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Compile Data Set for Download or QSAR

Found 354 hits Enz. Inhib. hit(s) with Target = 'Transient receptor potential cation channel subfamily M member 8' AND taxid = 10116   
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 cation channel subfamily M member 8


(Rattus norvegicus)
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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n/an/a 4n/an/an/an/an/an/a


TBA

Assay Description
Antagonist activity at rat TRPM8 expressed in HEK293 cells assessed as inhibition of intracellular calcium accumulation at 0.2 uM by FLIPR assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50036517
PNG
(CHEMBL3353597)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc(OC(F)(F)F)cc1)c1ncc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C21H13ClF6N2O5S/c22-17-9-14(20(23,24)25)10-29-18(17)30(11-12-1-5-15(6-2-12)35-21(26,27)28)36(33,34)16-7-3-13(4-8-16)19(31)32/h1-10H,11H2,(H,31,32)
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n/an/a 5.80n/an/an/an/an/an/a



RaQualia Pharma Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 assessed as inhibition of menthol induced Ca2+ influx by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50036554
PNG
(CHEMBL3353609)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc(cc1)C(F)(F)F)c1ncc(Cl)cc1Cl
Show InChI InChI=1S/C20H13Cl2F3N2O4S/c21-15-9-17(22)18(26-10-15)27(11-12-1-5-14(6-2-12)20(23,24)25)32(30,31)16-7-3-13(4-8-16)19(28)29/h1-10H,11H2,(H,28,29)
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n/an/a 9n/an/an/an/an/an/a



RaQualia Pharma Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 assessed as inhibition of menthol induced Ca2+ influx by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50442406
PNG
(CHEMBL2443061)
Show SMILES O[C@@H]1CC2(CCN(CC2)C(=O)Nc2ccc(OC(F)(F)F)cc2)Oc2c(Cl)cccc12
Show InChI InChI=1S/C21H20ClF3N2O4/c22-16-3-1-2-15-17(28)12-20(31-18(15)16)8-10-27(11-9-20)19(29)26-13-4-6-14(7-5-13)30-21(23,24)25/h1-7,17,28H,8-12H2,(H,26,29)/t17-/m1/s1
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n/an/a 17n/an/an/an/an/an/a



Glenmark Pharmaceuticals Ltd.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 by 45Ca2+ uptake assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008716
PNG
(CHEMBL3235983)
Show SMILES C[C@H](NC(=O)N1CCc2ccccc2[C@H]1c1ccc(c(F)c1)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C20H17F7N2O/c1-11(19(22,23)24)28-18(30)29-9-8-12-4-2-3-5-14(12)17(29)13-6-7-15(16(21)10-13)20(25,26)27/h2-7,10-11,17H,8-9H2,1H3,(H,28,30)/t11-,17+/m0/s1
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n/an/a 18n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50365710
PNG
(CHEMBL1955989)
Show SMILES FC(F)(F)c1ccccc1-c1ccc2nc(C=CC3CCCCC3)[nH]c2c1
Show InChI InChI=1S/C22H21F3N2/c23-22(24,25)18-9-5-4-8-17(18)16-11-12-19-20(14-16)27-21(26-19)13-10-15-6-2-1-3-7-15/h4-5,8-15H,1-3,6-7H2,(H,26,27)
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n/an/a 20n/an/an/an/an/an/a



Janssen Research& Development

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 by calcium flux assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50317558
PNG
(CHEMBL1094770 | N-[(1R,2S,5R)-2-Isopropyl-5-methyl...)
Show SMILES CC(C)[C@@H]1CC[C@@H](C)C[C@H]1NC(=O)c1ccc(cc1)-c1ccccc1
Show InChI InChI=1S/C23H29NO/c1-16(2)21-14-9-17(3)15-22(21)24-23(25)20-12-10-19(11-13-20)18-7-5-4-6-8-18/h4-8,10-13,16-17,21-22H,9,14-15H2,1-3H3,(H,24,25)/t17-,21+,22-/m1/s1
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n/an/a 20n/an/an/an/an/an/a



Sapienza Universit£ di Roma

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRMP8 receptor expressed in HEK293 cells assessed as menthol-induced calcium elevation


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008696
PNG
(CHEMBL3235965)
Show SMILES FC(F)(F)c1ccc(cc1)[C@H]1N(CCc2ccccc12)C(=O)Nc1cccnc1
Show InChI InChI=1S/C22H18F3N3O/c23-22(24,25)17-9-7-16(8-10-17)20-19-6-2-1-4-15(19)11-13-28(20)21(29)27-18-5-3-12-26-14-18/h1-10,12,14,20H,11,13H2,(H,27,29)/t20-/m1/s1
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n/an/a 22n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008717
PNG
(CHEMBL3235984)
Show SMILES C[C@H](NC(=O)N1CCc2cccnc2[C@H]1c1ccc(c(F)c1)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C19H16F7N3O/c1-10(18(21,22)23)28-17(30)29-8-6-11-3-2-7-27-15(11)16(29)12-4-5-13(14(20)9-12)19(24,25)26/h2-5,7,9-10,16H,6,8H2,1H3,(H,28,30)/t10-,16+/m0/s1
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n/an/a 23n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008700
PNG
(CHEMBL3235969)
Show SMILES C[C@H](NC(=O)N1CCc2ccccc2[C@H]1c1ccc(cc1)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C20H18F6N2O/c1-12(19(21,22)23)27-18(29)28-11-10-13-4-2-3-5-16(13)17(28)14-6-8-15(9-7-14)20(24,25)26/h2-9,12,17H,10-11H2,1H3,(H,27,29)/t12-,17+/m0/s1
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n/an/a 27n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50036552
PNG
(CHEMBL3353607)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc2ccoc2c1)c1ncc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C22H14ClF3N2O5S/c23-18-10-16(22(24,25)26)11-27-20(18)28(12-13-1-2-14-7-8-33-19(14)9-13)34(31,32)17-5-3-15(4-6-17)21(29)30/h1-11H,12H2,(H,29,30)
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n/an/a 28n/an/an/an/an/an/a



RaQualia Pharma Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 assessed as inhibition of menthol induced Ca2+ influx by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008709
PNG
(CHEMBL3235976)
Show SMILES Fc1ccc(NC(=O)N2CCc3cccnc3[C@H]2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C22H17F4N3O/c23-17-7-9-18(10-8-17)28-21(30)29-13-11-14-2-1-12-27-19(14)20(29)15-3-5-16(6-4-15)22(24,25)26/h1-10,12,20H,11,13H2,(H,28,30)/t20-/m1/s1
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n/an/a 37n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50036540
PNG
(CHEMBL3353598)
Show SMILES OC(=O)c1ccc(cc1)S(=O)(=O)N(Cc1ccc(F)cc1)c1ncc(cc1Cl)C(F)(F)F
Show InChI InChI=1S/C20H13ClF4N2O4S/c21-17-9-14(20(23,24)25)10-26-18(17)27(11-12-1-5-15(22)6-2-12)32(30,31)16-7-3-13(4-8-16)19(28)29/h1-10H,11H2,(H,28,29)
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n/an/a 43n/an/an/an/an/an/a



RaQualia Pharma Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 assessed as inhibition of menthol induced Ca2+ influx by cell-based assay


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008698
PNG
(CHEMBL3235967)
Show SMILES CC(C)(C)NC(=O)N1CCc2ccccc2[C@H]1c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C21H23F3N2O/c1-20(2,3)25-19(27)26-13-12-14-6-4-5-7-17(14)18(26)15-8-10-16(11-9-15)21(22,23)24/h4-11,18H,12-13H2,1-3H3,(H,25,27)/t18-/m1/s1
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n/an/a 45n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008699
PNG
(CHEMBL3235968)
Show SMILES CC(C)NC(=O)N1CCc2ccccc2[C@H]1c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C20H21F3N2O/c1-13(2)24-19(26)25-12-11-14-5-3-4-6-17(14)18(25)15-7-9-16(10-8-15)20(21,22)23/h3-10,13,18H,11-12H2,1-2H3,(H,24,26)/t18-/m1/s1
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n/an/a 47n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008712
PNG
(CHEMBL3235979)
Show SMILES FC(F)(F)c1ccc(cc1)[C@H]1N(CCc2cccnc12)C(=O)Nc1cccnc1
Show InChI InChI=1S/C21H17F3N4O/c22-21(23,24)16-7-5-15(6-8-16)19-18-14(3-1-11-26-18)9-12-28(19)20(29)27-17-4-2-10-25-13-17/h1-8,10-11,13,19H,9,12H2,(H,27,29)/t19-/m1/s1
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n/an/a 48n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50317558
PNG
(CHEMBL1094770 | N-[(1R,2S,5R)-2-Isopropyl-5-methyl...)
Show SMILES CC(C)[C@@H]1CC[C@@H](C)C[C@H]1NC(=O)c1ccc(cc1)-c1ccccc1
Show InChI InChI=1S/C23H29NO/c1-16(2)21-14-9-17(3)15-22(21)24-23(25)20-12-10-19(11-13-20)18-7-5-4-6-8-18/h4-8,10-13,16-17,21-22H,9,14-15H2,1-3H3,(H,24,25)/t17-,21+,22-/m1/s1
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n/an/a 50n/an/an/an/an/an/a



Sapienza Universit£ di Roma

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRMP8 receptor expressed in HEK293 cells assessed as menthol-induced calcium elevation


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50317567
PNG
(Biphenyl-3-yl-(1R,2S,5R)-2-isopropyl-5-methylcyclo...)
Show SMILES CC(C)[C@@H]1CC[C@@H](C)C[C@H]1NC(=O)Oc1cccc(c1)-c1ccccc1
Show InChI InChI=1S/C23H29NO2/c1-16(2)21-13-12-17(3)14-22(21)24-23(25)26-20-11-7-10-19(15-20)18-8-5-4-6-9-18/h4-11,15-17,21-22H,12-14H2,1-3H3,(H,24,25)/t17-,21+,22-/m1/s1
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n/an/a 50n/an/an/an/an/an/a



Sapienza Universit£ di Roma

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRMP8 receptor expressed in HEK293 cells assessed as menthol-induced calcium elevation


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383255
PNG
(CHEMBL2032202)
Show SMILES Fc1ccc(NC(=O)N2CCc3ccccc3C2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C23H18F4N2O/c24-18-9-11-19(12-10-18)28-22(30)29-14-13-15-3-1-2-4-20(15)21(29)16-5-7-17(8-6-16)23(25,26)27/h1-12,21H,13-14H2,(H,28,30)
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n/an/a 53n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383263
PNG
(CHEMBL2032210)
Show SMILES Fc1ccc(NC(=O)N2CCc3ccccc3[C@H]2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C23H18F4N2O/c24-18-9-11-19(12-10-18)28-22(30)29-14-13-15-3-1-2-4-20(15)21(29)16-5-7-17(8-6-16)23(25,26)27/h1-12,21H,13-14H2,(H,28,30)/t21-/m1/s1
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n/an/a 56n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383263
PNG
(CHEMBL2032210)
Show SMILES Fc1ccc(NC(=O)N2CCc3ccccc3[C@H]2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C23H18F4N2O/c24-18-9-11-19(12-10-18)28-22(30)29-14-13-15-3-1-2-4-20(15)21(29)16-5-7-17(8-6-16)23(25,26)27/h1-12,21H,13-14H2,(H,28,30)/t21-/m1/s1
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n/an/a 57n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50241426
PNG
(3-(2-hydroxyphenyl)-6-(3-nitrophenyl)-3,4-dihydrop...)
Show SMILES Oc1ccccc1N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O
Show InChI InChI=1S/C16H13N3O4/c20-15-7-2-1-6-14(15)18-9-8-13(17-16(18)21)11-4-3-5-12(10-11)19(22)23/h1-8,10,20H,9H2,(H,17,21)
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n/an/a 58n/an/an/an/an/an/a



National Research Council

Curated by ChEMBL


Assay Description
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins ...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50083056
PNG
(CHEMBL3422837)
Show SMILES [O-][N+](=O)c1cccc(\C=C\C(=O)Nc2cccc(I)c2)c1
Show InChI InChI=1S/C15H11IN2O3/c16-12-4-2-5-13(10-12)17-15(19)8-7-11-3-1-6-14(9-11)18(20)21/h1-10H,(H,17,19)/b8-7+
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n/an/a 73n/an/an/an/an/an/a



National Research Council

Curated by ChEMBL


Assay Description
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins ...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50317566
PNG
(4-tert-Butylphenyl-(1R,2S,5R)-2-isopropyl-5-methyl...)
Show SMILES CC(C)[C@@H]1CC[C@@H](C)C[C@H]1NC(=O)Oc1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C21H33NO2/c1-14(2)18-12-7-15(3)13-19(18)22-20(23)24-17-10-8-16(9-11-17)21(4,5)6/h8-11,14-15,18-19H,7,12-13H2,1-6H3,(H,22,23)/t15-,18+,19-/m1/s1
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n/an/a 80n/an/an/an/an/an/a



Sapienza Universit£ di Roma

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRMP8 receptor expressed in HEK293 cells assessed as menthol-induced calcium elevation


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008718
PNG
(CHEMBL3235964)
Show SMILES FC(F)(F)c1ccc(cc1)[C@H]1N(CCc2ccccc12)C(=O)Nc1ccccn1
Show InChI InChI=1S/C22H18F3N3O/c23-22(24,25)17-10-8-16(9-11-17)20-18-6-2-1-5-15(18)12-14-28(20)21(29)27-19-7-3-4-13-26-19/h1-11,13,20H,12,14H2,(H,26,27,29)/t20-/m1/s1
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n/an/a 81n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383252
PNG
(CHEMBL2032199)
Show SMILES Fc1ccc(NC(=O)N2CCc3scnc3C2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C20H15F4N3OS/c21-14-5-7-15(8-6-14)26-19(28)27-10-9-16-17(25-11-29-16)18(27)12-1-3-13(4-2-12)20(22,23)24/h1-8,11,18H,9-10H2,(H,26,28)
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n/an/a 93n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383256
PNG
(CHEMBL2032203)
Show SMILES Fc1ccc(NC(=O)N2CCc3c(F)cccc3C2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C23H17F5N2O/c24-16-8-10-17(11-9-16)29-22(31)30-13-12-18-19(2-1-3-20(18)25)21(30)14-4-6-15(7-5-14)23(26,27)28/h1-11,21H,12-13H2,(H,29,31)
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n/an/a 100n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50317566
PNG
(4-tert-Butylphenyl-(1R,2S,5R)-2-isopropyl-5-methyl...)
Show SMILES CC(C)[C@@H]1CC[C@@H](C)C[C@H]1NC(=O)Oc1ccc(cc1)C(C)(C)C
Show InChI InChI=1S/C21H33NO2/c1-14(2)18-12-7-15(3)13-19(18)22-20(23)24-17-10-8-16(9-11-17)21(4,5)6/h8-11,14-15,18-19H,7,12-13H2,1-6H3,(H,22,23)/t15-,18+,19-/m1/s1
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n/an/a 100n/an/an/an/an/an/a



Sapienza Universit£ di Roma

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRMP8 receptor expressed in HEK293 cells assessed as menthol-induced calcium elevation


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008721
PNG
(CHEMBL3235961)
Show SMILES FC(F)(F)c1ccc(cc1)[C@H]1N(CCc2ccccc12)C(=O)Nc1ccccc1C#N
Show InChI InChI=1S/C24H18F3N3O/c25-24(26,27)19-11-9-17(10-12-19)22-20-7-3-1-5-16(20)13-14-30(22)23(31)29-21-8-4-2-6-18(21)15-28/h1-12,22H,13-14H2,(H,29,31)/t22-/m1/s1
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n/an/a 104n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008714
PNG
(CHEMBL3235981)
Show SMILES C[C@H](NC(=O)N1CCc2cccnc2[C@H]1c1ccc(cc1)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C19H17F6N3O/c1-11(18(20,21)22)27-17(29)28-10-8-12-3-2-9-26-15(12)16(28)13-4-6-14(7-5-13)19(23,24)25/h2-7,9,11,16H,8,10H2,1H3,(H,27,29)/t11-,16+/m0/s1
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n/an/a 115n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008713
PNG
(CHEMBL3235980)
Show SMILES FC(F)(F)c1ccc(cc1)[C@H]1N(CCc2cccnc12)C(=O)Nc1ccc(cc1)C#N
Show InChI InChI=1S/C23H17F3N4O/c24-23(25,26)18-7-5-17(6-8-18)21-20-16(2-1-12-28-20)11-13-30(21)22(31)29-19-9-3-15(14-27)4-10-19/h1-10,12,21H,11,13H2,(H,29,31)/t21-/m1/s1
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n/an/a 120n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008715
PNG
(CHEMBL3235982)
Show SMILES C[C@H](NC(=O)N1CCc2ccccc2[C@H]1c1ccc(nc1)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C19H17F6N3O/c1-11(18(20,21)22)27-17(29)28-9-8-12-4-2-3-5-14(12)16(28)13-6-7-15(26-10-13)19(23,24)25/h2-7,10-11,16H,8-9H2,1H3,(H,27,29)/t11-,16+/m0/s1
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n/an/a 127n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50083055
PNG
(CHEMBL3422836)
Show SMILES [O-][N+](=O)c1cccc(\C=C\C(=O)Nc2cccc(Br)c2)c1
Show InChI InChI=1S/C15H11BrN2O3/c16-12-4-2-5-13(10-12)17-15(19)8-7-11-3-1-6-14(9-11)18(20)21/h1-10H,(H,17,19)/b8-7+
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n/an/a 140n/an/an/an/an/an/a



National Research Council

Curated by ChEMBL


Assay Description
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins ...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383227
PNG
(CHEMBL2032173)
Show SMILES Clc1ccccc1C1N(CCc2sccc12)C(=O)Nc1ccccc1
Show InChI InChI=1S/C20H17ClN2OS/c21-17-9-5-4-8-15(17)19-16-11-13-25-18(16)10-12-23(19)20(24)22-14-6-2-1-3-7-14/h1-9,11,13,19H,10,12H2,(H,22,24)
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n/an/a 140n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008701
PNG
(CHEMBL3235970)
Show SMILES C[C@@H](NC(=O)N1CCc2ccccc2[C@H]1c1ccc(cc1)C(F)(F)F)C(F)(F)F
Show InChI InChI=1S/C20H18F6N2O/c1-12(19(21,22)23)27-18(29)28-11-10-13-4-2-3-5-16(13)17(28)14-6-8-15(9-7-14)20(24,25)26/h2-9,12,17H,10-11H2,1H3,(H,27,29)/t12-,17-/m1/s1
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n/an/a 146n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383249
PNG
(CHEMBL2032195)
Show SMILES Fc1ccc(NC(=O)N2CCc3ccsc3C2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C21H16F4N2OS/c22-16-5-7-17(8-6-16)26-20(28)27-11-9-14-10-12-29-19(14)18(27)13-1-3-15(4-2-13)21(23,24)25/h1-8,10,12,18H,9,11H2,(H,26,28)
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n/an/a 150n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008719
PNG
(CHEMBL3235963)
Show SMILES FC(F)(F)c1ccc(cc1)[C@H]1N(CCc2ccccc12)C(=O)Nc1ccc(cc1)C#N
Show InChI InChI=1S/C24H18F3N3O/c25-24(26,27)19-9-7-18(8-10-19)22-21-4-2-1-3-17(21)13-14-30(22)23(31)29-20-11-5-16(15-28)6-12-20/h1-12,22H,13-14H2,(H,29,31)/t22-/m1/s1
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n/an/a 154n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50318487
PNG
(CHEMBL497318 | Cannabigerol)
Show SMILES CCCCCc1cc(O)c(C\C=C(/C)CCC=C(C)C)c(O)c1
Show InChI InChI=1S/C21H32O2/c1-5-6-7-11-18-14-20(22)19(21(23)15-18)13-12-17(4)10-8-9-16(2)3/h9,12,14-15,22-23H,5-8,10-11,13H2,1-4H3/b17-12+
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n/an/a 160n/an/an/an/an/an/a



Universita` del Piemonte Orientale

Curated by ChEMBL


Assay Description
Antagonist activity at rat recombinant TRPM8 receptor expressed in HEK293 cells assessed as inhibition of 0.25 uM icilin-induced stimulation of intra...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008702
PNG
(CHEMBL3235971)
Show SMILES FC(F)(F)C(NC(=O)N1CCc2ccccc2[C@H]1c1ccc(cc1)C(F)(F)F)c1ccccc1
Show InChI InChI=1S/C25H20F6N2O/c26-24(27,28)19-12-10-17(11-13-19)21-20-9-5-4-6-16(20)14-15-33(21)23(34)32-22(25(29,30)31)18-7-2-1-3-8-18/h1-13,21-22H,14-15H2,(H,32,34)/t21-,22?/m1/s1
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n/an/a 168n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50083054
PNG
(CHEMBL3422835)
Show SMILES [O-][N+](=O)c1cccc(\C=C\C(=O)Nc2cccc(Cl)c2)c1
Show InChI InChI=1S/C15H11ClN2O3/c16-12-4-2-5-13(10-12)17-15(19)8-7-11-3-1-6-14(9-11)18(20)21/h1-10H,(H,17,19)/b8-7+
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n/an/a 170n/an/an/an/an/an/a



National Research Council

Curated by ChEMBL


Assay Description
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins ...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50083062
PNG
(CHEMBL3422842)
Show SMILES CC(C)c1cccc(NC(=O)\C=C\c2cccc(c2)[N+]([O-])=O)c1
Show InChI InChI=1S/C18H18N2O3/c1-13(2)15-6-4-7-16(12-15)19-18(21)10-9-14-5-3-8-17(11-14)20(22)23/h3-13H,1-2H3,(H,19,21)/b10-9+
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n/an/a 170n/an/an/an/an/an/a



National Research Council

Curated by ChEMBL


Assay Description
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins ...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383251
PNG
(CHEMBL2032198)
Show SMILES Fc1ccc(NC(=O)N2CCn3cccc3C2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C21H17F4N3O/c22-16-7-9-17(10-8-16)26-20(29)28-13-12-27-11-1-2-18(27)19(28)14-3-5-15(6-4-14)21(23,24)25/h1-11,19H,12-13H2,(H,26,29)
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Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383258
PNG
(CHEMBL2032205)
Show SMILES Fc1ccc(NC(=O)N2CCc3ccc(F)cc3C2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C23H17F5N2O/c24-17-7-9-19(10-8-17)29-22(31)30-12-11-14-3-6-18(25)13-20(14)21(30)15-1-4-16(5-2-15)23(26,27)28/h1-10,13,21H,11-12H2,(H,29,31)
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n/an/a 190n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008720
PNG
(CHEMBL3235962)
Show SMILES FC(F)(F)c1ccc(cc1)[C@H]1N(CCc2ccccc12)C(=O)Nc1cccc(c1)C#N
Show InChI InChI=1S/C24H18F3N3O/c25-24(26,27)19-10-8-18(9-11-19)22-21-7-2-1-5-17(21)12-13-30(22)23(31)29-20-6-3-4-16(14-20)15-28/h1-11,14,22H,12-13H2,(H,29,31)/t22-/m1/s1
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n/an/a 190n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50008723
PNG
(CHEMBL3235959)
Show SMILES Fc1ccccc1NC(=O)N1CCc2ccccc2[C@H]1c1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C23H18F4N2O/c24-19-7-3-4-8-20(19)28-22(30)29-14-13-15-5-1-2-6-18(15)21(29)16-9-11-17(12-10-16)23(25,26)27/h1-12,21H,13-14H2,(H,28,30)/t21-/m1/s1
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n/an/a 197n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior to icilin chall...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50317564
PNG
(4-(Trifluoromethyl)phenyl(1R,2S,5R)-2-isopropyl-5-...)
Show SMILES CC(C)[C@@H]1CC[C@@H](C)C[C@H]1NC(=O)Oc1ccc(cc1)C(F)(F)F
Show InChI InChI=1S/C18H24F3NO2/c1-11(2)15-9-4-12(3)10-16(15)22-17(23)24-14-7-5-13(6-8-14)18(19,20)21/h5-8,11-12,15-16H,4,9-10H2,1-3H3,(H,22,23)/t12-,15+,16-/m1/s1
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n/an/a 200n/an/an/an/an/an/a



Sapienza Universit£ di Roma

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRMP8 receptor expressed in HEK293 cells assessed as menthol-induced calcium elevation


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383217
PNG
(CHEMBL2032197)
Show SMILES Fc1ccc(NC(=O)N2CCc3ccoc3C2c2ccc(cc2)C(F)(F)F)cc1
Show InChI InChI=1S/C21H16F4N2O2/c22-16-5-7-17(8-6-16)26-20(28)27-11-9-14-10-12-29-19(14)18(27)13-1-3-15(4-2-13)21(23,24)25/h1-8,10,12,18H,9,11H2,(H,26,28)
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n/an/a 230n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50082781
PNG
(CHEMBL3422796)
Show SMILES COc1cccc(c1)N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O
Show InChI InChI=1S/C17H15N3O4/c1-24-15-7-3-5-13(11-15)19-9-8-16(18-17(19)21)12-4-2-6-14(10-12)20(22)23/h2-8,10-11H,9H2,1H3,(H,18,21)
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n/an/a 240n/an/an/an/an/an/a



National Research Council

Curated by ChEMBL


Assay Description
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins ...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50383224
PNG
(CHEMBL2032170)
Show SMILES FC(F)(F)c1ccccc1C1N(CCc2sccc12)C(=O)Nc1ccccc1
Show InChI InChI=1S/C21H17F3N2OS/c22-21(23,24)17-9-5-4-8-15(17)19-16-11-13-28-18(16)10-12-26(19)20(27)25-14-6-2-1-3-7-14/h1-9,11,13,19H,10,12H2,(H,25,27)
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n/an/a 240n/an/an/an/an/an/a



Amgen Inc.

Curated by ChEMBL


Assay Description
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin inductio...


Citation and Details
More data for this
Ligand-Target Pair
Transient receptor potential cation channel subfamily M member 8


(Rattus norvegicus)
BDBM50083005
PNG
(CHEMBL3422799)
Show SMILES Cc1ccc(O)c(c1)N1CC=C(NC1=O)c1cccc(c1)[N+]([O-])=O
Show InChI InChI=1S/C17H15N3O4/c1-11-5-6-16(21)15(9-11)19-8-7-14(18-17(19)22)12-3-2-4-13(10-12)20(23)24/h2-7,9-10,21H,8H2,1H3,(H,18,22)
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n/an/a 260n/an/an/an/an/an/a



National Research Council

Curated by ChEMBL


Assay Description
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins ...


Citation and Details
More data for this
Ligand-Target Pair
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