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Compile Data Set for Download or QSAR

Found 2023 hits of ic50 data for polymerid = 10879,6944,7406   
Target/Host
(Institution)
LigandTarget/Host
Links
Ligand
Links
Trg + Lig
Links
Ki
nM
ΔG°
kcal/mole
IC50
nM
Kd
nM
EC50/IC50
nM
koff
s-1
kon
M-1s-1
pHTemp
°C
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

GoogleScholar
PC cid
PC sid
UniChem
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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
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

GoogleScholar
CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/a 0.200n/an/an/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


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


J Med Chem 54: 233-47 (2011)


Article DOI: 10.1021/jm101075v
BindingDB Entry DOI: 10.7270/Q20C4WRJ
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256277
PNG
(US9487488, 1)
Show SMILES FC(F)(F)Oc1ccc(CN(c2ncc3ccccc3c2C2CC2)S(=O)(=O)c2ccc(cc2)-c2nnn[nH]2)cc1
Show InChI InChI=1S/C27H21F3N6O3S/c28-27(29,30)39-21-11-5-17(6-12-21)16-36(26-24(18-7-8-18)23-4-2-1-3-20(23)15-31-26)40(37,38)22-13-9-19(10-14-22)25-32-34-35-33-25/h1-6,9-15,18H,7-8,16H2,(H,32,33,34,35)
KEGG

UniProtKB/SwissProt

DrugBank
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.300n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256293
PNG
(US9487488, 17)
Show SMILES Cc1cc(ccc1-c1nnn[nH]1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1ncc2ccccc2c1C1CC1
Show InChI InChI=1S/C28H23F3N6O3S/c1-17-14-22(12-13-23(17)26-33-35-36-34-26)41(38,39)37(16-18-6-10-21(11-7-18)40-28(29,30)31)27-25(19-8-9-19)24-5-3-2-4-20(24)15-32-27/h2-7,10-15,19H,8-9,16H2,1H3,(H,33,34,35,36)
KEGG

UniProtKB/SwissProt

DrugBank
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.300n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
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

GoogleScholar
PC cid
PC sid
UniChem

Similars

US Patent
n/an/a 0.400n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
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

UniProtKB/SwissProt

DrugBank
GoogleScholar
Purchase

CHEMBL
PC cid
PC sid
UniChem

Similars

Article
PubMed
n/an/a 0.413n/an/an/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


Assay Description
Inhibition of human TRPM8 expressed in HEK293 cells assessed as inhibition of cold-induced channel current by whole cell electrophysiology


J Med Chem 54: 233-47 (2011)


Article DOI: 10.1021/jm101075v
BindingDB Entry DOI: 10.7270/Q20C4WRJ
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256310
PNG
(US9487488, 34)
Show SMILES Cc1cc(ccc1-c1noc(=O)[nH]1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1ncc2ccccc2c1C1CC1
Show InChI InChI=1S/C29H23F3N4O5S/c1-17-14-22(12-13-23(17)26-34-28(37)41-35-26)42(38,39)36(16-18-6-10-21(11-7-18)40-29(30,31)32)27-25(19-8-9-19)24-5-3-2-4-20(24)15-33-27/h2-7,10-15,19H,8-9,16H2,1H3,(H,34,35,37)
KEGG

UniProtKB/SwissProt

DrugBank
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.5n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256299
PNG
(US9487488, 23)
Show SMILES Cc1cc(ccc1-c1ncn[nH]1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1ncc2ccccc2c1C1CC1
Show InChI InChI=1S/C29H24F3N5O3S/c1-18-14-23(12-13-24(18)27-34-17-35-36-27)41(38,39)37(16-19-6-10-22(11-7-19)40-29(30,31)32)28-26(20-8-9-20)25-5-3-2-4-21(25)15-33-28/h2-7,10-15,17,20H,8-9,16H2,1H3,(H,34,35,36)
KEGG

UniProtKB/SwissProt

DrugBank
GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.5n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241685
PNG
(US9409915, 89 | US9718820, Compound 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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.530n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q23J3BVJ
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241685
PNG
(US9409915, 89 | US9718820, Compound 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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.530n/an/an/an/an/a25



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, ...


US Patent US9718820 (2017)

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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241633
PNG
(US9409915, 16 | US9718820, Compound 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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.590n/an/an/an/an/a25



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, ...


US Patent US9718820 (2017)

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


(Canis lupus familiaris (Dog))
BDBM241633
PNG
(US9409915, 16 | US9718820, Compound 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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.590n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q23J3BVJ
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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.600n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256298
PNG
(US9487488, 22)
Show SMILES Cc1n[nH]c(n1)-c1ccc(cc1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1ncc2ccccc2c1C1CC1
Show InChI InChI=1S/C29H24F3N5O3S/c1-18-34-27(36-35-18)21-10-14-24(15-11-21)41(38,39)37(17-19-6-12-23(13-7-19)40-29(30,31)32)28-26(20-8-9-20)25-5-3-2-4-22(25)16-33-28/h2-7,10-16,20H,8-9,17H2,1H3,(H,34,35,36)
KEGG

UniProtKB/SwissProt

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PC cid
PC sid
UniChem
US Patent
n/an/a 0.600n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM151765
PNG
(US8987445, 201)
Show SMILES Cc1c(ncc2ccccc12)N(Cc1ccc(c(Cl)c1)C(F)(F)C1CC1)S(=O)(=O)c1ccc(cc1)C(O)=O
Show InChI InChI=1S/C28H23ClF2N2O4S/c1-17-23-5-3-2-4-20(23)15-32-26(17)33(38(36,37)22-11-7-19(8-12-22)27(34)35)16-18-6-13-24(25(29)14-18)28(30,31)21-9-10-21/h2-8,11-15,21H,9-10,16H2,1H3,(H,34,35)
KEGG

UniProtKB/SwissProt

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UniChem

Similars

US Patent
n/an/a 0.600n/an/an/an/an/a37



Mitsubishi Tanabe Pharma Corporation

US Patent


Assay Description
The functional activity of compounds was determined by measuring changes in intracellular calcium concentration using a Ca2+ sensitive fluorescent dy...


US Patent US8987445 (2015)


BindingDB Entry DOI: 10.7270/Q2BZ64R5
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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UniChem

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Article
PubMed
n/an/a 0.600n/an/an/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


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


J Med Chem 54: 233-47 (2011)


Article DOI: 10.1021/jm101075v
BindingDB Entry DOI: 10.7270/Q20C4WRJ
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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.600n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241638
PNG
(US9409915, 21 | US9718820, Compound 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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.690n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q23J3BVJ
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241638
PNG
(US9409915, 21 | US9718820, Compound 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

GoogleScholar
PC cid
PC sid
UniChem
US Patent
n/an/a 0.690n/an/an/an/an/a25



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, ...


US Patent US9718820 (2017)

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



Janssen Research and Development

Curated by ChEMBL


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


J Med Chem 54: 233-47 (2011)


Article DOI: 10.1021/jm101075v
BindingDB Entry DOI: 10.7270/Q20C4WRJ
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256290
PNG
(US9487488, 14)
Show SMILES Cc1c(nc(C2CC2)c2ccccc12)N(Cc1ccc(OC(F)(F)F)cc1)S(=O)(=O)c1ccc(cc1)-c1nnn[nH]1
Show InChI InChI=1S/C28H23F3N6O3S/c1-17-23-4-2-3-5-24(23)25(19-8-9-19)32-27(17)37(16-18-6-12-21(13-7-18)40-28(29,30)31)41(38,39)22-14-10-20(11-15-22)26-33-35-36-34-26/h2-7,10-15,19H,8-9,16H2,1H3,(H,33,34,35,36)
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n/an/a 0.700n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
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)
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n/an/a 0.700n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256314
PNG
(US9487488, 38)
Show SMILES Cc1cc(ccc1S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1ncc2ccccc2c1C1CC1)C(O)=O
Show InChI InChI=1S/C28H23F3N2O5S/c1-17-14-20(27(34)35)10-13-24(17)39(36,37)33(16-18-6-11-22(12-7-18)38-28(29,30)31)26-25(19-8-9-19)23-5-3-2-4-21(23)15-32-26/h2-7,10-15,19H,8-9,16H2,1H3,(H,34,35)
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n/an/a 0.700n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
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)
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n/an/a 0.700n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256301
PNG
(US9487488, 25)
Show SMILES Cc1n[nH]c(n1)-c1ccc(cc1)S(=O)(=O)N(Cc1ccc(cn1)C(F)(F)F)c1ncc2ccccc2c1C1CC1
Show InChI InChI=1S/C28H23F3N6O2S/c1-17-34-26(36-35-17)19-8-12-23(13-9-19)40(38,39)37(16-22-11-10-21(15-32-22)28(29,30)31)27-25(18-6-7-18)24-5-3-2-4-20(24)14-33-27/h2-5,8-15,18H,6-7,16H2,1H3,(H,34,35,36)
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n/an/a 0.700n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256278
PNG
(US9487488, 2)
Show SMILES FC(F)(F)Oc1ccc(CN(c2ncc3ccccc3c2C2CC2)S(=O)(=O)c2ccc(nc2)-c2nnn[nH]2)cc1
Show InChI InChI=1S/C26H20F3N7O3S/c27-26(28,29)39-19-9-5-16(6-10-19)15-36(25-23(17-7-8-17)21-4-2-1-3-18(21)13-31-25)40(37,38)20-11-12-22(30-14-20)24-32-34-35-33-24/h1-6,9-14,17H,7-8,15H2,(H,32,33,34,35)
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MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241686
PNG
(US9409915, 90 | US9718820, Compound 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)
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n/an/a 0.730n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q23J3BVJ
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241686
PNG
(US9409915, 90 | US9718820, Compound 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)
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n/an/a 0.730n/an/an/an/an/a25



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, ...


US Patent US9718820 (2017)

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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Janssen Research and Development

Curated by ChEMBL


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


J Med Chem 54: 233-47 (2011)


Article DOI: 10.1021/jm101075v
BindingDB Entry DOI: 10.7270/Q20C4WRJ
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256303
PNG
(US9487488, 27)
Show SMILES Cc1n[nH]c(n1)-c1ccc(cc1C)S(=O)(=O)N(Cc1ccc(cn1)C(F)(F)F)c1ncc2ccccc2c1C1CC1
Show InChI InChI=1S/C29H25F3N6O2S/c1-17-13-23(11-12-24(17)27-35-18(2)36-37-27)41(39,40)38(16-22-10-9-21(15-33-22)29(30,31)32)28-26(19-7-8-19)25-6-4-3-5-20(25)14-34-28/h3-6,9-15,19H,7-8,16H2,1-2H3,(H,35,36,37)
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MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
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)
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n/an/a 0.800n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
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
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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
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)
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n/an/a 0.800n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
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)
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n/an/a 0.800n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM151774
PNG
(US8987445, 210)
Show SMILES Fc1cc(CN(c2ncc3ccccc3c2C2CC2)S(=O)(=O)c2ccc(cc2)C(=O)O[Na])ccc1C(F)(F)C1CC1
Show InChI InChI=1S/C30H25F3N2O4S.Na/c31-26-15-18(5-14-25(26)30(32,33)22-10-11-22)17-35(40(38,39)23-12-8-20(9-13-23)29(36)37)28-27(19-6-7-19)24-4-2-1-3-21(24)16-34-28;/h1-5,8-9,12-16,19,22H,6-7,10-11,17H2,(H,36,37);/q;+1/p-1
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Mitsubishi Tanabe Pharma Corporation

US Patent


Assay Description
The functional activity of compounds was determined by measuring changes in intracellular calcium concentration using a Ca2+ sensitive fluorescent dy...


US Patent US8987445 (2015)


BindingDB Entry DOI: 10.7270/Q2BZ64R5
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)
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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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
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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Janssen Research and Development

Curated by ChEMBL


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


J Med Chem 54: 233-47 (2011)


Article DOI: 10.1021/jm101075v
BindingDB Entry DOI: 10.7270/Q20C4WRJ
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241636
PNG
(US9409915, 19 | US9718820, Compound 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, ...


US Patent US9718820 (2017)

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


(Canis lupus familiaris (Dog))
BDBM241636
PNG
(US9409915, 19 | US9718820, Compound 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)


BindingDB Entry DOI: 10.7270/Q23J3BVJ
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM151797
PNG
(US8987445, 233)
Show SMILES FC(F)(F)c1c(ncc2ccccc12)N(Cc1ccc(c(Cl)c1)C(F)(F)C1CC1)S(=O)(=O)c1ccc(cc1)C(=O)O[Na]
Show InChI InChI=1S/C28H20ClF5N2O4S.Na/c29-23-13-16(5-12-22(23)27(30,31)19-8-9-19)15-36(41(39,40)20-10-6-17(7-11-20)26(37)38)25-24(28(32,33)34)21-4-2-1-3-18(21)14-35-25;/h1-7,10-14,19H,8-9,15H2,(H,37,38);/q;+1/p-1
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n/an/a 0.900n/an/an/an/an/a37



Mitsubishi Tanabe Pharma Corporation

US Patent


Assay Description
The functional activity of compounds was determined by measuring changes in intracellular calcium concentration using a Ca2+ sensitive fluorescent dy...


US Patent US8987445 (2015)


BindingDB Entry DOI: 10.7270/Q2BZ64R5
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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n/an/a 0.900n/an/an/an/an/an/a



Janssen Research and Development

Curated by ChEMBL


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


J Med Chem 54: 233-47 (2011)


Article DOI: 10.1021/jm101075v
BindingDB Entry DOI: 10.7270/Q20C4WRJ
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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n/an/a 0.900n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
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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n/an/a 0.900n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM256294
PNG
(US9487488, 18)
Show SMILES FC(F)(F)c1ccc(CN(c2ncc3ccccc3c2C2CC2)S(=O)(=O)c2ccc(cc2)-c2nnn[nH]2)nc1
Show InChI InChI=1S/C26H20F3N7O2S/c27-26(28,29)19-9-10-20(30-14-19)15-36(25-23(16-5-6-16)22-4-2-1-3-18(22)13-31-25)39(37,38)21-11-7-17(8-12-21)24-32-34-35-33-24/h1-4,7-14,16H,5-6,15H2,(H,32,33,34,35)
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n/an/a 0.900n/an/an/an/an/a37



MITSUBISHI TANABE PHARMA CORPORATION

US Patent


Assay Description
The functional activity of a test compound was determined by measuring change in intracellular calcium concentration using a calcium sensitive fluore...


US Patent US9487488 (2016)


BindingDB Entry DOI: 10.7270/Q2MG7NGT
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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n/an/a 0.900n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q2H41QB6
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM151677
PNG
(US8987445, 104)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1ncc2ccccc2c1C1CC1
Show InChI InChI=1S/C27H21F3N2O5S/c28-27(29,30)37-21-11-5-17(6-12-21)16-32(38(35,36)22-13-9-19(10-14-22)26(33)34)25-24(18-7-8-18)23-4-2-1-3-20(23)15-31-25/h1-6,9-15,18H,7-8,16H2,(H,33,34)
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n/an/a 0.900n/an/an/an/an/a37



Mitsubishi Tanabe Pharma Corporation

US Patent


Assay Description
The functional activity of compounds was determined by measuring changes in intracellular calcium concentration using a Ca2+ sensitive fluorescent dy...


US Patent US8987445 (2015)


BindingDB Entry DOI: 10.7270/Q2BZ64R5
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241637
PNG
(US9409915, 20 | US9718820, Compound 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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n/an/a 0.950n/an/an/an/an/a37



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)


BindingDB Entry DOI: 10.7270/Q23J3BVJ
More data for this
Ligand-Target Pair
Transient receptor potential M8 protein (TRPM8)


(Canis lupus familiaris (Dog))
BDBM241637
PNG
(US9409915, 20 | US9718820, Compound 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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n/an/a 0.950n/an/an/an/an/a25



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, ...


US Patent US9718820 (2017)

More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8 (TRPM8)


(Homo sapiens (Human))
BDBM50036542
PNG
(CHEMBL3353600)
Show SMILES CC(C)(C)c1ccc(CN(c2ncc(cc2Cl)C(F)(F)F)S(=O)(=O)c2ccc(cc2)C(O)=O)cc1
Show InChI InChI=1S/C24H22ClF3N2O4S/c1-23(2,3)17-8-4-15(5-9-17)14-30(21-20(25)12-18(13-29-21)24(26,27)28)35(33,34)19-10-6-16(7-11-19)22(31)32/h4-13H,14H2,1-3H3,(H,31,32)
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n/an/a 0.960n/an/an/an/an/an/a



RaQualia Pharma Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at human TRPM8 expressed in HEK293 cells assessed as inhibition of menthol induced Ca2+ influx


Bioorg Med Chem Lett 24: 5364-8 (2014)


Article DOI: 10.1016/j.bmcl.2014.10.074
BindingDB Entry DOI: 10.7270/Q2TB18HX
More data for this
Ligand-Target Pair
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