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Compile Data Set for Download or QSAR

Found 1032 hits Enz. Inhib. hit(s) with Target = 'Transient receptor potential M8 protein (TRPM8)' AND taxid = 9615   
Target
(Institution)
LigandTarget
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
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248583
PNG
(US9434711, 496)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H18F3NO5S2/c1-15-20-4-2-3-5-21(20)34-22(15)28(14-16-6-10-18(11-7-16)33-24(25,26)27)35(31,32)19-12-8-17(9-13-19)23(29)30/h2-13H,14H2,1H3,(H,29,30)
KEGG

UniProtKB/TrEMBL

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US Patent
n/an/a 0.183n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
For patch clamp experiments, HEK293 cells are stably transfected with canine TRPM8 and cultured in DMEM supplemented with 10% fetal bovine serum, 100...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335165
PNG
(3-[2-(1-Oxa-2-aza-spiro[4.5]dec-2-en-3-yl)-6-(2-tr...)
Show SMILES OCCCc1cc(cc2[nH]c(nc12)C1=NOC2(C1)CCCCC2)-c1ccccc1C(F)(F)F
Show InChI InChI=1S/C25H26F3N3O2/c26-25(27,28)19-9-3-2-8-18(19)17-13-16(7-6-12-32)22-20(14-17)29-23(30-22)21-15-24(33-31-21)10-4-1-5-11-24/h2-3,8-9,13-14,32H,1,4-7,10-12,15H2,(H,29,30)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.200n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50036555
PNG
(CHEMBL3353610 | US9434711, 497)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(c(F)c1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H17F4NO4S2/c1-14-18-4-2-3-5-21(18)34-22(14)29(13-15-6-11-19(20(25)12-15)24(26,27)28)35(32,33)17-9-7-16(8-10-17)23(30)31/h2-12H,13H2,1H3,(H,30,31)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.400n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241685
PNG
(US9409915, 89)
Show SMILES Cn1nc(c(Cl)c1-c1nc2cc(nc(OCC(F)(F)F)c2[nH]1)-c1ccccc1Cl)C(C)(C)C
Show InChI InChI=1S/C22H20Cl2F3N5O/c1-21(2,3)18-15(24)17(32(4)31-18)19-28-14-9-13(11-7-5-6-8-12(11)23)29-20(16(14)30-19)33-10-22(25,26)27/h5-9H,10H2,1-4H3,(H,28,30)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.530n/an/an/an/an/an/a



Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248583
PNG
(US9434711, 496)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H18F3NO5S2/c1-15-20-4-2-3-5-21(20)34-22(15)28(14-16-6-10-18(11-7-16)33-24(25,26)27)35(31,32)19-12-8-17(9-13-19)23(29)30/h2-13H,14H2,1H3,(H,29,30)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.554n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
For patch clamp experiments, HEK293 cells are stably transfected with canine TRPM8 and cultured in DMEM supplemented with 10% fetal bovine serum, 100...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241633
PNG
(US9409915, 16)
Show SMILES CC(C)Oc1nc(cc2nc([nH]c12)-c1c(Cl)c(nn1C)C(C)(C)C)-c1ccccc1C(F)(F)F
Show InChI InChI=1S/C24H25ClF3N5O/c1-12(2)34-22-18-16(11-15(30-22)13-9-7-8-10-14(13)24(26,27)28)29-21(31-18)19-17(25)20(23(3,4)5)32-33(19)6/h7-12H,1-6H3,(H,29,31)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.590n/an/an/an/an/an/a



Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335170
PNG
(3-[5-(2-Fluoro-6-trifluoromethylphenyl)-1H-benzimi...)
Show SMILES Fc1cccc(c1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCCCC2)C(F)(F)F
Show InChI InChI=1S/C22H19F4N3O/c23-15-6-4-5-14(22(24,25)26)19(15)13-7-8-16-17(11-13)28-20(27-16)18-12-21(30-29-18)9-2-1-3-10-21/h4-8,11H,1-3,9-10,12H2,(H,27,28)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.600n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248576
PNG
(US9434711, 489)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(F)c(Cl)c1)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C23H17ClFNO4S2/c1-14-18-4-2-3-5-21(18)31-22(14)26(13-15-6-11-20(25)19(24)12-15)32(29,30)17-9-7-16(8-10-17)23(27)28/h2-12H,13H2,1H3,(H,27,28)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.600n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248370
PNG
(US9434711, 227)
Show SMILES CCS(=O)(=O)N(Cc1ccc(F)c(c1)C(F)(F)F)c1sc2ccccc2c1C(C)(C)O
Show InChI InChI=1S/C21H21F4NO3S2/c1-4-31(28,29)26(12-13-9-10-16(22)15(11-13)21(23,24)25)19-18(20(2,3)27)14-7-5-6-8-17(14)30-19/h5-11,27H,4,12H2,1-3H3
KEGG

UniProtKB/TrEMBL

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n/an/a 0.600n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241638
PNG
(US9409915, 21)
Show SMILES COCCOc1nc(cc2nc([nH]c12)-c1c(C#N)c(nn1C)C(C)(C)C)-c1ccccc1C(F)(F)F
Show InChI InChI=1S/C25H25F3N6O2/c1-24(2,3)21-15(13-29)20(34(4)33-21)22-30-18-12-17(14-8-6-7-9-16(14)25(26,27)28)31-23(19(18)32-22)36-11-10-35-5/h6-9,12H,10-11H2,1-5H3,(H,30,32)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.690n/an/an/an/an/an/a



Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335160
PNG
(2-(1-Oxa-2-aza-spiro[4.5]dec-2-en-3-yl)-6-(2-trifl...)
Show SMILES FC(F)(F)c1ccccc1-c1cc(C#N)c2[nH]c(nc2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C23H19F3N4O/c24-23(25,26)17-7-3-2-6-16(17)14-10-15(13-27)20-18(11-14)28-21(29-20)19-12-22(31-30-19)8-4-1-5-9-22/h2-3,6-7,10-11H,1,4-5,8-9,12H2,(H,28,29)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.700n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248838
PNG
(US9434711, 808)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(nc1)-c1noc(=O)[nH]1
Show InChI InChI=1S/C24H17F3N4O5S2/c1-14-18-4-2-3-5-20(18)37-22(14)31(13-15-6-8-16(9-7-15)35-24(25,26)27)38(33,34)17-10-11-19(28-12-17)21-29-23(32)36-30-21/h2-12H,13H2,1H3,(H,29,30,32)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.700n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248599
PNG
(US9434711, 518)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(cc1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H18F3NO4S2/c1-15-20-4-2-3-5-21(20)33-22(15)28(14-16-6-10-18(11-7-16)24(25,26)27)34(31,32)19-12-8-17(9-13-19)23(29)30/h2-13H,14H2,1H3,(H,29,30)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.700n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241686
PNG
(US9409915, 90)
Show SMILES Cn1nc(c(Cl)c1-c1nc2cc(nc(OCC(F)(F)F)c2[nH]1)-c1ccccc1OC(F)(F)F)C(C)(C)C
Show InChI InChI=1S/C23H20ClF6N5O2/c1-21(2,3)18-15(24)17(35(4)34-18)19-31-13-9-12(11-7-5-6-8-14(11)37-23(28,29)30)32-20(16(13)33-19)36-10-22(25,26)27/h5-9H,10H2,1-4H3,(H,31,33)
KEGG

UniProtKB/TrEMBL

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US Patent
n/an/a 0.730n/an/an/an/an/an/a



Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335171
PNG
(3-[5-(2-Fluoro-6-trifluoromethoxyphenyl)-1H-benzim...)
Show SMILES Fc1cccc(OC(F)(F)F)c1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C22H19F4N3O2/c23-14-5-4-6-18(30-22(24,25)26)19(14)13-7-8-15-16(11-13)28-20(27-15)17-12-21(31-29-17)9-2-1-3-10-21/h4-8,11H,1-3,9-10,12H2,(H,27,28)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.800n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50426573
PNG
(CHEMBL2324349 | US9434711, 306)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(F)c(c1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H17F4NO4S2/c1-14-18-4-2-3-5-21(18)34-22(14)29(13-15-6-11-20(25)19(12-15)24(26,27)28)35(32,33)17-9-7-16(8-10-17)23(30)31/h2-12H,13H2,1H3,(H,30,31)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.800n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248583
PNG
(US9434711, 496)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H18F3NO5S2/c1-15-20-4-2-3-5-21(20)34-22(15)28(14-16-6-10-18(11-7-16)33-24(25,26)27)35(31,32)19-12-8-17(9-13-19)23(29)30/h2-13H,14H2,1H3,(H,29,30)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.800n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248580
PNG
(US9434711, 493)
Show SMILES Cc1c(sc2ccccc12)N(Cc1c(F)c(F)c(F)c(F)c1F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C23H14F5NO4S2/c1-11-14-4-2-3-5-16(14)34-22(11)29(10-15-17(24)19(26)21(28)20(27)18(15)25)35(32,33)13-8-6-12(7-9-13)23(30)31/h2-9H,10H2,1H3,(H,30,31)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.800n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335157
PNG
(3-[7-Trifluoromethyl-5-(2-trifluoromethyl-phenyl)-...)
Show SMILES FC(F)(F)c1ccccc1-c1cc(c2[nH]c(nc2c1)C1=NOC2(C1)CCCCC2)C(F)(F)F
Show InChI InChI=1S/C23H19F6N3O/c24-22(25,26)15-7-3-2-6-14(15)13-10-16(23(27,28)29)19-17(11-13)30-20(31-19)18-12-21(33-32-18)8-4-1-5-9-21/h2-3,6-7,10-11H,1,4-5,8-9,12H2,(H,30,31)
KEGG

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TBA

Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248480
PNG
(US9434711, 361)
Show SMILES CC(C)(O)c1c(sc2ccccc12)N(Cc1ccc(F)c(c1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C26H21F4NO5S2/c1-25(2,34)22-18-5-3-4-6-21(18)37-23(22)31(14-15-7-12-20(27)19(13-15)26(28,29)30)38(35,36)17-10-8-16(9-11-17)24(32)33/h3-13,34H,14H2,1-2H3,(H,32,33)
KEGG

UniProtKB/TrEMBL

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US Patent
n/an/a 0.800n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248426
PNG
(US9434711, 292)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc(F)c(c1)C(F)(F)F)c1sc2ccccc2c1Br
Show InChI InChI=1S/C23H14BrF4NO4S2/c24-20-16-3-1-2-4-19(16)34-21(20)29(12-13-5-10-18(25)17(11-13)23(26,27)28)35(32,33)15-8-6-14(7-9-15)22(30)31/h1-11H,12H2,(H,30,31)
KEGG

UniProtKB/TrEMBL

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n/an/a 0.800n/an/an/an/an/an/a



Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241636
PNG
(US9409915, 19)
Show SMILES Cn1nc(c(Cl)c1-c1nc2cc(nc(OCC(F)(F)F)c2[nH]1)-c1ccccc1C(F)(F)F)C(C)(C)C
Show InChI InChI=1S/C23H20ClF6N5O/c1-21(2,3)18-15(24)17(35(4)34-18)19-31-14-9-13(11-7-5-6-8-12(11)23(28,29)30)32-20(16(14)33-19)36-10-22(25,26)27/h5-9H,10H2,1-4H3,(H,31,33)
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Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248789
PNG
(US9434711, 755)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1sc2ccccc2c1C1CC1
Show InChI InChI=1S/C26H20F3NO5S2/c27-26(28,29)35-19-11-5-16(6-12-19)15-30(37(33,34)20-13-9-18(10-14-20)25(31)32)24-23(17-7-8-17)21-3-1-2-4-22(21)36-24/h1-6,9-14,17H,7-8,15H2,(H,31,32)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248581
PNG
(US9434711, 494)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(cc1)S(=O)(=O)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H18F3NO6S3/c1-15-20-4-2-3-5-21(20)35-22(15)28(37(33,34)19-12-8-17(9-13-19)23(29)30)14-16-6-10-18(11-7-16)36(31,32)24(25,26)27/h2-13H,14H2,1H3,(H,29,30)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248389
PNG
(US9434711, 249)
Show SMILES Brc1c(sc2ccccc12)N(CC12CC3CC(CC(C3)C1)C2)S(=O)(=O)c1ccccc1
Show InChI InChI=1S/C25H26BrNO2S2/c26-23-21-8-4-5-9-22(21)30-24(23)27(31(28,29)20-6-2-1-3-7-20)16-25-13-17-10-18(14-25)12-19(11-17)15-25/h1-9,17-19H,10-16H2
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335173
PNG
(8,8-Difluoro-3-[5-(2-trifluoromethylphenyl)-1H-ben...)
Show SMILES FC(F)(F)c1ccccc1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCC(F)(F)CC2
Show InChI InChI=1S/C22H18F5N3O/c23-21(24)9-7-20(8-10-21)12-18(30-31-20)19-28-16-6-5-13(11-17(16)29-19)14-3-1-2-4-15(14)22(25,26)27/h1-6,11H,7-10,12H2,(H,28,29)
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Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241637
PNG
(US9409915, 20)
Show SMILES COCCOc1nc(cc2nc([nH]c12)-c1c(Cl)c(nn1C)C(C)(C)C)-c1ccccc1C(F)(F)F
Show InChI InChI=1S/C24H25ClF3N5O2/c1-23(2,3)20-17(25)19(33(4)32-20)21-29-16-12-15(13-8-6-7-9-14(13)24(26,27)28)30-22(18(16)31-21)35-11-10-34-5/h6-9,12H,10-11H2,1-5H3,(H,29,31)
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Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248367
PNG
(US9434711, 224)
Show SMILES CC(O)c1c(sc2ccccc12)N(Cc1ccc(F)c(c1)C(F)(F)F)S(C)(=O)=O
Show InChI InChI=1/C19H17F4NO3S2/c1-11(25)17-13-5-3-4-6-16(13)28-18(17)24(29(2,26)27)10-12-7-8-15(20)14(9-12)19(21,22)23/h3-9,11,25H,10H2,1-2H3
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248613
PNG
(US9434711, 535)
Show SMILES CCS(=O)(=O)N(Cc1ccc(F)c(c1)C(F)(F)F)c1sc2ccccc2c1[C@@H](C)O
Show InChI InChI=1S/C20H19F4NO3S2/c1-3-30(27,28)25(11-13-8-9-16(21)15(10-13)20(22,23)24)19-18(12(2)26)14-6-4-5-7-17(14)29-19/h4-10,12,26H,3,11H2,1-2H3/t12-/m1/s1
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248607
PNG
(US9434711, 526)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(SC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H18F3NO4S3/c1-15-20-4-2-3-5-21(20)33-22(15)28(14-16-6-10-18(11-7-16)34-24(25,26)27)35(31,32)19-12-8-17(9-13-19)23(29)30/h2-13H,14H2,1H3,(H,29,30)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248840
PNG
(US9434711, 810)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)-c1nsc(=O)[nH]1
Show InChI InChI=1S/C25H18F3N3O4S3/c1-15-20-4-2-3-5-21(20)36-23(15)31(14-16-6-10-18(11-7-16)35-25(26,27)28)38(33,34)19-12-8-17(9-13-19)22-29-24(32)37-30-22/h2-13H,14H2,1H3,(H,29,30,32)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335164
PNG
(3-[5-(2-Chlorophenyl)-7-trifluoromethyl-1H-benzimi...)
Show SMILES FC(F)(F)c1cc(cc2nc([nH]c12)C1=NOC2(C1)CCCCC2)-c1ccccc1Cl
Show InChI InChI=1S/C22H19ClF3N3O/c23-16-7-3-2-6-14(16)13-10-15(22(24,25)26)19-17(11-13)27-20(28-19)18-12-21(30-29-18)8-4-1-5-9-21/h2-3,6-7,10-11H,1,4-5,8-9,12H2,(H,27,28)
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Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248414
PNG
(US9434711, 278)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(CC12CC3CC(CC(C3)C1)C2)c1sc2ccccc2c1Br
Show InChI InChI=1S/C26H26BrNO4S2/c27-23-21-3-1-2-4-22(21)33-24(23)28(34(31,32)20-7-5-19(6-8-20)25(29)30)15-26-12-16-9-17(13-26)11-18(10-16)14-26/h1-8,16-18H,9-15H2,(H,29,30)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248575
PNG
(US9434711, 488)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(F)c(F)c1)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C23H17F2NO4S2/c1-14-18-4-2-3-5-21(18)31-22(14)26(13-15-6-11-19(24)20(25)12-15)32(29,30)17-9-7-16(8-10-17)23(27)28/h2-12H,13H2,1H3,(H,27,28)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248577
PNG
(US9434711, 490)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)F)cc1)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H19F2NO5S2/c1-15-20-4-2-3-5-21(20)33-22(15)27(14-16-6-10-18(11-7-16)32-24(25)26)34(30,31)19-12-8-17(9-13-19)23(28)29/h2-13,24H,14H2,1H3,(H,28,29)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248578
PNG
(US9434711, 491)
Show SMILES Cc1c(sc2ccccc12)N(Cc1cccc(c1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H18F3NO4S2/c1-15-20-7-2-3-8-21(20)33-22(15)28(14-16-5-4-6-18(13-16)24(25,26)27)34(31,32)19-11-9-17(10-12-19)23(29)30/h2-13H,14H2,1H3,(H,29,30)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248361
PNG
(US9434711, 218)
Show SMILES OCc1c(sc2ccccc12)N(Cc1ccc(F)c(c1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H17F4NO5S2/c25-20-10-5-14(11-19(20)24(26,27)28)12-29(22-18(13-30)17-3-1-2-4-21(17)35-22)36(33,34)16-8-6-15(7-9-16)23(31)32/h1-11,30H,12-13H2,(H,31,32)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248458
PNG
(US9434711, 335)
Show SMILES CC(O)c1c(sc2ccccc12)N(Cc1ccc(F)c(c1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1/C25H19F4NO5S2/c1-14(31)22-18-4-2-3-5-21(18)36-23(22)30(13-15-6-11-20(26)19(12-15)25(27,28)29)37(34,35)17-9-7-16(8-10-17)24(32)33/h2-12,14,31H,13H2,1H3,(H,32,33)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335154
PNG
(3-[5-(2-Trifluoromethoxyphenyl)-1H-benzimidazol-2-...)
Show SMILES FC(F)(F)Oc1ccccc1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C22H20F3N3O2/c23-22(24,25)29-19-7-3-2-6-15(19)14-8-9-16-17(12-14)27-20(26-16)18-13-21(30-28-18)10-4-1-5-11-21/h2-3,6-9,12H,1,4-5,10-11,13H2,(H,26,27)
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Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241620
PNG
(US9409915, 59)
Show SMILES Cn1nc(c(Cl)c1-c1nc2cc(nc(N3CCOCC3)c2[nH]1)-c1ccccc1C(F)(F)F)C(C)(C)C
Show InChI InChI=1S/C25H26ClF3N6O/c1-24(2,3)21-18(26)20(34(4)33-21)22-30-17-13-16(14-7-5-6-8-15(14)25(27,28)29)31-23(19(17)32-22)35-9-11-36-12-10-35/h5-8,13H,9-12H2,1-4H3,(H,30,32)
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Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50426573
PNG
(CHEMBL2324349 | US9434711, 306)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(F)c(c1)C(F)(F)F)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C24H17F4NO4S2/c1-14-18-4-2-3-5-21(18)34-22(14)29(13-15-6-11-20(25)19(12-15)24(26,27)28)35(32,33)17-9-7-16(8-10-17)23(30)31/h2-12H,13H2,1H3,(H,30,31)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
For patch clamp experiments, HEK293 cells are stably transfected with canine TRPM8 and cultured in DMEM supplemented with 10% fetal bovine serum, 100...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241689
PNG
(US9409915, 93)
Show SMILES CC(C)Oc1nc(cc2nc([nH]c12)-c1c(Cl)c(nn1C)C(C)(C)C)-c1ccccc1OC(F)(F)F
Show InChI InChI=1S/C24H25ClF3N5O2/c1-12(2)34-22-18-15(11-14(30-22)13-9-7-8-10-16(13)35-24(26,27)28)29-21(31-18)19-17(25)20(23(3,4)5)32-33(19)6/h7-12H,1-6H3,(H,29,31)
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Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241631
PNG
(US9409915, 14)
Show SMILES CC(C)Oc1nc(cc2nc([nH]c12)-c1c(C#N)c(nn1C)C(C)(C)C)-c1ccccc1C(F)(F)F
Show InChI InChI=1S/C25H25F3N6O/c1-13(2)35-23-19-18(11-17(31-23)14-9-7-8-10-16(14)25(26,27)28)30-22(32-19)20-15(12-29)21(24(3,4)5)33-34(20)6/h7-11,13H,1-6H3,(H,30,32)
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US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335163
PNG
(3-[5-(2-Trifluoromethoxyphenyl)-7-trifluoromethyl-...)
Show SMILES FC(F)(F)Oc1ccccc1-c1cc(c2[nH]c(nc2c1)C1=NOC2(C1)CCCCC2)C(F)(F)F
Show InChI InChI=1S/C23H19F6N3O2/c24-22(25,26)15-10-13(14-6-2-3-7-18(14)33-23(27,28)29)11-16-19(15)31-20(30-16)17-12-21(34-32-17)8-4-1-5-9-21/h2-3,6-7,10-11H,1,4-5,8-9,12H2,(H,30,31)
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Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248363
PNG
(US9434711, 220)
Show SMILES CCS(=O)(=O)N(Cc1ccc(F)c(c1)C(F)(F)F)c1sc2ccccc2c1C(C)O
Show InChI InChI=1/C20H19F4NO3S2/c1-3-30(27,28)25(11-13-8-9-16(21)15(10-13)20(22,23)24)19-18(12(2)26)14-6-4-5-7-17(14)29-19/h4-10,12,26H,3,11H2,1-2H3
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UniProtKB/TrEMBL

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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248415
PNG
(US9434711, 279)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(CC1CCCCC1)c1sc2ccccc2c1Br
Show InChI InChI=1S/C22H22BrNO4S2/c23-20-18-8-4-5-9-19(18)29-21(20)24(14-15-6-2-1-3-7-15)30(27,28)17-12-10-16(11-13-17)22(25)26/h4-5,8-13,15H,1-3,6-7,14H2,(H,25,26)
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248808
PNG
(US9434711, 774)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(C(O)=O)c(F)c1
Show InChI InChI=1S/C24H17F4NO5S2/c1-14-18-4-2-3-5-21(18)35-22(14)29(13-15-6-8-16(9-7-15)34-24(26,27)28)36(32,33)17-10-11-19(23(30)31)20(25)12-17/h2-12H,13H2,1H3,(H,30,31)
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UniProtKB/TrEMBL

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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM50335174
PNG
(3-[7-Trifluoromethyl-5-(2-trifluoromethylphenyl)-1...)
Show SMILES FC(F)(F)c1ccccc1-c1cc(c2[nH]c(nc2c1)C1=NOC2(C1)CCOCC2)C(F)(F)F
Show InChI InChI=1S/C22H17F6N3O2/c23-21(24,25)14-4-2-1-3-13(14)12-9-15(22(26,27)28)18-16(10-12)29-19(30-18)17-11-20(33-31-17)5-7-32-8-6-20/h1-4,9-10H,5-8,11H2,(H,29,30)
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Assay Description
Antagonist activity at canine TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241639
PNG
(US9409915, 22)
Show SMILES Cn1nc(c(C#N)c1-c1nc2cc(nc(N3CCCCC3)c2[nH]1)-c1ccccc1C(F)(F)F)C(C)(C)C
Show InChI InChI=1S/C27H28F3N7/c1-26(2,3)23-17(15-31)22(36(4)35-23)24-32-20-14-19(16-10-6-7-11-18(16)27(28,29)30)33-25(21(20)34-24)37-12-8-5-9-13-37/h6-7,10-11,14H,5,8-9,12-13H2,1-4H3,(H,32,34)
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Janssen Pharmaceutica NV

US Patent


Assay Description
HEK293 cells stably expressing canine TRPM8 were routinely grown as monolayers in Dulbecco's minimum essential medium supplemented with 10% FBS, 2 mM...


US Patent US9409915 (2016)

More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM248356
PNG
(US9434711, 213)
Show SMILES OCc1c(sc2ccccc12)N(Cc1ccc(F)c(F)c1)S(=O)(=O)c1ccccc1
Show InChI InChI=1S/C22H17F2NO3S2/c23-19-11-10-15(12-20(19)24)13-25(30(27,28)16-6-2-1-3-7-16)22-18(14-26)17-8-4-5-9-21(17)29-22/h1-12,26H,13-14H2
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Janssen Pharmaceutica, N.V.

US Patent


Assay Description
The functional activity of compounds of the formula (I) was determined by measuring changes in intracellular calcium concentration using a Ca2+-sensi...


US Patent US9434711 (2016)

More data for this
Ligand-Target Pair
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