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Patent code US10807971

Compile Data Set for Download or QSAR
Found 68 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
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468963
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1cc(cn1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2)C1=O
Show InChI InChI=1S/C26H25Cl2F2N5O4/c27-15-5-14(6-16(28)7-15)10-32-24(36)26(38)3-4-34(25(26)37)19-11-33-35(12-19)18-9-22(31)23(39-13-18)20-8-17(29)1-2-21(20)30/h1-2,5-8,11-12,18,22-23,38H,3-4,9-10,13,31H2,(H,32,36)/t18-,22+,23-,26?/m1/s1
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n/an/a 0.474n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468964
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1cc(cn1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C26H24Cl2F3N5O4/c27-14-5-13(22(31)19(28)6-14)9-33-24(37)26(39)3-4-35(25(26)38)17-10-34-36(11-17)16-8-21(32)23(40-12-16)18-7-15(29)1-2-20(18)30/h1-2,5-7,10-11,16,21,23,39H,3-4,8-9,12,32H2,(H,33,37)/t16-,21+,23-,26?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468972
PNG
((3S)-1-[2-[(3R,5S,6R)-5-Amino-6-(2,5-difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C25H24ClF3N6O4/c26-14-5-13(6-16(28)7-14)10-31-23(36)25(38)3-4-34(24(25)37)21-11-32-35(33-21)17-9-20(30)22(39-12-17)18-8-15(27)1-2-19(18)29/h1-2,5-8,11,17,20,22,38H,3-4,9-10,12,30H2,(H,31,36)/t17-,20+,22-,25+/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468975
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C25H23Cl2F3N6O4/c26-13-5-12(21(30)17(27)6-13)9-32-23(37)25(39)3-4-35(24(25)38)20-10-33-36(34-20)15-8-19(31)22(40-11-15)16-7-14(28)1-2-18(16)29/h1-2,5-7,10,15,19,22,39H,3-4,8-9,11,31H2,(H,32,37)/t15-,19+,22-,25?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468975
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C25H23Cl2F3N6O4/c26-13-5-12(21(30)17(27)6-13)9-32-23(37)25(39)3-4-35(24(25)38)20-10-33-36(34-20)15-8-19(31)22(40-11-15)16-7-14(28)1-2-18(16)29/h1-2,5-7,10,15,19,22,39H,3-4,8-9,11,31H2,(H,32,37)/t15-,19+,22-,25?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468974
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C25H23F5N6O4/c26-13-1-2-17(28)16(6-13)22-19(31)8-15(11-40-22)36-33-10-20(34-36)35-4-3-25(39,24(35)38)23(37)32-9-12-5-14(27)7-18(29)21(12)30/h1-2,5-7,10,15,19,22,39H,3-4,8-9,11,31H2,(H,32,37)/t15-,19+,22-,25?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468972
PNG
((3S)-1-[2-[(3R,5S,6R)-5-Amino-6-(2,5-difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C25H24ClF3N6O4/c26-14-5-13(6-16(28)7-14)10-31-23(36)25(38)3-4-34(24(25)37)21-11-32-35(33-21)17-9-20(30)22(39-12-17)18-8-15(27)1-2-19(18)29/h1-2,5-8,11,17,20,22,38H,3-4,9-10,12,30H2,(H,31,36)/t17-,20+,22-,25+/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468964
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1cc(cn1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C26H24Cl2F3N5O4/c27-14-5-13(22(31)19(28)6-14)9-33-24(37)26(39)3-4-35(25(26)38)17-10-34-36(11-17)16-8-21(32)23(40-12-16)18-7-15(29)1-2-20(18)30/h1-2,5-7,10-11,16,21,23,39H,3-4,8-9,12,32H2,(H,33,37)/t16-,21+,23-,26?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468963
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1cc(cn1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2)C1=O
Show InChI InChI=1S/C26H25Cl2F2N5O4/c27-15-5-14(6-16(28)7-15)10-32-24(36)26(38)3-4-34(25(26)37)19-11-33-35(12-19)18-9-22(31)23(39-13-18)20-8-17(29)1-2-21(20)30/h1-2,5-8,11-12,18,22-23,38H,3-4,9-10,13,31H2,(H,32,36)/t18-,22+,23-,26?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468977
PNG
(1-[2-[(3R,5S,6R)-5-Aamino- 6-(2,5- difluorophenyl)...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C26H24Cl2F3N5O4/c27-14-7-13(22(31)18(28)8-14)11-33-24(37)26(39)4-6-35(25(26)38)21-3-5-36(34-21)16-10-20(32)23(40-12-16)17-9-15(29)1-2-19(17)30/h1-3,5,7-9,16,20,23,39H,4,6,10-12,32H2,(H,33,37)/t16-,20+,23-,26?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468976
PNG
((3S)-1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C26H25ClF3N5O4/c27-15-7-14(8-17(29)9-15)12-32-24(36)26(38)4-6-34(25(26)37)22-3-5-35(33-22)18-11-21(31)23(39-13-18)19-10-16(28)1-2-20(19)30/h1-3,5,7-10,18,21,23,38H,4,6,11-13,31H2,(H,32,36)/t18-,21+,23-,26+/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468973
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C25H24F4N6O4/c26-14-4-5-17(27)16(8-14)22-19(30)9-15(12-39-22)35-32-11-20(33-35)34-7-6-25(38,24(34)37)23(36)31-10-13-2-1-3-18(28)21(13)29/h1-5,8,11,15,19,22,38H,6-7,9-10,12,30H2,(H,31,36)/t15-,19+,22-,25?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468974
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C25H23F5N6O4/c26-13-1-2-17(28)16(6-13)22-19(31)8-15(11-40-22)36-33-10-20(34-36)35-4-3-25(39,24(35)38)23(37)32-9-12-5-14(27)7-18(29)21(12)30/h1-2,5-7,10,15,19,22,39H,3-4,8-9,11,31H2,(H,32,37)/t15-,19+,22-,25?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468957
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2ccc(cc2C1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C31H29F5N4O4/c32-19-2-4-24(34)23(9-19)28-26(37)11-22(15-44-28)39-13-16-1-3-21(8-18(16)14-39)40-6-5-31(43,30(40)42)29(41)38-12-17-7-20(33)10-25(35)27(17)36/h1-4,7-10,22,26,28,43H,5-6,11-15,37H2,(H,38,41)/t22-,26+,28-,31?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468977
PNG
(1-[2-[(3R,5S,6R)-5-Aamino- 6-(2,5- difluorophenyl)...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C26H24Cl2F3N5O4/c27-14-7-13(22(31)18(28)8-14)11-33-24(37)26(39)4-6-35(25(26)38)21-3-5-36(34-21)16-10-20(32)23(40-12-16)17-9-15(29)1-2-19(17)30/h1-3,5,7-9,16,20,23,39H,4,6,10-12,32H2,(H,33,37)/t16-,20+,23-,26?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468976
PNG
((3S)-1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C26H25ClF3N5O4/c27-15-7-14(8-17(29)9-15)12-32-24(36)26(38)4-6-34(25(26)37)22-3-5-35(33-22)18-11-21(31)23(39-13-18)19-10-16(28)1-2-20(19)30/h1-3,5,7-10,18,21,23,38H,4,6,11-13,31H2,(H,32,36)/t18-,21+,23-,26+/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468973
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C25H24F4N6O4/c26-14-4-5-17(27)16(8-14)22-19(30)9-15(12-39-22)35-32-11-20(33-35)34-7-6-25(38,24(34)37)23(36)31-10-13-2-1-3-18(28)21(13)29/h1-5,8,11,15,19,22,38H,6-7,9-10,12,30H2,(H,31,36)/t15-,19+,22-,25?/m1/s1
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n/an/a 3.57n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468958
PNG
(1-[2-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2ccc(cc2C1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C31H30F4N4O4/c32-20-5-7-24(33)23(11-20)28-26(36)12-22(16-43-28)38-14-18-4-6-21(10-19(18)15-38)39-9-8-31(42,30(39)41)29(40)37-13-17-2-1-3-25(34)27(17)35/h1-7,10-11,22,26,28,42H,8-9,12-16,36H2,(H,37,40)/t22-,26+,28-,31?/m1/s1
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n/an/a 3.67n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468979
PNG
(1-[1-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2)C1=O
Show InChI InChI=1S/C26H25F4N5O4/c27-15-1-2-20(30)19(10-15)23-21(31)11-18(13-39-23)35-5-3-22(33-35)34-6-4-26(38,25(34)37)24(36)32-12-14-7-16(28)9-17(29)8-14/h1-3,5,7-10,18,21,23,38H,4,6,11-13,31H2,(H,32,36)/t18-,21+,23-,26?/m1/s1
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n/an/a 6.23n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468958
PNG
(1-[2-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2ccc(cc2C1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C31H30F4N4O4/c32-20-5-7-24(33)23(11-20)28-26(36)12-22(16-43-28)38-14-18-4-6-21(10-19(18)15-38)39-9-8-31(42,30(39)41)29(40)37-13-17-2-1-3-25(34)27(17)35/h1-7,10-11,22,26,28,42H,8-9,12-16,36H2,(H,37,40)/t22-,26+,28-,31?/m1/s1
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n/an/a 6.46n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468957
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2ccc(cc2C1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C31H29F5N4O4/c32-19-2-4-24(34)23(9-19)28-26(37)11-22(15-44-28)39-13-16-1-3-21(8-18(16)14-39)40-6-5-31(43,30(40)42)29(41)38-12-17-7-20(33)10-25(35)27(17)36/h1-4,7-10,22,26,28,43H,5-6,11-15,37H2,(H,38,41)/t22-,26+,28-,31?/m1/s1
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n/an/a 6.53n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468980
PNG
(1-[1-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cccc(F)c2)C1=O
Show InChI InChI=1S/C26H26F3N5O4/c27-16-3-1-2-15(10-16)13-31-24(35)26(37)7-9-33(25(26)36)22-6-8-34(32-22)18-12-21(30)23(38-14-18)19-11-17(28)4-5-20(19)29/h1-6,8,10-11,18,21,23,37H,7,9,12-14,30H2,(H,31,35)/t18-,21+,23-,26?/m1/s1
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n/an/a 6.76n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468978
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C26H24F5N5O4/c27-14-1-2-18(29)17(8-14)23-20(32)10-16(12-40-23)36-5-3-21(34-36)35-6-4-26(39,25(35)38)24(37)33-11-13-7-15(28)9-19(30)22(13)31/h1-3,5,7-9,16,20,23,39H,4,6,10-12,32H2,(H,33,37)/t16-,20+,23-,26?/m1/s1
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n/an/a 7.56n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468979
PNG
(1-[1-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2)C1=O
Show InChI InChI=1S/C26H25F4N5O4/c27-15-1-2-20(30)19(10-15)23-21(31)11-18(13-39-23)35-5-3-22(33-35)34-6-4-26(38,25(34)37)24(36)32-12-14-7-16(28)9-17(29)8-14/h1-3,5,7-10,18,21,23,38H,4,6,11-13,31H2,(H,32,36)/t18-,21+,23-,26?/m1/s1
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n/an/a 7.73n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468977
PNG
(1-[2-[(3R,5S,6R)-5-Aamino- 6-(2,5- difluorophenyl)...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C26H24Cl2F3N5O4/c27-14-7-13(22(31)18(28)8-14)11-33-24(37)26(39)4-6-35(25(26)38)21-3-5-36(34-21)16-10-20(32)23(40-12-16)17-9-15(29)1-2-19(17)30/h1-3,5,7-9,16,20,23,39H,4,6,10-12,32H2,(H,33,37)/t16-,20+,23-,26?/m1/s1
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n/an/a 10.6n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468975
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C25H23Cl2F3N6O4/c26-13-5-12(21(30)17(27)6-13)9-32-23(37)25(39)3-4-35(24(25)38)20-10-33-36(34-20)15-8-19(31)22(40-11-15)16-7-14(28)1-2-18(16)29/h1-2,5-7,10,15,19,22,39H,3-4,8-9,11,31H2,(H,32,37)/t15-,19+,22-,25?/m1/s1
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n/an/a 12.8n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468978
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C26H24F5N5O4/c27-14-1-2-18(29)17(8-14)23-20(32)10-16(12-40-23)36-5-3-21(34-36)35-6-4-26(39,25(35)38)24(37)33-11-13-7-15(28)9-19(30)22(13)31/h1-3,5,7-9,16,20,23,39H,4,6,10-12,32H2,(H,33,37)/t16-,20+,23-,26?/m1/s1
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n/an/a 13.1n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468981
PNG
((3S)-1-[2-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluoroph...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCC(=CC1)c1ncc(cn1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C32H32ClF3N6O4/c33-20-9-18(10-22(35)11-20)14-40-30(43)32(45)5-8-42(31(32)44)24-15-38-29(39-16-24)19-3-6-41(7-4-19)23-13-27(37)28(46-17-23)25-12-21(34)1-2-26(25)36/h1-3,9-12,15-16,23,27-28,45H,4-8,13-14,17,37H2,(H,40,43)/t23-,27+,28-,32+/m1/s1
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n/an/a 14.7n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468977
PNG
(1-[2-[(3R,5S,6R)-5-Aamino- 6-(2,5- difluorophenyl)...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C26H24Cl2F3N5O4/c27-14-7-13(22(31)18(28)8-14)11-33-24(37)26(39)4-6-35(25(26)38)21-3-5-36(34-21)16-10-20(32)23(40-12-16)17-9-15(29)1-2-19(17)30/h1-3,5,7-9,16,20,23,39H,4,6,10-12,32H2,(H,33,37)/t16-,20+,23-,26?/m1/s1
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n/an/a 15n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468959
PNG
(1-[2-[4-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C31H33F4N7O4/c32-19-4-5-23(33)22(12-19)27-25(36)13-20(17-46-27)40-8-10-41(11-9-40)30-38-15-21(16-39-30)42-7-6-31(45,29(42)44)28(43)37-14-18-2-1-3-24(34)26(18)35/h1-5,12,15-16,20,25,27,45H,6-11,13-14,17,36H2,(H,37,43)/t20-,25+,27-,31?/m1/s1
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n/an/a 16.4n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468960
PNG
(1-[2-[4-[(3R,5S,6R)-5- Amino-6-(2,5- difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C31H32F5N7O4/c32-18-1-2-23(34)22(10-18)27-25(37)12-20(16-47-27)41-5-7-42(8-6-41)30-39-14-21(15-40-30)43-4-3-31(46,29(43)45)28(44)38-13-17-9-19(33)11-24(35)26(17)36/h1-2,9-11,14-15,20,25,27,46H,3-8,12-13,16,37H2,(H,38,44)/t20-,25+,27-,31?/m1/s1
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n/an/a 16.5n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Homo sapiens (Human))
BDBM468961
PNG
((3S)-1-[6-[4-[(3S,5S,6R)-5-Amino-6-(2,5-difluoroph...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ccc(cn1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C32H34ClF3N6O4/c33-20-11-19(12-22(35)13-20)16-39-30(43)32(45)5-6-42(31(32)44)23-2-4-28(38-17-23)41-9-7-40(8-10-41)24-15-27(37)29(46-18-24)25-14-21(34)1-3-26(25)36/h1-4,11-14,17,24,27,29,45H,5-10,15-16,18,37H2,(H,39,43)/t24-,27+,29-,32+/m1/s1
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n/an/a 17.5n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468980
PNG
(1-[1-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cccc(F)c2)C1=O
Show InChI InChI=1S/C26H26F3N5O4/c27-16-3-1-2-15(10-16)13-31-24(35)26(37)7-9-33(25(26)36)22-6-8-34(32-22)18-12-21(30)23(38-14-18)19-11-17(28)4-5-20(19)29/h1-6,8,10-11,18,21,23,37H,7,9,12-14,30H2,(H,31,35)/t18-,21+,23-,26?/m1/s1
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n/an/a 18.6n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468975
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C25H23Cl2F3N6O4/c26-13-5-12(21(30)17(27)6-13)9-32-23(37)25(39)3-4-35(24(25)38)20-10-33-36(34-20)15-8-19(31)22(40-11-15)16-7-14(28)1-2-18(16)29/h1-2,5-7,10,15,19,22,39H,3-4,8-9,11,31H2,(H,32,37)/t15-,19+,22-,25?/m1/s1
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n/an/a 20.8n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468957
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2ccc(cc2C1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C31H29F5N4O4/c32-19-2-4-24(34)23(9-19)28-26(37)11-22(15-44-28)39-13-16-1-3-21(8-18(16)14-39)40-6-5-31(43,30(40)42)29(41)38-12-17-7-20(33)10-25(35)27(17)36/h1-4,7-10,22,26,28,43H,5-6,11-15,37H2,(H,38,41)/t22-,26+,28-,31?/m1/s1
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n/an/a 21.9n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468981
PNG
((3S)-1-[2-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluoroph...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCC(=CC1)c1ncc(cn1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C32H32ClF3N6O4/c33-20-9-18(10-22(35)11-20)14-40-30(43)32(45)5-8-42(31(32)44)24-15-38-29(39-16-24)19-3-6-41(7-4-19)23-13-27(37)28(46-17-23)25-12-21(34)1-2-26(25)36/h1-3,9-12,15-16,23,27-28,45H,4-8,13-14,17,37H2,(H,40,43)/t23-,27+,28-,32+/m1/s1
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n/an/a 25.5n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468961
PNG
((3S)-1-[6-[4-[(3S,5S,6R)-5-Amino-6-(2,5-difluoroph...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ccc(cn1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C32H34ClF3N6O4/c33-20-11-19(12-22(35)13-20)16-39-30(43)32(45)5-6-42(31(32)44)23-2-4-28(38-17-23)41-9-7-40(8-10-41)24-15-27(37)29(46-18-24)25-14-21(34)1-3-26(25)36/h1-4,11-14,17,24,27,29,45H,5-10,15-16,18,37H2,(H,39,43)/t24-,27+,29-,32+/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468978
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C26H24F5N5O4/c27-14-1-2-18(29)17(8-14)23-20(32)10-16(12-40-23)36-5-3-21(34-36)35-6-4-26(39,25(35)38)24(37)33-11-13-7-15(28)9-19(30)22(13)31/h1-3,5,7-9,16,20,23,39H,4,6,10-12,32H2,(H,33,37)/t16-,20+,23-,26?/m1/s1
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n/an/a 29.2n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468979
PNG
(1-[1-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2)C1=O
Show InChI InChI=1S/C26H25F4N5O4/c27-15-1-2-20(30)19(10-15)23-21(31)11-18(13-39-23)35-5-3-22(33-35)34-6-4-26(38,25(34)37)24(36)32-12-14-7-16(28)9-17(29)8-14/h1-3,5,7-10,18,21,23,38H,4,6,11-13,31H2,(H,32,36)/t18-,21+,23-,26?/m1/s1
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n/an/a 30.5n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468960
PNG
(1-[2-[4-[(3R,5S,6R)-5- Amino-6-(2,5- difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C31H32F5N7O4/c32-18-1-2-23(34)22(10-18)27-25(37)12-20(16-47-27)41-5-7-42(8-6-41)30-39-14-21(15-40-30)43-4-3-31(46,29(43)45)28(44)38-13-17-9-19(33)11-24(35)26(17)36/h1-2,9-11,14-15,20,25,27,46H,3-8,12-13,16,37H2,(H,38,44)/t20-,25+,27-,31?/m1/s1
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n/an/a 30.7n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468976
PNG
((3S)-1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C26H25ClF3N5O4/c27-15-7-14(8-17(29)9-15)12-32-24(36)26(38)4-6-34(25(26)37)22-3-5-35(33-22)18-11-21(31)23(39-13-18)19-10-16(28)1-2-20(19)30/h1-3,5,7-10,18,21,23,38H,4,6,11-13,31H2,(H,32,36)/t18-,21+,23-,26+/m1/s1
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n/an/a 32.1n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Dipeptidyl peptidase 4


(Mus musculus)
BDBM468959
PNG
(1-[2-[4-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C31H33F4N7O4/c32-19-4-5-23(33)22(12-19)27-25(36)13-20(17-46-27)40-8-10-41(11-9-40)30-38-15-21(16-39-30)42-7-6-31(45,29(42)44)28(43)37-14-18-2-1-3-24(34)26(18)35/h1-5,12,15-16,20,25,27,45H,6-11,13-14,17,36H2,(H,37,43)/t20-,25+,27-,31?/m1/s1
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n/an/a 32.5n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
Human DPP-4 ((39-766)-His) and mouse DPP-4 ((29-760)-His) are purified by gel chromatography for use in the assay. The final concentration of hDPP-4 ...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468978
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C26H24F5N5O4/c27-14-1-2-18(29)17(8-14)23-20(32)10-16(12-40-23)36-5-3-21(34-36)35-6-4-26(39,25(35)38)24(37)33-11-13-7-15(28)9-19(30)22(13)31/h1-3,5,7-9,16,20,23,39H,4,6,10-12,32H2,(H,33,37)/t16-,20+,23-,26?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468958
PNG
(1-[2-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2ccc(cc2C1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C31H30F4N4O4/c32-20-5-7-24(33)23(11-20)28-26(36)12-22(16-43-28)38-14-18-4-6-21(10-19(18)15-38)39-9-8-31(42,30(39)41)29(40)37-13-17-2-1-3-25(34)27(17)35/h1-7,10-11,22,26,28,42H,8-9,12-16,36H2,(H,37,40)/t22-,26+,28-,31?/m1/s1
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n/an/a 33.6n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468964
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1cc(cn1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C26H24Cl2F3N5O4/c27-14-5-13(22(31)19(28)6-14)9-33-24(37)26(39)3-4-35(25(26)38)17-10-34-36(11-17)16-8-21(32)23(40-12-16)18-7-15(29)1-2-20(18)30/h1-2,5-7,10-11,16,21,23,39H,3-4,8-9,12,32H2,(H,33,37)/t16-,21+,23-,26?/m1/s1
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n/an/a 36.8n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468972
PNG
((3S)-1-[2-[(3R,5S,6R)-5-Amino-6-(2,5-difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C25H24ClF3N6O4/c26-14-5-13(6-16(28)7-14)10-31-23(36)25(38)3-4-34(24(25)37)21-11-32-35(33-21)17-9-20(30)22(39-12-17)18-8-15(27)1-2-19(18)29/h1-2,5-8,11,17,20,22,38H,3-4,9-10,12,30H2,(H,31,36)/t17-,20+,22-,25+/m1/s1
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n/an/a 48n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468957
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2ccc(cc2C1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C31H29F5N4O4/c32-19-2-4-24(34)23(9-19)28-26(37)11-22(15-44-28)39-13-16-1-3-21(8-18(16)14-39)40-6-5-31(43,30(40)42)29(41)38-12-17-7-20(33)10-25(35)27(17)36/h1-4,7-10,22,26,28,43H,5-6,11-15,37H2,(H,38,41)/t22-,26+,28-,31?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468979
PNG
(1-[1-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2)C1=O
Show InChI InChI=1S/C26H25F4N5O4/c27-15-1-2-20(30)19(10-15)23-21(31)11-18(13-39-23)35-5-3-22(33-35)34-6-4-26(38,25(34)37)24(36)32-12-14-7-16(28)9-17(29)8-14/h1-3,5,7-10,18,21,23,38H,4,6,11-13,31H2,(H,32,36)/t18-,21+,23-,26?/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468976
PNG
((3S)-1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C26H25ClF3N5O4/c27-15-7-14(8-17(29)9-15)12-32-24(36)26(38)4-6-34(25(26)37)22-3-5-35(33-22)18-11-21(31)23(39-13-18)19-10-16(28)1-2-20(19)30/h1-3,5,7-10,18,21,23,38H,4,6,11-13,31H2,(H,32,36)/t18-,21+,23-,26+/m1/s1
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Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468980
PNG
(1-[1-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cccc(F)c2)C1=O
Show InChI InChI=1S/C26H26F3N5O4/c27-16-3-1-2-15(10-16)13-31-24(35)26(37)7-9-33(25(26)36)22-6-8-34(32-22)18-12-21(30)23(38-14-18)19-11-17(28)4-5-20(19)29/h1-6,8,10-11,18,21,23,37H,7,9,12-14,30H2,(H,31,35)/t18-,21+,23-,26?/m1/s1
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n/an/a 60.3n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468958
PNG
(1-[2-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1Cc2ccc(cc2C1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C31H30F4N4O4/c32-20-5-7-24(33)23(11-20)28-26(36)12-22(16-43-28)38-14-18-4-6-21(10-19(18)15-38)39-9-8-31(42,30(39)41)29(40)37-13-17-2-1-3-25(34)27(17)35/h1-7,10-11,22,26,28,42H,8-9,12-16,36H2,(H,37,40)/t22-,26+,28-,31?/m1/s1
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n/an/a 68n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468961
PNG
((3S)-1-[6-[4-[(3S,5S,6R)-5-Amino-6-(2,5-difluoroph...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ccc(cn1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C32H34ClF3N6O4/c33-20-11-19(12-22(35)13-20)16-39-30(43)32(45)5-6-42(31(32)44)23-2-4-28(38-17-23)41-9-7-40(8-10-41)24-15-27(37)29(46-18-24)25-14-21(34)1-3-26(25)36/h1-4,11-14,17,24,27,29,45H,5-10,15-16,18,37H2,(H,39,43)/t24-,27+,29-,32+/m1/s1
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n/an/a 80.2n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468964
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1cc(cn1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2F)C1=O
Show InChI InChI=1S/C26H24Cl2F3N5O4/c27-14-5-13(22(31)19(28)6-14)9-33-24(37)26(39)3-4-35(25(26)38)17-10-34-36(11-17)16-8-21(32)23(40-12-16)18-7-15(29)1-2-20(18)30/h1-2,5-7,10-11,16,21,23,39H,3-4,8-9,12,32H2,(H,33,37)/t16-,21+,23-,26?/m1/s1
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n/an/a 81.4n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468974
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C25H23F5N6O4/c26-13-1-2-17(28)16(6-13)22-19(31)8-15(11-40-22)36-33-10-20(34-36)35-4-3-25(39,24(35)38)23(37)32-9-12-5-14(27)7-18(29)21(12)30/h1-2,5-7,10,15,19,22,39H,3-4,8-9,11,31H2,(H,32,37)/t15-,19+,22-,25?/m1/s1
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n/an/a 94.7n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468972
PNG
((3S)-1-[2-[(3R,5S,6R)-5-Amino-6-(2,5-difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C25H24ClF3N6O4/c26-14-5-13(6-16(28)7-14)10-31-23(36)25(38)3-4-34(24(25)37)21-11-32-35(33-21)17-9-20(30)22(39-12-17)18-8-15(27)1-2-19(18)29/h1-2,5-8,11,17,20,22,38H,3-4,9-10,12,30H2,(H,31,36)/t17-,20+,22-,25+/m1/s1
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n/an/a 95.2n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468959
PNG
(1-[2-[4-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C31H33F4N7O4/c32-19-4-5-23(33)22(12-19)27-25(36)13-20(17-46-27)40-8-10-41(11-9-40)30-38-15-21(16-39-30)42-7-6-31(45,29(42)44)28(43)37-14-18-2-1-3-24(34)26(18)35/h1-5,12,15-16,20,25,27,45H,6-11,13-14,17,36H2,(H,37,43)/t20-,25+,27-,31?/m1/s1
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n/an/a 103n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468980
PNG
(1-[1-[(3R,5S,6R)-5-Amino- 6-(2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ccc(n1)N1CCC(O)(C(=O)NCc2cccc(F)c2)C1=O
Show InChI InChI=1S/C26H26F3N5O4/c27-16-3-1-2-15(10-16)13-31-24(35)26(37)7-9-33(25(26)36)22-6-8-34(32-22)18-12-21(30)23(38-14-18)19-11-17(28)4-5-20(19)29/h1-6,8,10-11,18,21,23,37H,7,9,12-14,30H2,(H,31,35)/t18-,21+,23-,26?/m1/s1
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n/an/a 106n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468960
PNG
(1-[2-[4-[(3R,5S,6R)-5- Amino-6-(2,5- difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C31H32F5N7O4/c32-18-1-2-23(34)22(10-18)27-25(37)12-20(16-47-27)41-5-7-42(8-6-41)30-39-14-21(15-40-30)43-4-3-31(46,29(43)45)28(44)38-13-17-9-19(33)11-24(35)26(17)36/h1-2,9-11,14-15,20,25,27,46H,3-8,12-13,16,37H2,(H,38,44)/t20-,25+,27-,31?/m1/s1
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n/an/a 111n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468963
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1cc(cn1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2)C1=O
Show InChI InChI=1S/C26H25Cl2F2N5O4/c27-15-5-14(6-16(28)7-15)10-32-24(36)26(38)3-4-34(25(26)37)19-11-33-35(12-19)18-9-22(31)23(39-13-18)20-8-17(29)1-2-21(20)30/h1-2,5-8,11-12,18,22-23,38H,3-4,9-10,13,31H2,(H,32,36)/t18-,22+,23-,26?/m1/s1
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n/an/a 123n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468961
PNG
((3S)-1-[6-[4-[(3S,5S,6R)-5-Amino-6-(2,5-difluoroph...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ccc(cn1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C32H34ClF3N6O4/c33-20-11-19(12-22(35)13-20)16-39-30(43)32(45)5-6-42(31(32)44)23-2-4-28(38-17-23)41-9-7-40(8-10-41)24-15-27(37)29(46-18-24)25-14-21(34)1-3-26(25)36/h1-4,11-14,17,24,27,29,45H,5-10,15-16,18,37H2,(H,39,43)/t24-,27+,29-,32+/m1/s1
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n/an/a 125n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468960
PNG
(1-[2-[4-[(3R,5S,6R)-5- Amino-6-(2,5- difluoropheny...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C31H32F5N7O4/c32-18-1-2-23(34)22(10-18)27-25(37)12-20(16-47-27)41-5-7-42(8-6-41)30-39-14-21(15-40-30)43-4-3-31(46,29(43)45)28(44)38-13-17-9-19(33)11-24(35)26(17)36/h1-2,9-11,14-15,20,25,27,46H,3-8,12-13,16,37H2,(H,38,44)/t20-,25+,27-,31?/m1/s1
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n/an/a 125n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468973
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C25H24F4N6O4/c26-14-4-5-17(27)16(8-14)22-19(30)9-15(12-39-22)35-32-11-20(33-35)34-7-6-25(38,24(34)37)23(36)31-10-13-2-1-3-18(28)21(13)29/h1-5,8,11,15,19,22,38H,6-7,9-10,12,30H2,(H,31,36)/t15-,19+,22-,25?/m1/s1
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n/an/a 154n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468959
PNG
(1-[2-[4-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCN(CC1)c1ncc(cn1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C31H33F4N7O4/c32-19-4-5-23(33)22(12-19)27-25(36)13-20(17-46-27)40-8-10-41(11-9-40)30-38-15-21(16-39-30)42-7-6-31(45,29(42)44)28(43)37-14-18-2-1-3-24(34)26(18)35/h1-5,12,15-16,20,25,27,45H,6-11,13-14,17,36H2,(H,37,43)/t20-,25+,27-,31?/m1/s1
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n/an/a 155n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468974
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cc(F)cc(F)c2F)C1=O
Show InChI InChI=1S/C25H23F5N6O4/c26-13-1-2-17(28)16(6-13)22-19(31)8-15(11-40-22)36-33-10-20(34-36)35-4-3-25(39,24(35)38)23(37)32-9-12-5-14(27)7-18(29)21(12)30/h1-2,5-7,10,15,19,22,39H,3-4,8-9,11,31H2,(H,32,37)/t15-,19+,22-,25?/m1/s1
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n/an/a 204n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468963
PNG
(1-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluorophenyl)tet...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1cc(cn1)N1CCC(O)(C(=O)NCc2cc(Cl)cc(Cl)c2)C1=O
Show InChI InChI=1S/C26H25Cl2F2N5O4/c27-15-5-14(6-16(28)7-15)10-32-24(36)26(38)3-4-34(25(26)37)19-11-33-35(12-19)18-9-22(31)23(39-13-18)20-8-17(29)1-2-21(20)30/h1-2,5-8,11-12,18,22-23,38H,3-4,9-10,13,31H2,(H,32,36)/t18-,22+,23-,26?/m1/s1
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n/an/a 261n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Mus musculus (Mouse))
BDBM468981
PNG
((3S)-1-[2-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluoroph...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCC(=CC1)c1ncc(cn1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C32H32ClF3N6O4/c33-20-9-18(10-22(35)11-20)14-40-30(43)32(45)5-8-42(31(32)44)24-15-38-29(39-16-24)19-3-6-41(7-4-19)23-13-27(37)28(46-17-23)25-12-21(34)1-2-26(25)36/h1-3,9-12,15-16,23,27-28,45H,4-8,13-14,17,37H2,(H,40,43)/t23-,27+,28-,32+/m1/s1
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n/an/a 283n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468973
PNG
(1-[2-[(3R,5S,6R)-5-Amino-6- (2,5- difluorophenyl)t...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)n1ncc(n1)N1CCC(O)(C(=O)NCc2cccc(F)c2F)C1=O
Show InChI InChI=1S/C25H24F4N6O4/c26-14-4-5-17(27)16(8-14)22-19(30)9-15(12-39-22)35-32-11-20(33-35)34-7-6-25(38,24(34)37)23(36)31-10-13-2-1-3-18(28)21(13)29/h1-5,8,11,15,19,22,38H,6-7,9-10,12,30H2,(H,31,36)/t15-,19+,22-,25?/m1/s1
PDB
MMDB

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PC sid
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US Patent
n/an/a 293n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
Methionine aminopeptidase 2


(Homo sapiens (Human))
BDBM468981
PNG
((3S)-1-[2-[1-[(3R,5S,6R)-5-Amino-6-(2,5-difluoroph...)
Show SMILES N[C@H]1C[C@H](CO[C@@H]1c1cc(F)ccc1F)N1CCC(=CC1)c1ncc(cn1)N1CC[C@](O)(C(=O)NCc2cc(F)cc(Cl)c2)C1=O
Show InChI InChI=1S/C32H32ClF3N6O4/c33-20-9-18(10-22(35)11-20)14-40-30(43)32(45)5-8-42(31(32)44)24-15-38-29(39-16-24)19-3-6-41(7-4-19)23-13-27(37)28(46-17-23)25-12-21(34)1-2-26(25)36/h1-3,9-12,15-16,23,27-28,45H,4-8,13-14,17,37H2,(H,40,43)/t23-,27+,28-,32+/m1/s1
PDB
MMDB

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PC cid
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UniChem
US Patent
n/an/a 430n/an/an/an/an/an/a



Eli Lilly and Company

US Patent


Assay Description
The compounds exemplified herein are tested essentially as described below and exhibit an IC50 for the human and mouse MetAP2 assay as shown in Table...


US Patent US10807971 (2020)

More data for this
Ligand-Target Pair
* indicates data uncertainty>20%