-16)31-15-27-28-29-31/h2-3,8,10-11,15,18-20H,4-7,9,12-14H2,1H3/t19-,20+/m0/s1
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n/an/an/an/a 1.10n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells by cAMP assay

ACS Med Chem Lett 6: 936-41 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00207
BindingDB Entry DOI: 10.7270/Q2BK1F5K
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50343447
PNG
(CHEMBL1775169 | tert-butyl 4-(1-(4-(methylsulfonyl...)
Show SMILES CC(C)(C)OC(=O)N1CCC(CC1)Oc1ncnc2n(ncc12)-c1ccc(cc1)S(C)(=O)=O
Show InChI InChI=1S/C22H27N5O5S/c1-22(2,3)32-21(28)26-11-9-16(10-12-26)31-20-18-13-25-27(19(18)23-14-24-20)15-5-7-17(8-6-15)33(4,29)30/h5-8,13-14,16H,9-12H2,1-4H3
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n/an/an/an/a 1.10n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 by melanophore assay

Bioorg Med Chem Lett 21: 3134-41 (2011)


Article DOI: 10.1016/j.bmcl.2011.03.007
BindingDB Entry DOI: 10.7270/Q24T6JQF
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50106208
PNG
(CHEMBL3598101)
Show SMILES CS(=O)(=O)c1cnc(O[C@H]2CC[C@@H](CC2)OC2CCN(CC2)C(=O)OC(C(F)(F)F)C(F)(F)F)cn1 |r,wU:9.8,wD:12.15,(9.06,2.18,;8,1.56,;9.07,.95,;7.99,2.79,;6.67,.78,;6.67,-.76,;5.34,-1.53,;4,-.77,;2.67,-1.54,;1.33,-.77,;,-1.54,;-1.33,-.77,;-1.33,.77,;,1.54,;1.33,.77,;-2.67,1.54,;-2.66,3.08,;-4,3.86,;-3.99,5.4,;-2.65,6.16,;-1.32,5.39,;-1.33,3.85,;-2.65,7.7,;-3.71,8.33,;-1.31,8.47,;-1.3,10.01,;.04,10.77,;.05,12.01,;1.1,10.15,;1.11,11.38,;-2.63,10.78,;-3.7,10.17,;-2.63,12.02,;-3.7,11.4,;4,.77,;5.33,1.55,)|
Show InChI InChI=1S/C20H25F6N3O6S/c1-36(31,32)16-11-27-15(10-28-16)34-13-4-2-12(3-5-13)33-14-6-8-29(9-7-14)18(30)35-17(19(21,22)23)20(24,25)26/h10-14,17H,2-9H2,1H3/t12-,13-
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n/an/an/an/a 1.20n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 by HTRF cAMP assay

Bioorg Med Chem Lett 25: 3034-8 (2015)


Article DOI: 10.1016/j.bmcl.2015.04.102
BindingDB Entry DOI: 10.7270/Q2SB47JS
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50240387
PNG
(CHEMBL4098760)
Show SMILES [H][C@@]12CC[C@]([H])(C[C@@H]1Oc1ncnc(Nc3ccc(cc3F)S(C)(=O)=O)c1[N+]([O-])=O)N(C2)C(=O)OC(C)(C)C |r,TLB:8:7:3.2:31.30,THB:32:30:7.6:3.2|
Show InChI InChI=1S/C23H28FN5O7S/c1-23(2,3)36-22(30)28-11-13-5-6-14(28)9-18(13)35-21-19(29(31)32)20(25-12-26-21)27-17-8-7-15(10-16(17)24)37(4,33)34/h7-8,10,12-14,18H,5-6,9,11H2,1-4H3,(H,25,26,27)/t13-,14+,18-/m0/s1
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n/an/an/an/a 1.20n/an/an/an/a



Jiangxi University of Traditional Chinese Medicine

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay

Bioorg Med Chem Lett 27: 2515-2519 (2017)


Article DOI: 10.1016/j.bmcl.2017.03.092
BindingDB Entry DOI: 10.7270/Q2HH6N7Q
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50204225
PNG
(CHEMBL3912040)
Show SMILES CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(C2)Nc1ncnc(Nc2ccc(cc2F)C#N)c1[N+]([O-])=O |r,@@:13,THB:15:13:7:9.10,5:7:9.10:14.13.12|
Show InChI InChI=1S/C23H26FN7O4/c1-23(2,3)35-22(32)30-15-5-6-16(30)10-14(9-15)28-20-19(31(33)34)21(27-12-26-20)29-18-7-4-13(11-25)8-17(18)24/h4,7-8,12,14-16H,5-6,9-10H2,1-3H3,(H2,26,27,28,29)/t15-,16-/m1/s1
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n/an/an/an/a 1.30n/an/an/an/a



Jiangxi University of Traditional Chinese Medicine

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay

Bioorg Med Chem 25: 254-260 (2017)


Article DOI: 10.1016/j.bmc.2016.10.030
BindingDB Entry DOI: 10.7270/Q2Z321MK
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50204229
PNG
(CHEMBL3982536)
Show SMILES CCOC(=O)N1[C@@H]2CC[C@@H]1CC(C2)Oc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |r,@@:11,THB:13:11:5:7.8|
Show InChI InChI=1S/C21H24FN5O7S/c1-3-33-21(28)26-12-4-5-13(26)9-14(8-12)34-20-18(27(29)30)19(23-11-24-20)25-17-7-6-15(10-16(17)22)35(2,31)32/h6-7,10-14H,3-5,8-9H2,1-2H3,(H,23,24,25)/t12-,13-/m1/s1
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n/an/an/an/a 1.40n/an/an/an/a



Jiangxi University of Traditional Chinese Medicine

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay

Bioorg Med Chem 25: 254-260 (2017)


Article DOI: 10.1016/j.bmc.2016.10.030
BindingDB Entry DOI: 10.7270/Q2Z321MK
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50427059
PNG
(CHEMBL2322837)
Show SMILES CC(C)(C)OC(=O)N1[C@H]2CC[C@H]1CC(C2)Oc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |r,TLB:15:13:7:9.10|
Show InChI InChI=1S/C23H28FN5O7S/c1-23(2,3)36-22(30)28-13-5-6-14(28)10-15(9-13)35-21-19(29(31)32)20(25-12-26-21)27-18-8-7-16(11-17(18)24)37(4,33)34/h7-8,11-15H,5-6,9-10H2,1-4H3,(H,25,26,27)/t13-,14-/m0/s1
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n/an/an/an/a 1.40n/an/an/an/a



College of Pharmacy of Kangwon National University

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine

Bioorg Med Chem Lett 23: 1519-21 (2013)


Article DOI: 10.1016/j.bmcl.2012.12.011
BindingDB Entry DOI: 10.7270/Q2SQ91Q7
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50427063
PNG
(CHEMBL2322841)
Show SMILES CC(C)(C)OC(=O)N1[C@H]2CC[C@H]1CC(C2)Nc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |r,THB:15:13:7:9.10|
Show InChI InChI=1S/C23H29FN6O6S/c1-23(2,3)36-22(31)29-14-5-6-15(29)10-13(9-14)27-20-19(30(32)33)21(26-12-25-20)28-18-8-7-16(11-17(18)24)37(4,34)35/h7-8,11-15H,5-6,9-10H2,1-4H3,(H2,25,26,27,28)/t14-,15-/m0/s1
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n/an/an/an/a 1.5n/an/an/an/a



College of Pharmacy of Kangwon National University

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine

Bioorg Med Chem Lett 23: 1519-21 (2013)


Article DOI: 10.1016/j.bmcl.2012.12.011
BindingDB Entry DOI: 10.7270/Q2SQ91Q7
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50122933
PNG
(CHEMBL3622166)
Show SMILES CCc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1COCc1ccc(cn1)S(C)(=O)=O |r|
Show InChI InChI=1S/C22H30N4O3S/c1-3-16-11-24-22(25-12-16)26-8-6-17(7-9-26)21-10-18(21)14-29-15-19-4-5-20(13-23-19)30(2,27)28/h4-5,11-13,17-18,21H,3,6-10,14-15H2,1-2H3/t18-,21+/m0/s1
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n/an/an/an/a 1.5n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells by cAMP assay

ACS Med Chem Lett 6: 936-41 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00207
BindingDB Entry DOI: 10.7270/Q2BK1F5K
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50427059
PNG
(CHEMBL2322837)
Show SMILES CC(C)(C)OC(=O)N1[C@H]2CC[C@H]1CC(C2)Oc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |r,TLB:15:13:7:9.10|
Show InChI InChI=1S/C23H28FN5O7S/c1-23(2,3)36-22(30)28-13-5-6-14(28)10-15(9-13)35-21-19(29(31)32)20(25-12-26-21)27-18-8-7-16(11-17(18)24)37(4,33)34/h7-8,11-15H,5-6,9-10H2,1-4H3,(H,25,26,27)/t13-,14-/m0/s1
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n/an/an/an/a 1.5n/an/an/an/a



College of Pharmacy of Kangwon National University

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 transfected in HEK293 cells assessed as concentration for 50 % cAMP stimulation of oleylethanolamine

Bioorg Med Chem Lett 23: 1519-21 (2013)


Article DOI: 10.1016/j.bmcl.2012.12.011
BindingDB Entry DOI: 10.7270/Q2SQ91Q7
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50204231
PNG
(CHEMBL3951013)
Show SMILES CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(C2)Oc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |r,@@:13,THB:15:13:7:9.10|
Show InChI InChI=1S/C23H28FN5O7S/c1-23(2,3)36-22(30)28-13-5-6-14(28)10-15(9-13)35-21-19(29(31)32)20(25-12-26-21)27-18-8-7-16(11-17(18)24)37(4,33)34/h7-8,11-15H,5-6,9-10H2,1-4H3,(H,25,26,27)/t13-,14-/m1/s1
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n/an/an/an/a 1.5n/an/an/an/a



Jiangxi University of Traditional Chinese Medicine

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay

Bioorg Med Chem 25: 254-260 (2017)


Article DOI: 10.1016/j.bmc.2016.10.030
BindingDB Entry DOI: 10.7270/Q2Z321MK
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50244681
PNG
(CHEMBL518819 | {6-[4-(3-tert-Butyl-[1,2,4]oxadiazo...)
Show SMILES CC(C)(C)c1nc([o+][n-]1)C1CCN(CC1)c1ncnc(Nc2ccc(cc2)S(C)(=O)=O)c1[N+]([O-])=O
Show InChI InChI=1S/C22H27N7O5S/c1-22(2,3)21-26-20(34-27-21)14-9-11-28(12-10-14)19-17(29(30)31)18(23-13-24-19)25-15-5-7-16(8-6-15)35(4,32)33/h5-8,13-14H,9-12H2,1-4H3,(H,23,24,25)
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n/an/an/an/a 1.5n/an/an/an/a



Arena Pharmaceuticals

Curated by ChEMBL


Assay Description
Agonist activity at CPR119 (unknown origin) transfected in Xenopus dermal melanophore assessed as dispersion of melatonin-induced pigmentation

J Med Chem 51: 5172-5 (2008)


Article DOI: 10.1021/jm8006867
BindingDB Entry DOI: 10.7270/Q2KW5FVB
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50204226
PNG
(CHEMBL3914281)
Show SMILES CC(C)(C)OC(=O)N1[C@@H]2CC[C@@H]1CC(C2)Nc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |r,@@:13,THB:15:13:7:9.10|
Show InChI InChI=1S/C23H29FN6O6S/c1-23(2,3)36-22(31)29-14-5-6-15(29)10-13(9-14)27-20-19(30(32)33)21(26-12-25-20)28-18-8-7-16(11-17(18)24)37(4,34)35/h7-8,11-15H,5-6,9-10H2,1-4H3,(H2,25,26,27,28)/t14-,15-/m1/s1
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n/an/an/an/a 1.5n/an/an/an/a



Jiangxi University of Traditional Chinese Medicine

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay

Bioorg Med Chem 25: 254-260 (2017)


Article DOI: 10.1016/j.bmc.2016.10.030
BindingDB Entry DOI: 10.7270/Q2Z321MK
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50232626
PNG
(CHEMBL4070965)
Show SMILES Fc1cc(OCC[C@@H]2C[C@@H]2C2CCN(CC2)c2ncc(Cl)cn2)ccc1CC(=O)N1CCCCC1 |r|
Show InChI InChI=1S/C27H34ClFN4O2/c28-22-17-30-27(31-18-22)33-11-6-19(7-12-33)24-14-20(24)8-13-35-23-5-4-21(25(29)16-23)15-26(34)32-9-2-1-3-10-32/h4-5,16-20,24H,1-3,6-15H2/t20-,24-/m1/s1
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n/an/an/an/a 1.5n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay

Bioorg Med Chem Lett 27: 1124-1128 (2017)


Article DOI: 10.1016/j.bmcl.2017.01.091
BindingDB Entry DOI: 10.7270/Q2XK8HSD
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50204223
PNG
(CHEMBL3904015)
Show SMILES CS(=O)(=O)N1[C@@H]2CC[C@@H]1CC(C2)Oc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |r,@@:10,THB:1:4:6.7:11.10.9,12:10:4:6.7|
Show InChI InChI=1S/C19H22FN5O7S2/c1-33(28,29)14-5-6-16(15(20)9-14)23-18-17(25(26)27)19(22-10-21-18)32-13-7-11-3-4-12(8-13)24(11)34(2,30)31/h5-6,9-13H,3-4,7-8H2,1-2H3,(H,21,22,23)/t11-,12-/m1/s1
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n/an/an/an/a 1.60n/an/an/an/a



Jiangxi University of Traditional Chinese Medicine

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as stimulation of cAMP level measured after 60 mins by HTRF assay

Bioorg Med Chem 25: 254-260 (2017)


Article DOI: 10.1016/j.bmc.2016.10.030
BindingDB Entry DOI: 10.7270/Q2Z321MK
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50540315
PNG
(CHEMBL4639701)
Show SMILES CC(C)c1noc(n1)C1CCN(CC1)c1ccc(cn1)-c1cc(C)c(cc1C#N)C#N
Show InChI InChI=1S/C24H24N6O/c1-15(2)23-28-24(31-29-23)17-6-8-30(9-7-17)22-5-4-18(14-27-22)21-10-16(3)19(12-25)11-20(21)13-26/h4-5,10-11,14-15,17H,6-9H2,1-3H3
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n/an/an/an/a 1.70n/an/an/an/a



Pfizer Inc.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells preincubated for 30 mins followed by d2 cAMP addition and measured after 60 mins by HTRF a...

J Med Chem 63: 6387-6406 (2020)


Article DOI: 10.1021/acs.jmedchem.9b01840
BindingDB Entry DOI: 10.7270/Q2X06BK1
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50122931
PNG
(CHEMBL3622168)
Show SMILES CC(C)c1noc(n1)N1CCC(CC1)[C@H]1C[C@H]1COCc1ccc(cc1F)-n1cnnn1 |r|
Show InChI InChI=1S/C22H28FN7O2/c1-14(2)21-25-22(32-26-21)29-7-5-15(6-8-29)19-9-17(19)12-31-11-16-3-4-18(10-20(16)23)30-13-24-27-28-30/h3-4,10,13-15,17,19H,5-9,11-12H2,1-2H3/t17-,19+/m0/s1
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n/an/an/an/a 1.70n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells by cAMP assay

ACS Med Chem Lett 6: 936-41 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00207
BindingDB Entry DOI: 10.7270/Q2BK1F5K
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50122870
PNG
(CHEMBL3622171)
Show SMILES CCOc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1COCc1ccc(c(F)c1)S(C)(=O)=O |r|
Show InChI InChI=1S/C23H30FN3O4S/c1-3-31-19-12-25-23(26-13-19)27-8-6-17(7-9-27)20-11-18(20)15-30-14-16-4-5-22(21(24)10-16)32(2,28)29/h4-5,10,12-13,17-18,20H,3,6-9,11,14-15H2,1-2H3/t18-,20+/m0/s1
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n/an/an/an/a 1.70n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells by cAMP assay

ACS Med Chem Lett 6: 936-41 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00207
BindingDB Entry DOI: 10.7270/Q2BK1F5K
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50122936
PNG
(CHEMBL3622181)
Show SMILES CCS(=O)(=O)c1ccc(OCC[C@@H]2C[C@@H]2C2CCN(CC2)c2nc(no2)C(C)C)c(F)c1 |r|
Show InChI InChI=1S/C23H32FN3O4S/c1-4-32(28,29)18-5-6-21(20(24)14-18)30-12-9-17-13-19(17)16-7-10-27(11-8-16)23-25-22(15(2)3)26-31-23/h5-6,14-17,19H,4,7-13H2,1-3H3/t17-,19-/m1/s1
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n/an/an/an/a 1.70n/an/an/an/a



Merck Research Laboratories

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells by cAMP assay

ACS Med Chem Lett 6: 936-41 (2015)


Article DOI: 10.1021/acsmedchemlett.5b00207
BindingDB Entry DOI: 10.7270/Q2BK1F5K
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50232632
PNG
(CHEMBL4083676)
Show SMILES Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(CC(=O)NC2CC2)cc1 |r|
Show InChI InChI=1S/C25H31ClN4O2/c26-20-15-27-25(28-16-20)30-10-7-18(8-11-30)23-14-19(23)9-12-32-22-5-1-17(2-6-22)13-24(31)29-21-3-4-21/h1-2,5-6,15-16,18-19,21,23H,3-4,7-14H2,(H,29,31)/t19-,23-/m1/s1
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n/an/an/an/a 1.80n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in intracellular cAMP level after 60 mins by HTRF assay

Bioorg Med Chem Lett 27: 1124-1128 (2017)


Article DOI: 10.1016/j.bmcl.2017.01.091
BindingDB Entry DOI: 10.7270/Q2XK8HSD
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50240388
PNG
(CHEMBL4078300)
Show SMILES CC(C)(C)OC(=O)N1CC2CCC1CC2Nc1ncnc(Nc2ccc(cc2F)S(C)(=O)=O)c1[N+]([O-])=O |THB:5:7:10.11:14.13,15:14:10.11:8.7|
Show InChI InChI=1S/C23H29FN6O6S/c1-23(2,3)36-22(31)29-11-13-5-6-14(29)9-18(13)28-21-19(30(32)33)20(25-12-26-21)27-17-8-7-15(10-16(17)24)37(4,34)35/h7-8,10,12-14,18H,5-6,9,11H2,1-4H3,(H2,25,26,27,28)
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n/an/an/an/a 1.80n/an/an/an/a



Jiangxi University of Traditional Chinese Medicine

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in HEK293 cells assessed as increase in cAMP stimulation measured after 60 mins by TR-FRET assay

Bioorg Med Chem Lett 27: 2515-2519 (2017)


Article DOI: 10.1016/j.bmcl.2017.03.092
BindingDB Entry DOI: 10.7270/Q2HH6N7Q
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50342701
PNG
(2-(4-((1R,2S)-2-(2-(5-(1H-1,2,3-triazol-1-yl)pyrid...)
Show SMILES Clc1cnc(nc1)N1CCC(CC1)[C@H]1C[C@H]1CCOc1ccc(cn1)-n1ccnn1 |r|
Show InChI InChI=1S/C21H24ClN7O/c22-17-12-24-21(25-13-17)28-7-3-15(4-8-28)19-11-16(19)5-10-30-20-2-1-18(14-23-20)29-9-6-26-27-29/h1-2,6,9,12-16,19H,3-5,7-8,10-11H2/t16-,19-/m1/s1
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n/an/an/an/a 2n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins ...

Bioorg Med Chem Lett 21: 2665-9 (2011)


Article DOI: 10.1016/j.bmcl.2010.12.086
BindingDB Entry DOI: 10.7270/Q2M61KJV
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM254730
PNG
(US9469631, 40)
Show SMILES CC(C)(C)OC(=O)N1CC[C@@H]([C@H](F)C1)N(C1CC1)C(=O)c1ccc(cc1)-c1cnco1 |r|
Show InChI InChI=1S/C23H28FN3O4/c1-23(2,3)31-22(29)26-11-10-19(18(24)13-26)27(17-8-9-17)21(28)16-6-4-15(5-7-16)20-12-25-14-30-20/h4-7,12,14,17-19H,8-11,13H2,1-3H3/t18-,19+/m1/s1
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n/an/an/an/a 2n/an/a7.437



Boehringer Ingelheim International GmbH

US Patent


Assay Description
MIN6 cells [Miyazaki J et al. Endocrinology. 1990 July; 127(1):126-32] are stably transfected with an expression vector for human GPR119 cDNA (Acc. N...

US Patent US9469631 (2016)


BindingDB Entry DOI: 10.7270/Q2V40T4G
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50036671
PNG
(CHEMBL3354804)
Show SMILES OCc1nn2c3c(CN[C@]3(Cc3cccc(F)c3)C3CC3)cnc2c1-c1ccc(cc1)C(F)(F)F |r|
Show InChI InChI=1S/C26H22F4N4O/c27-20-3-1-2-15(10-20)11-25(18-8-9-18)23-17(13-32-25)12-31-24-22(21(14-35)33-34(23)24)16-4-6-19(7-5-16)26(28,29)30/h1-7,10,12,18,32,35H,8-9,11,13-14H2/t25-/m1/s1
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n/an/an/an/a 2n/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method

Bioorg Med Chem Lett 24: 5478-83 (2015)


Article DOI: 10.1016/j.bmcl.2014.10.010
BindingDB Entry DOI: 10.7270/Q29C7019
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50036667
PNG
(CHEMBL3354798)
Show SMILES COC(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(c(CO)nn3c12)-c1ccc(cc1)C(F)(F)F |r|
Show InChI InChI=1S/C25H20F4N4O3/c1-36-23(35)24(10-14-3-2-4-18(26)9-14)21-16(12-31-24)11-30-22-20(19(13-34)32-33(21)22)15-5-7-17(8-6-15)25(27,28)29/h2-9,11,31,34H,10,12-13H2,1H3/t24-/m0/s1
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n/an/an/an/a 2n/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method

Bioorg Med Chem Lett 24: 5478-83 (2015)


Article DOI: 10.1016/j.bmcl.2014.10.010
BindingDB Entry DOI: 10.7270/Q29C7019
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50036664
PNG
(CHEMBL3354795)
Show SMILES COCCN(C)C(=O)[C@@]1(Cc2cccc(F)c2)NCc2cnc3c(cnn3c12)-c1ccc(cc1)C(F)(F)F |r|
Show InChI InChI=1S/C27H25F4N5O2/c1-35(10-11-38-2)25(37)26(13-17-4-3-5-21(28)12-17)23-19(15-33-26)14-32-24-22(16-34-36(23)24)18-6-8-20(9-7-18)27(29,30)31/h3-9,12,14,16,33H,10-11,13,15H2,1-2H3/t26-/m0/s1
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n/an/an/an/a 2n/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method

Bioorg Med Chem Lett 24: 5478-83 (2015)


Article DOI: 10.1016/j.bmcl.2014.10.010
BindingDB Entry DOI: 10.7270/Q29C7019
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50036642
PNG
(CHEMBL3354779)
Show SMILES COC(=O)C1(Cc2ccccc2)CCc2cnc3c(cnn3c12)-c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C25H20F3N3O2/c1-33-23(32)24(13-16-5-3-2-4-6-16)12-11-18-14-29-22-20(15-30-31(22)21(18)24)17-7-9-19(10-8-17)25(26,27)28/h2-10,14-15H,11-13H2,1H3
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n/an/an/an/a 2n/an/an/an/a



Genomics Institute of the Novartis Research Foundation

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 overexpressed in CHO cells assessed as increase in cellular cAMP production by HTRF method

Bioorg Med Chem Lett 24: 5478-83 (2015)


Article DOI: 10.1016/j.bmcl.2014.10.010
BindingDB Entry DOI: 10.7270/Q29C7019
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50342692
PNG
(4-(1'-(5-chloropyrimidin-2-yl)-4,4'-bipiperidin-1-...)
Show SMILES Cc1cc(nc(n1)C#N)N1CCC(CC1)C1CCN(CC1)c1ncc(Cl)cn1
Show InChI InChI=1S/C20H24ClN7/c1-14-10-19(26-18(11-22)25-14)27-6-2-15(3-7-27)16-4-8-28(9-5-16)20-23-12-17(21)13-24-20/h10,12-13,15-16H,2-9H2,1H3
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n/an/an/an/a 2n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins ...

Bioorg Med Chem Lett 21: 2665-9 (2011)


Article DOI: 10.1016/j.bmcl.2010.12.086
BindingDB Entry DOI: 10.7270/Q2M61KJV
More data for this
Ligand-Target Pair
Glucose-dependent insulinotropic receptor


(Homo sapiens (Human))		BDBM50342681
PNG
(CHEMBL1771082 | tert-butyl 1'-(6-cyano-2-methylpyr...)
Show SMILES Cc1nc(cc(n1)N1CCC(CC1)C1CCN(CC1)C(=O)OC(C)(C)C)C#N
Show InChI InChI=1S/C21H31N5O2/c1-15-23-18(14-22)13-19(24-15)25-9-5-16(6-10-25)17-7-11-26(12-8-17)20(27)28-21(2,3)4/h13,16-17H,5-12H2,1-4H3
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n/an/an/an/a 2n/an/an/an/a



Merck& Co.

Curated by ChEMBL


Assay Description
Agonist activity at human GPR119 expressed in CHO cells co-expressing Galpha15 assessed as increase of intracellular cAMP accumulation after 60 mins ...

Bioorg Med Chem Lett 21: 2665-9 (2011)


Article DOI: 10.1016/j.bmcl.2010.12.086
BindingDB Entry DOI: 10.7270/Q2M61KJV
More data for this
Ligand-Target Pair
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