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USPatent US10208019

Compile Data Set for Download or QSAR

Found 434 hits of Enzyme Inhibition Constant Data   
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
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349656
PNG
(2-{[(2S)-4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin...)
Show SMILES COCCn1c(CN2CCN(C[C@@H]2C)c2cccc(OCc3ccc(cc3F)C#N)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H31FN6O4/c1-20-17-36(27-4-3-5-29(34-27)41-19-23-7-6-21(16-32)14-24(23)31)11-10-35(20)18-28-33-25-9-8-22(30(38)39)15-26(25)37(28)12-13-40-2/h3-9,14-15,20H,10-13,17-19H2,1-2H3,(H,38,39)/t20-/m0/s1
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n/an/an/an/a 4.30n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349659
PNG
(2-{[(2S)-4-{6-[(4-chloro-2-fluorobenzyl)oxy]-3-flu...)
Show SMILES COCCn1c(CN2CCN(C[C@@H]2C)c2nc(OCc3ccc(Cl)cc3F)ccc2F)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C29H30ClF2N5O4/c1-18-15-36(28-22(31)6-8-27(34-28)41-17-20-3-5-21(30)14-23(20)32)10-9-35(18)16-26-33-24-7-4-19(29(38)39)13-25(24)37(26)11-12-40-2/h3-8,13-14,18H,9-12,15-17H2,1-2H3,(H,38,39)/t18-/m0/s1
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n/an/an/an/a 350n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349662
PNG
(2-{[4-(6-{[(4-cyano-2-fluorophenyl)(methyl-d2)]oxy...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(cc4F)C#N)n3)n(C[C@@H]3CCO3)c2c1
Show InChI InChI=1S/C31H30FN5O4/c32-25-14-20(16-33)4-5-23(25)19-41-30-3-1-2-26(35-30)21-8-11-36(12-9-21)18-29-34-27-7-6-22(31(38)39)15-28(27)37(29)17-24-10-13-40-24/h1-7,14-15,21,24H,8-13,17-19H2,(H,38,39)/t24-/m0/s1
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n/an/an/an/a 0.950n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
3D
3D Structure (crystal)
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349669
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES Cn1cncc1Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(cc3F)C#N)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H30FN7O3/c1-38-20-35-16-25(38)17-40-29-14-23(32(41)42)7-8-28(29)36-30(40)18-39-11-9-22(10-12-39)27-3-2-4-31(37-27)43-19-24-6-5-21(15-34)13-26(24)33/h2-8,13-14,16,20,22H,9-12,17-19H2,1H3,(H,41,42)
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n/an/an/an/a 1.5n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349670
PNG
(2-[(4-{6-[(2,4-difluorobenzyl)oxy]pyridin-2-yl}pip...)
Show SMILES Cn1cncc1Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(F)cc3F)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H30F2N6O3/c1-37-19-34-15-24(37)16-39-28-13-21(31(40)41)6-8-27(28)35-29(39)17-38-11-9-20(10-12-38)26-3-2-4-30(36-26)42-18-22-5-7-23(32)14-25(22)33/h2-8,13-15,19-20H,9-12,16-18H2,1H3,(H,40,41)
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n/an/an/an/a 2.40n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349673
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES Cn1cnnc1Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(cc3F)C#N)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H29FN8O3/c1-38-19-34-37-29(38)17-40-27-14-22(31(41)42)7-8-26(27)35-28(40)16-39-11-9-21(10-12-39)25-3-2-4-30(36-25)43-18-23-6-5-20(15-33)13-24(23)32/h2-8,13-14,19,21H,9-12,16-18H2,1H3,(H,41,42)
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n/an/an/an/a 44n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349674
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(cc4F)C#N)n3)n(C[C@@H]3CCCO3)c2c1
Show InChI InChI=1S/C32H32FN5O4/c33-26-15-21(17-34)6-7-24(26)20-42-31-5-1-4-27(36-31)22-10-12-37(13-11-22)19-30-35-28-9-8-23(32(39)40)16-29(28)38(30)18-25-3-2-14-41-25/h1,4-9,15-16,22,25H,2-3,10-14,18-20H2,(H,39,40)/t25-/m0/s1
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n/an/an/an/a 75n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349676
PNG
(US10208019, Example 1A-23 | rac-2-{[(3S,4S)-4-{6-[...)
Show SMILES COCCn1c(CN2CC[C@H]([C@H](O)C2)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ccc(cc12)C(O)=O |r|
Show InChI InChI=1S/C29H30ClFN4O5/c1-39-12-11-35-25-13-18(29(37)38)6-8-24(25)32-27(35)16-34-10-9-21(26(36)15-34)23-3-2-4-28(33-23)40-17-19-5-7-20(30)14-22(19)31/h2-8,13-14,21,26,36H,9-12,15-17H2,1H3,(H,37,38)/t21-,26+/m0/s1
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n/an/an/an/a 1.00E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349680
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES CO[C@@H]1CCC[C@H]1n1c(CN2CCC(CC2)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H34ClFN4O4/c1-41-29-6-3-5-27(29)38-28-16-21(32(39)40)9-11-26(28)35-30(38)18-37-14-12-20(13-15-37)25-4-2-7-31(36-25)42-19-22-8-10-23(33)17-24(22)34/h2,4,7-11,16-17,20,27,29H,3,5-6,12-15,18-19H2,1H3,(H,39,40)/t27-,29-/m1/s1
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n/an/an/an/a 1.40E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349691
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ccc(C(O)=O)c(F)c12
Show InChI InChI=1S/C29H29ClF2N4O4/c1-39-14-13-36-25(33-24-8-7-21(29(37)38)27(32)28(24)36)16-35-11-9-18(10-12-35)23-3-2-4-26(34-23)40-17-19-5-6-20(30)15-22(19)31/h2-8,15,18H,9-14,16-17H2,1H3,(H,37,38)
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n/an/an/an/a 5.80n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349693
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES COCCn1c(CN2CCC(CC2)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ncc(nc12)C(O)=O
Show InChI InChI=1S/C27H28ClFN6O4/c1-38-12-11-35-23(33-25-26(35)32-22(14-30-25)27(36)37)15-34-9-7-17(8-10-34)21-3-2-4-24(31-21)39-16-18-5-6-19(28)13-20(18)29/h2-6,13-14,17H,7-12,15-16H2,1H3,(H,36,37)
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349695
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES Cc1nc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(C)c2cc1C(O)=O
Show InChI InChI=1S/C27H27ClFN5O3/c1-16-20(27(35)36)13-23-26(30-16)32-24(33(23)2)14-34-10-8-17(9-11-34)22-4-3-5-25(31-22)37-15-18-6-7-19(28)12-21(18)29/h3-7,12-13,17H,8-11,14-15H2,1-2H3,(H,35,36)
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n/an/an/an/a 340n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349701
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(Cc3ncco3)c2n1
Show InChI InChI=1S/C29H26ClFN6O4/c30-20-5-4-19(21(31)14-20)17-41-26-3-1-2-22(34-26)18-8-11-36(12-9-18)15-25-33-23-6-7-24(29(38)39)35-28(23)37(25)16-27-32-10-13-40-27/h1-7,10,13-14,18H,8-9,11-12,15-17H2,(H,38,39)
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349706
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(C[C@@H]3CCO3)c2n1
Show InChI InChI=1S/C29H29ClFN5O4/c30-20-5-4-19(22(31)14-20)17-40-27-3-1-2-23(33-27)18-8-11-35(12-9-18)16-26-32-24-6-7-25(29(37)38)34-28(24)36(26)15-21-10-13-39-21/h1-7,14,18,21H,8-13,15-17H2,(H,37,38)/t21-/m0/s1
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349709
PNG
(2-[(4-{6-[(4-Cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES OC(=O)c1ccc2nc(CN3CCN(CC3)c3cccc(OCc4ccc(cc4F)C#N)n3)n(C[C@@H]3CCO3)c2c1
Show InChI InChI=1S/C30H29FN6O4/c31-24-14-20(16-32)4-5-22(24)19-41-29-3-1-2-27(34-29)36-11-9-35(10-12-36)18-28-33-25-7-6-21(30(38)39)15-26(25)37(28)17-23-8-13-40-23/h1-7,14-15,23H,8-13,17-19H2,(H,38,39)/t23-/m0/s1
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n/an/an/an/a 7.40n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349710
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(cc4F)C#N)n3)n(C[C@@H]3CCO3)c2n1
Show InChI InChI=1S/C30H29FN6O4/c31-23-14-19(15-32)4-5-21(23)18-41-28-3-1-2-24(34-28)20-8-11-36(12-9-20)17-27-33-25-6-7-26(30(38)39)35-29(25)37(27)16-22-10-13-40-22/h1-7,14,20,22H,8-13,16-18H2,(H,38,39)/t22-/m0/s1
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n/an/an/an/a 0.760n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349711
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(cc4F)C#N)n3)n(Cc3ncco3)c2c1
Show InChI InChI=1S/C31H27FN6O4/c32-24-14-20(16-33)4-5-23(24)19-42-29-3-1-2-25(36-29)21-8-11-37(12-9-21)17-28-35-26-7-6-22(31(39)40)15-27(26)38(28)18-30-34-10-13-41-30/h1-7,10,13-15,21H,8-9,11-12,17-19H2,(H,39,40)
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n/an/an/an/a 3.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349716
PNG
(2-((4-(6-(Benzyloxy)pyridin-2-yl)piperidin-1-yl)me...)
Show SMILES Cn1c(CN2CCC(CC2)c2cccc(OCc3ccccc3)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C27H28N4O3/c1-30-24-16-21(27(32)33)10-11-23(24)28-25(30)17-31-14-12-20(13-15-31)22-8-5-9-26(29-22)34-18-19-6-3-2-4-7-19/h2-11,16,20H,12-15,17-18H2,1H3,(H,32,33)
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n/an/an/an/a 1.20E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349724
PNG
(1-methyl-2-{[4-(6-{[4-(trifluoromethoxy)benzyl]oxy...)
Show SMILES Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(OC(F)(F)F)cc3)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C28H27F3N4O4/c1-34-24-15-20(27(36)37)7-10-23(24)32-25(34)16-35-13-11-19(12-14-35)22-3-2-4-26(33-22)38-17-18-5-8-21(9-6-18)39-28(29,30)31/h2-10,15,19H,11-14,16-17H2,1H3,(H,36,37)
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n/an/an/an/a 880n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349729
PNG
(2-[(4-{6-[(2,5-difluorobenzyl)oxy]pyridin-2-yl}pip...)
Show SMILES Cn1c(CN2CCC(CC2)c2cccc(OCc3cc(F)ccc3F)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C27H26F2N4O3/c1-32-24-14-18(27(34)35)5-8-23(24)30-25(32)15-33-11-9-17(10-12-33)22-3-2-4-26(31-22)36-16-19-13-20(28)6-7-21(19)29/h2-8,13-14,17H,9-12,15-16H2,1H3,(H,34,35)
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n/an/an/an/a 1.80E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349732
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES CCn1cncc1Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H32ClFN6O3/c1-2-39-20-35-16-25(39)17-40-29-14-22(32(41)42)7-9-28(29)36-30(40)18-38-12-10-21(11-13-38)27-4-3-5-31(37-27)43-19-23-6-8-24(33)15-26(23)34/h3-9,14-16,20-21H,2,10-13,17-19H2,1H3,(H,41,42)
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n/an/an/an/a 2.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349735
PNG
(2-[(4-{6-[(2,4-difluorobenzyl)oxy]pyridin-2-yl}pip...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(F)cc4F)n3)n(C[C@@H]3CCO3)c2c1
Show InChI InChI=1S/C30H30F2N4O4/c31-22-6-4-21(24(32)15-22)18-40-29-3-1-2-25(34-29)19-8-11-35(12-9-19)17-28-33-26-7-5-20(30(37)38)14-27(26)36(28)16-23-10-13-39-23/h1-7,14-15,19,23H,8-13,16-18H2,(H,37,38)/t23-/m0/s1
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n/an/an/an/a 2.40n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349742
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(CCN3CCCC3=O)c2c1
Show InChI InChI=1S/C32H33ClFN5O4/c33-24-8-6-23(25(34)18-24)20-43-30-4-1-3-26(36-30)21-10-13-37(14-11-21)19-29-35-27-9-7-22(32(41)42)17-28(27)39(29)16-15-38-12-2-5-31(38)40/h1,3-4,6-9,17-18,21H,2,5,10-16,19-20H2,(H,41,42)
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n/an/an/an/a 4.40E+3n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349743
PNG
(2-{[(2S)-4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridi...)
Show SMILES C[C@H]1CN(CCN1Cc1nc2ccc(cc2n1Cc1cocn1)C(O)=O)c1cccc(OCc2ccc(Cl)cc2F)n1
Show InChI InChI=1S/C30H28ClFN6O4/c1-19-13-37(27-3-2-4-29(35-27)42-16-21-5-7-22(31)12-24(21)32)10-9-36(19)15-28-34-25-8-6-20(30(39)40)11-26(25)38(28)14-23-17-41-18-33-23/h2-8,11-12,17-19H,9-10,13-16H2,1H3,(H,39,40)/t19-/m0/s1
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n/an/an/an/a 170n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349746
PNG
(2-{[(2S)-4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridi...)
Show SMILES C[C@H]1CN(CCN1Cc1nc2ccc(cc2n1Cc1cnco1)C(O)=O)c1cccc(OCc2ccc(Cl)cc2F)n1
Show InChI InChI=1S/C30H28ClFN6O4/c1-19-14-37(27-3-2-4-29(35-27)41-17-21-5-7-22(31)12-24(21)32)10-9-36(19)16-28-34-25-8-6-20(30(39)40)11-26(25)38(28)15-23-13-33-18-42-23/h2-8,11-13,18-19H,9-10,14-17H2,1H3,(H,39,40)/t19-/m0/s1
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n/an/an/an/a 1.70n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349748
PNG
(2-{[(2S)-4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridi...)
Show SMILES C[C@H]1CN(CCN1Cc1nc2ccc(cc2n1Cc1ncco1)C(O)=O)c1cccc(OCc2ccc(Cl)cc2F)n1
Show InChI InChI=1S/C30H28ClFN6O4/c1-19-15-37(26-3-2-4-28(35-26)42-18-21-5-7-22(31)14-23(21)32)11-10-36(19)16-27-34-24-8-6-20(30(39)40)13-25(24)38(27)17-29-33-9-12-41-29/h2-9,12-14,19H,10-11,15-18H2,1H3,(H,39,40)/t19-/m0/s1
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n/an/an/an/a 33n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349750
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES Cc1nnc(Cn2c(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)nc3ccc(cc23)C(O)=O)n1C
Show InChI InChI=1S/C31H31ClFN7O3/c1-19-36-37-29(38(19)2)17-40-27-14-21(31(41)42)7-9-26(27)34-28(40)16-39-12-10-20(11-13-39)25-4-3-5-30(35-25)43-18-22-6-8-23(32)15-24(22)33/h3-9,14-15,20H,10-13,16-18H2,1-2H3,(H,41,42)
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349755
PNG
(2-{[(2S)-4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin...)
Show SMILES C[C@H]1CN(CCN1Cc1nc2ccc(cc2n1Cc1cncn1C)C(O)=O)c1cccc(OCc2ccc(cc2F)C#N)n1
Show InChI InChI=1S/C32H31FN8O3/c1-21-16-40(29-4-3-5-31(37-29)44-19-24-7-6-22(14-34)12-26(24)33)11-10-39(21)18-30-36-27-9-8-23(32(42)43)13-28(27)41(30)17-25-15-35-20-38(25)2/h3-9,12-13,15,20-21H,10-11,16-19H2,1-2H3,(H,42,43)/t21-/m0/s1
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349761
PNG
(2-[(4-{6-[(2,4-difluorobenzyl)oxy]pyridin-2-yl}pip...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(F)cc4F)n3)n(Cc3ncco3)c2c1
Show InChI InChI=1S/C30H27F2N5O4/c31-22-6-4-21(23(32)15-22)18-41-28-3-1-2-24(35-28)19-8-11-36(12-9-19)16-27-34-25-7-5-20(30(38)39)14-26(25)37(27)17-29-33-10-13-40-29/h1-7,10,13-15,19H,8-9,11-12,16-18H2,(H,38,39)
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n/an/an/an/a 59n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349764
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES OC(=O)c1ccc2nc(CN3CCN(CC3)c3cccc(OCc4ccc(cc4F)C#N)n3)n(Cc3ncco3)c2c1
Show InChI InChI=1S/C30H26FN7O4/c31-23-14-20(16-32)4-5-22(23)19-42-28-3-1-2-26(35-28)37-11-9-36(10-12-37)17-27-34-24-7-6-21(30(39)40)15-25(24)38(27)18-29-33-8-13-41-29/h1-8,13-15H,9-12,17-19H2,(H,39,40)
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349765
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES CCn1cncc1Cn1c(CN2CCN(CC2)c2cccc(OCc3ccc(cc3F)C#N)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H31FN8O3/c1-2-39-21-35-17-25(39)18-41-28-15-23(32(42)43)8-9-27(28)36-30(41)19-38-10-12-40(13-11-38)29-4-3-5-31(37-29)44-20-24-7-6-22(16-34)14-26(24)33/h3-9,14-15,17,21H,2,10-13,18-20H2,1H3,(H,42,43)
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n/an/an/an/a 0.300n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349766
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES Cn1cncc1Cn1c(CN2CCN(CC2)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H29ClFN7O3/c1-36-19-33-15-23(36)16-39-26-13-20(30(40)41)6-8-25(26)34-28(39)17-37-9-11-38(12-10-37)27-3-2-4-29(35-27)42-18-21-5-7-22(31)14-24(21)32/h2-8,13-15,19H,9-12,16-18H2,1H3,(H,40,41)
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n/an/an/an/a 0.330n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349767
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES Cn1cncc1Cn1c(CN2CCN(CC2)c2cccc(OCc3ccc(cc3F)C#N)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C31H29FN8O3/c1-37-20-34-16-24(37)17-40-27-14-22(31(41)42)7-8-26(27)35-29(40)18-38-9-11-39(12-10-38)28-3-2-4-30(36-28)43-19-23-6-5-21(15-33)13-25(23)32/h2-8,13-14,16,20H,9-12,17-19H2,1H3,(H,41,42)
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349772
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(Cc3ncco3)c2c1
Show InChI InChI=1S/C30H27ClFN5O4/c31-22-6-4-21(23(32)15-22)18-41-28-3-1-2-24(35-28)19-8-11-36(12-9-19)16-27-34-25-7-5-20(30(38)39)14-26(25)37(27)17-29-33-10-13-40-29/h1-7,10,13-15,19H,8-9,11-12,16-18H2,(H,38,39)
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349773
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(cc4F)C#N)n3)n(Cc3cnco3)c2c1
Show InChI InChI=1S/C31H27FN6O4/c32-25-12-20(14-33)4-5-23(25)18-41-30-3-1-2-26(36-30)21-8-10-37(11-9-21)17-29-35-27-7-6-22(31(39)40)13-28(27)38(29)16-24-15-34-19-42-24/h1-7,12-13,15,19,21H,8-11,16-18H2,(H,39,40)
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349785
PNG
(2-[(4-{6-[(4-cyanobenzyl)oxy]-5-fluoropyridin-2-yl...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3ccc(F)c(OCc4ccc(cc4)C#N)n3)n(C[C@@H]3CCO3)c2c1
Show InChI InChI=1S/C31H30FN5O4/c32-25-6-8-26(35-30(25)41-19-21-3-1-20(16-33)2-4-21)22-9-12-36(13-10-22)18-29-34-27-7-5-23(31(38)39)15-28(27)37(29)17-24-11-14-40-24/h1-8,15,22,24H,9-14,17-19H2,(H,38,39)/t24-/m0/s1
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n/an/an/an/a 1.20n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349789
PNG
(2-{[(2S)-4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin...)
Show SMILES C[C@H]1CN(CCN1Cc1nc2ccc(cc2n1C[C@H]1CCOC1)C(O)=O)c1cccc(OCc2ccc(cc2F)C#N)n1
Show InChI InChI=1S/C32H33FN6O4/c1-21-16-38(29-3-2-4-31(36-29)43-20-25-6-5-22(15-34)13-26(25)33)11-10-37(21)18-30-35-27-8-7-24(32(40)41)14-28(27)39(30)17-23-9-12-42-19-23/h2-8,13-14,21,23H,9-12,16-20H2,1H3,(H,40,41)/t21-,23+/m0/s1
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n/an/an/an/a 4.70n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349794
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(Cc3ccno3)c2c1
Show InChI InChI=1S/C30H27ClFN5O4/c31-22-6-4-21(24(32)15-22)18-40-29-3-1-2-25(35-29)19-9-12-36(13-10-19)17-28-34-26-7-5-20(30(38)39)14-27(26)37(28)16-23-8-11-33-41-23/h1-8,11,14-15,19H,9-10,12-13,16-18H2,(H,38,39)
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n/an/an/an/a 2n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349797
PNG
(2-{[(2S)-4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridi...)
Show SMILES CCn1cncc1Cn1c(CN2CCN(C[C@@H]2C)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H33ClFN7O3/c1-3-38-20-35-15-25(38)17-41-28-13-22(32(42)43)8-10-27(28)36-30(41)18-39-11-12-40(16-21(39)2)29-5-4-6-31(37-29)44-19-23-7-9-24(33)14-26(23)34/h4-10,13-15,20-21H,3,11-12,16-19H2,1-2H3,(H,42,43)/t21-/m0/s1
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n/an/an/an/a 6.80n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349798
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(Cc3cnoc3)c2c1
Show InChI InChI=1S/C30H27ClFN5O4/c31-23-6-4-22(24(32)13-23)18-40-29-3-1-2-25(35-29)20-8-10-36(11-9-20)16-28-34-26-7-5-21(30(38)39)12-27(26)37(28)15-19-14-33-41-17-19/h1-7,12-14,17,20H,8-11,15-16,18H2,(H,38,39)
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n/an/an/an/a 140n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349804
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCN(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(C[C@@H]3CCO3)c2n1
Show InChI InChI=1S/C28H28ClFN6O4/c29-19-5-4-18(21(30)14-19)17-40-26-3-1-2-24(33-26)35-11-9-34(10-12-35)16-25-31-22-6-7-23(28(37)38)32-27(22)36(25)15-20-8-13-39-20/h1-7,14,20H,8-13,15-17H2,(H,37,38)/t20-/m0/s1
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n/an/an/an/a 0.900n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349805
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES CCn1cncc1Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(cc3F)C#N)n2)nc2ccc(nc12)C(O)=O
Show InChI InChI=1S/C32H31FN8O3/c1-2-40-20-35-16-24(40)17-41-29(36-27-8-9-28(32(42)43)38-31(27)41)18-39-12-10-22(11-13-39)26-4-3-5-30(37-26)44-19-23-7-6-21(15-34)14-25(23)33/h3-9,14,16,20,22H,2,10-13,17-19H2,1H3,(H,42,43)
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n/an/an/an/a 0.950n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349806
PNG
(2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl...)
Show SMILES Cn1cncc1Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(cc3F)C#N)n2)nc2ccc(nc12)C(O)=O
Show InChI InChI=1S/C31H29FN8O3/c1-38-19-34-15-23(38)16-40-28(35-26-7-8-27(31(41)42)37-30(26)40)17-39-11-9-21(10-12-39)25-3-2-4-29(36-25)43-18-22-6-5-20(14-33)13-24(22)32/h2-8,13,15,19,21H,9-12,16-18H2,1H3,(H,41,42)
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n/an/an/an/a 2.90n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349810
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES Cn1cnc(CCn2c(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)nc3ccc(cc23)C(O)=O)c1
Show InChI InChI=1S/C32H32ClFN6O3/c1-38-17-25(35-20-38)11-14-40-29-15-22(32(41)42)6-8-28(29)36-30(40)18-39-12-9-21(10-13-39)27-3-2-4-31(37-27)43-19-23-5-7-24(33)16-26(23)34/h2-8,15-17,20-21H,9-14,18-19H2,1H3,(H,41,42)
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n/an/an/an/a>1.00E+4n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349814
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(CCC3CCCCO3)c2c1
Show InChI InChI=1S/C33H36ClFN4O4/c34-25-9-7-24(27(35)19-25)21-43-32-6-3-5-28(37-32)22-11-14-38(15-12-22)20-31-36-29-10-8-23(33(40)41)18-30(29)39(31)16-13-26-4-1-2-17-42-26/h3,5-10,18-19,22,26H,1-2,4,11-17,20-21H2,(H,40,41)
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Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349828
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES COCCn1cnnc1Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C32H33ClFN7O4/c1-44-14-13-40-20-35-38-30(40)18-41-28-15-22(32(42)43)6-8-27(28)36-29(41)17-39-11-9-21(10-12-39)26-3-2-4-31(37-26)45-19-23-5-7-24(33)16-25(23)34/h2-8,15-16,20-21H,9-14,17-19H2,1H3,(H,42,43)
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n/an/an/an/a 15n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349833
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(Cc3cc[nH]n3)c2c1
Show InChI InChI=1S/C30H28ClFN6O3/c31-22-6-4-21(24(32)15-22)18-41-29-3-1-2-25(35-29)19-9-12-37(13-10-19)17-28-34-26-7-5-20(30(39)40)14-27(26)38(28)16-23-8-11-33-36-23/h1-8,11,14-15,19H,9-10,12-13,16-18H2,(H,33,36)(H,39,40)
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n/an/an/an/a 28n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349833
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(Cc3cc[nH]n3)c2c1
Show InChI InChI=1S/C30H28ClFN6O3/c31-22-6-4-21(24(32)15-22)18-41-29-3-1-2-25(35-29)19-9-12-37(13-10-19)17-28-34-26-7-5-20(30(39)40)14-27(26)38(28)16-23-8-11-33-36-23/h1-8,11,14-15,19H,9-10,12-13,16-18H2,(H,33,36)(H,39,40)
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n/an/an/an/a 450n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349834
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES OC(=O)c1ccc2nc(CN3CCC(CC3)c3cccc(OCc4ccc(Cl)cc4F)n3)n(Cc3nnc[nH]3)c2c1
Show InChI InChI=1S/C29H27ClFN7O3/c30-21-6-4-20(22(31)13-21)16-41-28-3-1-2-23(35-28)18-8-10-37(11-9-18)15-27-34-24-7-5-19(29(39)40)12-25(24)38(27)14-26-32-17-33-36-26/h1-7,12-13,17-18H,8-11,14-16H2,(H,39,40)(H,32,33,36)
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n/an/an/an/a 360n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
Glucagon-like peptide 1 receptor


(Homo sapiens (Human))
BDBM349842
PNG
(2-[(4-{6-[(4-chloro-2-fluorobenzyl)oxy]pyridin-2-y...)
Show SMILES Cn1ncnc1Cn1c(CN2CCC(CC2)c2cccc(OCc3ccc(Cl)cc3F)n2)nc2ccc(cc12)C(O)=O
Show InChI InChI=1S/C30H29ClFN7O3/c1-37-27(33-18-34-37)16-39-26-13-20(30(40)41)6-8-25(26)35-28(39)15-38-11-9-19(10-12-38)24-3-2-4-29(36-24)42-17-21-5-7-22(31)14-23(21)32/h2-8,13-14,18-19H,9-12,15-17H2,1H3,(H,40,41)
PDB

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n/an/an/an/a 96n/an/an/an/a



Pfizer Inc.

US Patent


Assay Description
GLP-1R-mediated agonist activity was determined with a cell-based functional assay utilizing an HTRF (Homogeneous Time-Resolved Fluorescence) cAMP de...


US Patent US10208019 (2019)


BindingDB Entry DOI: 10.7270/Q2WH2S4X
More data for this
Ligand-Target Pair
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* indicates data uncertainty>20%