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Found 237 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))
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)
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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))
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)
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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))
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)
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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))
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)
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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))
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)
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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))
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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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))
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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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))
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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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))
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))
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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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))
BDBM50335162
PNG
(3-[5-(2-Fluorophenyl)-7-trifluoromethyl-1H-benzimi...)
Show SMILES Fc1ccccc1-c1cc(c2[nH]c(nc2c1)C1=NOC2(C1)CCCCC2)C(F)(F)F
Show InChI InChI=1S/C22H19F4N3O/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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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))
BDBM165941
PNG
(US9067935, 3)
Show SMILES FC(F)(F)Oc1ccc(CN(c2nc3ccccn3c2Cl)S(=O)(=O)c2ccccc2)cc1
Show InChI InChI=1S/C21H15ClF3N3O3S/c22-19-20(26-18-8-4-5-13-27(18)19)28(32(29,30)17-6-2-1-3-7-17)14-15-9-11-16(12-10-15)31-21(23,24)25/h1-13H,14H2
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Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM165992
PNG
(US9067935, 75)
Show SMILES Fc1cc(CN(c2nc3ccccn3c2Br)S(=O)(=O)c2ccc(cc2)-n2cccn2)ccc1C(F)(F)F
Show InChI InChI=1S/C24H16BrF4N5O2S/c25-22-23(31-21-4-1-2-12-32(21)22)34(15-16-5-10-19(20(26)14-16)24(27,28)29)37(35,36)18-8-6-17(7-9-18)33-13-3-11-30-33/h1-14H,15H2
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Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM50335158
PNG
(3-[7-Fluoro-5-(2-trifluoromethylphenyl)-1H-benzimi...)
Show SMILES Fc1cc(cc2[nH]c(nc12)C1=NOC2(C1)CCCCC2)-c1ccccc1C(F)(F)F
Show InChI InChI=1S/C22H19F4N3O/c23-16-10-13(14-6-2-3-7-15(14)22(24,25)26)11-17-19(16)28-20(27-17)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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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))
BDBM166039
PNG
(US9067935, 6)
Show SMILES FC(F)(F)Oc1ccc(CN(c2nc3ccccn3c2Cl)S(=O)(=O)c2ccc(cc2)C(=O)O[Na])cc1
Show InChI InChI=1S/C22H15ClF3N3O5S.Na/c23-19-20(27-18-3-1-2-12-28(18)19)29(13-14-4-8-16(9-5-14)34-22(24,25)26)35(32,33)17-10-6-15(7-11-17)21(30)31;/h1-12H,13H2,(H,30,31);/q;+1/p-1
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Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM165994
PNG
(US9067935, 77)
Show SMILES FC(F)(F)Oc1ccc(CN(c2nc3ccccn3c2Br)S(=O)(=O)c2ccc(cc2)-n2cccn2)cc1
Show InChI InChI=1S/C24H17BrF3N5O3S/c25-22-23(30-21-4-1-2-14-31(21)22)33(16-17-5-9-19(10-6-17)36-24(26,27)28)37(34,35)20-11-7-18(8-12-20)32-15-3-13-29-32/h1-15H,16H2
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Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM50335169
PNG
(3-[5-(2,6-Difluorophenyl)-1H-benzimidazol-2-yl]-1-...)
Show SMILES Fc1cccc(F)c1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C21H19F2N3O/c22-14-5-4-6-15(23)19(14)13-7-8-16-17(11-13)25-20(24-16)18-12-21(27-26-18)9-2-1-3-10-21/h4-8,11H,1-3,9-10,12H2,(H,24,25)
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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))
BDBM60436
PNG
(US9067935, 109)
Show SMILES CC(C)c1c(nc2ccccn12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)C([O-])=O
Show InChI InChI=1S/C25H22F3N3O5S/c1-16(2)22-23(29-21-5-3-4-14-30(21)22)31(15-17-6-10-19(11-7-17)36-25(26,27)28)37(34,35)20-12-8-18(9-13-20)24(32)33/h3-14,16H,15H2,1-2H3,(H,32,33)/p-1
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Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM50335151
PNG
(3-[5-(2-Chlorophenyl)-1H-benzimidazol-2-yl]-1-oxa-...)
Show SMILES Clc1ccccc1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C21H20ClN3O/c22-16-7-3-2-6-15(16)14-8-9-17-18(12-14)24-20(23-17)19-13-21(26-25-19)10-4-1-5-11-21/h2-3,6-9,12H,1,4-5,10-11,13H2,(H,23,24)
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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))
BDBM50335153
PNG
(3-[5-(2-Difluoromethoxyphenyl)-1H-benzimidazol-2-y...)
Show SMILES FC(F)Oc1ccccc1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C22H21F2N3O2/c23-21(24)28-19-7-3-2-6-15(19)14-8-9-16-17(12-14)26-20(25-16)18-13-22(29-27-18)10-4-1-5-11-22/h2-3,6-9,12,21H,1,4-5,10-11,13H2,(H,25,26)
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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))
BDBM50335161
PNG
(3-[7-Bromo-5-(2-trifluoromethylphenyl)-1H-benzimid...)
Show SMILES FC(F)(F)c1ccccc1-c1cc(Br)c2[nH]c(nc2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C22H19BrF3N3O/c23-16-10-13(14-6-2-3-7-15(14)22(24,25)26)11-17-19(16)28-20(27-17)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))
BDBM50335155
PNG
(3-[5-(2-Fluorophenyl)-1H-benzimidazol-2-yl]-1-oxa-...)
Show SMILES Fc1ccccc1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C21H20FN3O/c22-16-7-3-2-6-15(16)14-8-9-17-18(12-14)24-20(23-17)19-13-21(26-25-19)10-4-1-5-11-21/h2-3,6-9,12H,1,4-5,10-11,13H2,(H,23,24)
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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))
BDBM50431484
PNG
(CHEMBL2348660)
Show SMILES Fc1ccccc1NC(C(=O)N1CCC[C@H]1c1ccccc1F)c1cc2ccccc2s1
Show InChI InChI=1S/C26H22F2N2OS/c27-19-10-3-2-9-18(19)22-13-7-15-30(22)26(31)25(29-21-12-5-4-11-20(21)28)24-16-17-8-1-6-14-23(17)32-24/h1-6,8-12,14,16,22,25,29H,7,13,15H2/t22-,25?/m0/s1
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n/an/a 3n/an/an/an/an/an/a



Janssen Research& Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at dog TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced calcium influx incubated for 5 mins prior to icil...


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


(Canis lupus familiaris (Dog))
BDBM50335156
PNG
(3-[5-(2-Trifluoromethyl-phenyl)-1H-benzimidazol-2-...)
Show SMILES FC(F)(F)c1ccccc1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C22H20F3N3O/c23-22(24,25)16-7-3-2-6-15(16)14-8-9-17-18(12-14)27-20(26-17)19-13-21(29-28-19)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))
BDBM165996
PNG
(US9067935, 79)
Show SMILES Fc1ccc(CN(c2nc3ccccn3c2Br)S(=O)(=O)c2ccc(cc2)-n2cccn2)cc1C(F)(F)F
Show InChI InChI=1S/C24H16BrF4N5O2S/c25-22-23(31-21-4-1-2-12-32(21)22)34(15-16-5-10-20(26)19(14-16)24(27,28)29)37(35,36)18-8-6-17(7-9-18)33-13-3-11-30-33/h1-14H,15H2
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n/an/a 3.17n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM166005
PNG
(US9067935, 53)
Show SMILES CC(C)c1c(nc2ccccn12)N(Cc1ccc(cc1)C(F)(F)F)S(=O)(=O)c1ccccc1
Show InChI InChI=1S/C24H22F3N3O2S/c1-17(2)22-23(28-21-10-6-7-15-29(21)22)30(33(31,32)20-8-4-3-5-9-20)16-18-11-13-19(14-12-18)24(25,26)27/h3-15,17H,16H2,1-2H3
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n/an/a 3.19n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM165939
PNG
(US9067935, 1)
Show SMILES Fc1ccc(CN(c2nc3ccccn3c2Cl)S(=O)(=O)c2ccccc2)cc1C(F)(F)F
Show InChI InChI=1S/C21H14ClF4N3O2S/c22-19-20(27-18-8-4-5-11-28(18)19)29(32(30,31)15-6-2-1-3-7-15)13-14-9-10-17(23)16(12-14)21(24,25)26/h1-12H,13H2
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n/an/a 3.25n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM50335159
PNG
(3-[7-Chloro-5-(2-trifluoromethylphenyl)-1H-benzimi...)
Show SMILES FC(F)(F)c1ccccc1-c1cc(Cl)c2[nH]c(nc2c1)C1=NOC2(C1)CCCCC2
Show InChI InChI=1S/C22H19ClF3N3O/c23-16-10-13(14-6-2-3-7-15(14)22(24,25)26)11-17-19(16)28-20(27-17)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))
BDBM165962
PNG
(US9067935, 25)
Show SMILES Fc1cc(CN(c2nc3ccccn3c2Br)S(=O)(=O)c2ccccc2)ccc1C(F)(F)F
Show InChI InChI=1S/C21H14BrF4N3O2S/c22-19-20(27-18-8-4-5-11-28(18)19)29(32(30,31)15-6-2-1-3-7-15)13-14-9-10-16(17(23)12-14)21(24,25)26/h1-12H,13H2
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n/an/a 3.49n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM209011
PNG
(Piperidine-1-sulfonic acid (3-methyl-benzo[b]thiop...)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(COC(F)(F)F)cc1)S(=O)(=O)N1CCCCC1
Show InChI InChI=1S/C23H25F3N2O3S2/c1-17-20-7-3-4-8-21(20)32-22(17)28(33(29,30)27-13-5-2-6-14-27)15-18-9-11-19(12-10-18)16-31-23(24,25)26/h3-4,7-12H,2,5-6,13-16H2,1H3
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n/an/a 3.60n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9233947 (2016)

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


(Canis lupus familiaris (Dog))
BDBM50335175
PNG
(3-[7-Chloro-5-(2-trifluoromethyl-phenyl)-1H-benzim...)
Show SMILES FC(F)(F)c1ccccc1-c1cc(Cl)c2[nH]c(nc2c1)C1=NOC2(C1)CCOCC2
Show InChI InChI=1S/C21H17ClF3N3O2/c22-15-9-12(13-3-1-2-4-14(13)21(23,24)25)10-16-18(15)27-19(26-16)17-11-20(30-28-17)5-7-29-8-6-20/h1-4,9-10H,5-8,11H2,(H,26,27)
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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))
BDBM60437
PNG
(US9067935, 122)
Show SMILES Cc1c(nc2c(F)cccn12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)C([O-])=O
Show InChI InChI=1S/C23H17F4N3O5S/c1-14-20(28-21-19(24)3-2-12-29(14)21)30(13-15-4-8-17(9-5-15)35-23(25,26)27)36(33,34)18-10-6-16(7-11-18)22(31)32/h2-12H,13H2,1H3,(H,31,32)/p-1
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n/an/a 4.03n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM166022
PNG
(US9067935, 98)
Show SMILES FC(F)(F)c1ccc(CN(c2nc3ccccn3c2Cl)S(=O)(=O)c2ccc(cc2)-n2cccn2)cc1
Show InChI InChI=1S/C24H17ClF3N5O2S/c25-22-23(30-21-4-1-2-14-31(21)22)33(16-17-5-7-18(8-6-17)24(26,27)28)36(34,35)20-11-9-19(10-12-20)32-15-3-13-29-32/h1-15H,16H2
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n/an/a 4.04n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM209017
PNG
(1-[(3-Methyl-benzo[b]thiophen-2-yl)-(4-trifluorome...)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)N1CCC(CC1)C(O)=O
Show InChI InChI=1S/C23H23F3N2O5S2/c1-15-19-4-2-3-5-20(19)34-21(15)28(14-16-6-8-18(9-7-16)33-23(24,25)26)35(31,32)27-12-10-17(11-13-27)22(29)30/h2-9,17H,10-14H2,1H3,(H,29,30)
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n/an/a 4.60n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9233947 (2016)

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


(Canis lupus familiaris (Dog))
BDBM50431488
PNG
(CHEMBL2348665)
Show SMILES Fc1ccccc1NC(C(=O)N1CCC[C@@H]1c1ccccc1)c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C25H22F4N2O/c26-20-9-4-5-10-21(20)30-23(18-12-14-19(15-13-18)25(27,28)29)24(32)31-16-6-11-22(31)17-7-2-1-3-8-17/h1-5,7-10,12-15,22-23,30H,6,11,16H2/t22-,23?/m1/s1
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n/an/a 5n/an/an/an/an/an/a



Janssen Research& Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at dog TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced calcium influx incubated for 5 mins prior to icil...


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


(Canis lupus familiaris (Dog))
BDBM50431489
PNG
(CHEMBL2348666)
Show SMILES Fc1ccccc1NC(C(=O)N1CCC[C@H]1c1ccccc1)c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C25H22F4N2O/c26-20-9-4-5-10-21(20)30-23(18-12-14-19(15-13-18)25(27,28)29)24(32)31-16-6-11-22(31)17-7-2-1-3-8-17/h1-5,7-10,12-15,22-23,30H,6,11,16H2/t22-,23?/m0/s1
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n/an/a 5n/an/an/an/an/an/a



Janssen Research& Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at dog TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced calcium influx incubated for 5 mins prior to icil...


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


(Canis lupus familiaris (Dog))
BDBM166044
PNG
(US9067935, 116)
Show SMILES COC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1nc2ccccn2c1Cl
Show InChI InChI=1S/C23H17ClF3N3O5S/c1-34-22(31)16-7-11-18(12-8-16)36(32,33)30(21-20(24)29-13-3-2-4-19(29)28-21)14-15-5-9-17(10-6-15)35-23(25,26)27/h2-13H,14H2,1H3
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n/an/a 5.29n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM165943
PNG
(US9067935, 5)
Show SMILES FC(F)(F)Oc1ccc(CN(c2nc3ccccn3c2Br)S(=O)(=O)c2ccccc2)cc1
Show InChI InChI=1S/C21H15BrF3N3O3S/c22-19-20(26-18-8-4-5-13-27(18)19)28(32(29,30)17-6-2-1-3-7-17)14-15-9-11-16(12-10-15)31-21(23,24)25/h1-13H,14H2
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n/an/a 5.30n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM166020
PNG
(US9067935, 96)
Show SMILES Fc1cc(CN(c2nc3ccccn3c2Cl)S(=O)(=O)c2ccc(cc2)-n2cccn2)ccc1C(F)(F)F
Show InChI InChI=1S/C24H16ClF4N5O2S/c25-22-23(31-21-4-1-2-12-32(21)22)34(15-16-5-10-19(20(26)14-16)24(27,28)29)37(35,36)18-8-6-17(7-9-18)33-13-3-11-30-33/h1-14H,15H2
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n/an/a 5.5n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM60434
PNG
(US9067935, 107)
Show SMILES Cc1c(nc2ccccn12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)C([O-])=O
Show InChI InChI=1S/C23H18F3N3O5S/c1-15-21(27-20-4-2-3-13-28(15)20)29(14-16-5-9-18(10-6-16)34-23(24,25)26)35(32,33)19-11-7-17(8-12-19)22(30)31/h2-13H,14H2,1H3,(H,30,31)/p-1
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n/an/a 5.68n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM165948
PNG
(US9067935, 11)
Show SMILES Cc1c(nc2ccccn12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccccc1
Show InChI InChI=1S/C22H18F3N3O3S/c1-16-21(26-20-9-5-6-14-27(16)20)28(32(29,30)19-7-3-2-4-8-19)15-17-10-12-18(13-11-17)31-22(23,24)25/h2-14H,15H2,1H3
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n/an/a 5.68n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM209012
PNG
(Morpholine-1-sulfonic acid (3-methyl-benzo[b]thiop...)
Show SMILES Cc1c(sc2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)N1CCOCC1
Show InChI InChI=1S/C21H21F3N2O4S2/c1-15-18-4-2-3-5-19(18)31-20(15)26(32(27,28)25-10-12-29-13-11-25)14-16-6-8-17(9-7-16)30-21(22,23)24/h2-9H,10-14H2,1H3
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n/an/a 5.70n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9233947 (2016)

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


(Canis lupus familiaris (Dog))
BDBM50431473
PNG
(CHEMBL2348325)
Show SMILES Fc1ccccc1N[C@H](C(=O)N1CCC[C@H]1c1ccccc1F)c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C25H21F5N2O/c26-19-7-2-1-6-18(19)22-10-5-15-32(22)24(33)23(31-21-9-4-3-8-20(21)27)16-11-13-17(14-12-16)25(28,29)30/h1-4,6-9,11-14,22-23,31H,5,10,15H2/t22-,23-/m0/s1
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n/an/a 6n/an/an/an/an/an/a



Janssen Research& Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at dog TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced calcium influx incubated for 5 mins prior to icil...


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


(Canis lupus familiaris (Dog))
BDBM50335166
PNG
(2-(5-(2-(Trifluoromethyl)phenyl)-1H-benzo[d]imidaz...)
Show SMILES FC(F)(F)c1ccccc1-c1ccc2nc([nH]c2c1)C1=NC2(CO1)CCCCC2
Show InChI InChI=1S/C22H20F3N3O/c23-22(24,25)16-7-3-2-6-15(16)14-8-9-17-18(12-14)27-19(26-17)20-28-21(13-29-20)10-4-1-5-11-21/h2-3,6-9,12H,1,4-5,10-11,13H2,(H,26,27)
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n/an/a 6n/an/an/an/an/an/a


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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))
BDBM165964
PNG
(US9067935, 27)
Show SMILES Cc1c(nc2cc(C)ccn12)N(Cc1ccc(c(F)c1)C(F)(F)F)S(=O)(=O)c1ccccc1
Show InChI InChI=1S/C23H19F4N3O2S/c1-15-10-11-29-16(2)22(28-21(29)12-15)30(33(31,32)18-6-4-3-5-7-18)14-17-8-9-19(20(24)13-17)23(25,26)27/h3-13H,14H2,1-2H3
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n/an/a 6.11n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM166003
PNG
(US9067935, 51)
Show SMILES CC(C)c1c(nc2ccccn12)N(Cc1ccc(c(F)c1)C(F)(F)F)S(=O)(=O)c1ccccc1
Show InChI InChI=1S/C24H21F4N3O2S/c1-16(2)22-23(29-21-10-6-7-13-30(21)22)31(34(32,33)18-8-4-3-5-9-18)15-17-11-12-19(20(25)14-17)24(26,27)28/h3-14,16H,15H2,1-2H3
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n/an/a 6.56n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM50335172
PNG
(3-[5-(2-Trifluoromethylphenyl)-1H-benzimidazol-2-y...)
Show SMILES FC(F)(F)c1ccccc1-c1ccc2nc([nH]c2c1)C1=NOC2(C1)CCOCC2
Show InChI InChI=1S/C21H18F3N3O2/c22-21(23,24)15-4-2-1-3-14(15)13-5-6-16-17(11-13)26-19(25-16)18-12-20(29-27-18)7-9-28-10-8-20/h1-6,11H,7-10,12H2,(H,25,26)
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n/an/a 6.70n/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))
BDBM166019
PNG
(US9067935, 95)
Show SMILES Fc1ccc(CN(c2nc3ccccn3c2Cl)S(=O)(=O)c2ccc(cc2)-n2cccn2)cc1C(F)(F)F
Show InChI InChI=1S/C24H16ClF4N5O2S/c25-22-23(31-21-4-1-2-12-32(21)22)34(15-16-5-10-20(26)19(14-16)24(27,28)29)37(35,36)18-8-6-17(7-9-18)33-13-3-11-30-33/h1-14H,15H2
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n/an/a 7n/an/an/an/an/an/a



Janssen Pharmaceutica, NV

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 US9067935 (2015)

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


(Canis lupus familiaris (Dog))
BDBM50431477
PNG
(CHEMBL2348329)
Show SMILES Fc1ccccc1NC(C(=O)N1CCC[C@H]1c1ccccc1F)c1ccc(cc1)-c1cccnc1
Show InChI InChI=1S/C29H25F2N3O/c30-24-9-2-1-8-23(24)27-12-6-18-34(27)29(35)28(33-26-11-4-3-10-25(26)31)21-15-13-20(14-16-21)22-7-5-17-32-19-22/h1-5,7-11,13-17,19,27-28,33H,6,12,18H2/t27-,28?/m0/s1
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n/an/a 7n/an/an/an/an/an/a



Janssen Research& Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at dog TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced calcium influx incubated for 5 mins prior to icil...


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


(Canis lupus familiaris (Dog))
BDBM50431472
PNG
(CHEMBL2348324)
Show SMILES Fc1ccccc1N[C@@H](C(=O)N1CCC[C@H]1c1ccccc1F)c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C25H21F5N2O/c26-19-7-2-1-6-18(19)22-10-5-15-32(22)24(33)23(31-21-9-4-3-8-20(21)27)16-11-13-17(14-12-16)25(28,29)30/h1-4,6-9,11-14,22-23,31H,5,10,15H2/t22-,23+/m0/s1
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n/an/a 7n/an/an/an/an/an/a



Janssen Research& Development, L.L.C.

Curated by ChEMBL


Assay Description
Antagonist activity at dog TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced calcium influx incubated for 5 mins prior to icil...


Citation and Details
More data for this
Ligand-Target Pair
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