Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T41955 | Target Info | |||
| Target Name | Long transient receptor potential channel 8 (TRPM8) | ||||
| Synonyms |
Trp-p8; Transient receptor potential-p8; Transient receptor potential cation channel subfamily M member 8; TRPP8; TRPM8; LTrpC6
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| Target Type | Successful Target | ||||
| Gene Name | TRPM8 | ||||
| Biochemical Class | Transient receptor potential catioin channel | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 8 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(3S)-N-Ethyl-3-hydroxy-3-phenyl-N-(thiophen-2-ylmethyl)propanamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4071883; BDBM50268718
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| Activity |
EC50 = 52023 nM
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[1] | |||
| Compound Name |
N-[(1S)-2-Amino-2-oxo-1-phenylethyl]-N-[(3-methoxyphenyl)methyl]thiophene-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3908930; SCHEMBL16924240; BDBM50207650
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| Activity |
IC50 = 54000 nM
|
[2] | |||
| Compound Name |
2-[Benzoyl-[(3-methoxyphenyl)methyl]amino]-2-phenylacetic acid
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3910516; BDBM50207652
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| Activity |
IC50 = 59000 nM
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[2] | |||
| Compound Name |
2-(4-Methylphenoxy)-N-(1-methylpyrazol-4-yl)-N-(thiophen-2-ylmethyl)acetamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL4074235; BDBM50268771
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| Activity |
EC50 = 63000 nM
|
[1] | |||
| Compound Name |
N-[(1R)-2-(Dimethylamino)-2-oxo-1-phenylethyl]-N-[(3-methoxyphenyl)methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3901461; BDBM50207653
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| Activity |
IC50 = 86000 nM
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[2] | |||
| Compound Name |
Menthol
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Investigative | Compound Info | ||
| Synonyms |
dl-Menthol; 2-Isopropyl-5-methylcyclohexanol; p-Menthan-3-ol; Cyclohexanol, 5-methyl-2-(1-methylethyl)-; Menthyl alcohol; Racementhol; (+/-)-Menthol; Hexahydrothymol; 5-methyl-2-propan-2-ylcyclohexan-1-ol; Menthol [USP]; Neomenthol; Menthol natural; rac-Menthol; 5-Methyl-2-(1-methylethyl)cyclohexanol; 5-methyl-2-(propan-2-yl)cyclohexan-1-ol; (1R,2S,5R)-Menthol; Menthol, dl-; Menthol (USP); (1S, 2S, 5R)-(+)-Neomenthol; 5-methyl-2-(propan-2-yl)cyclohexanol; DSSTox_CID_805; DSSTox_RID_78794; DSSTox_GSID_29650; Racemic menthol; FEMA No. 2665; Caswell No. 540; 3-p-Menthanol; Mentholum; Mineral ice; MFCD00001484; Therapeutic mineral ice; 3-p-Menthol; (+)-Neo-menthol; CCRIS 9231; 3-Hydroxy-p-menthane; Fisherman's friend lozenges; Robitussin Cough Drops; EINECS 216-074-4; EPA Pesticide Chemical Code 051601; (+/-)-p-Menthan-3-ol; Menthol, cis-1,3,trans-1,4-; (1S,2R,5R)-(+)-Isomenthol; 5-Methyl-2-(1-methylethyl)-cyclohexanol; AI3-08161; HSDB 593; (-)menthol; NCGC00159382-02; (-) menthol; 2-Isopropyl-5-methylcyclohexan-1-ol; 4-Isopropyl-1-methylcyclohexan-3-ol; Menthol, 99%; p-menthan-3-ol group; dl-Menthol (JP17); 1-methyl-4-isopropyl-3-hydroxycyclohexane; ACMC-1BQW4; EC 216-074-4; SCHEMBL4612; Menthol, (.+/-.)-; Menthol, puriss., 99.0%; CHEMBL256087; DL-Menthol, analytical standard; DTXSID8029650; Fisherman's friend lozenges (TN); BDBM248162; HMS3744K19; 2-Isopropyl-5-methylcyclohexanol #; BCP27552; BCP31841; CS-M3737; HY-N1369; menthol crystals; 15356-70-4; Tox21_200010; Tox21_303464; ANW-21459; BBL009325; DL-Menthol, >=95%, FCC, FG; STK802468; AKOS000119740; AKOS016843634; AM81446; MCULE-3070949324; 5-methyl-2-propan-2-yl-1-cyclohexanol; Menthol 1000 microg/mL in Acetonitrile; Menthol, SAJ special grade, >=98.0%; NCGC00159382-03; NCGC00159382-04; NCGC00159382-05; NCGC00159382-06; NCGC00257403-01; NCGC00257564-01; 5-methyl-2-propan-2-yl-cyclohexan-1-ol; AK110724; AK158890; HY-75161; SC-01321; SC-54016; SC-84251; SY004225; SY010603; VS-02042; DB-063989; Levomenthol; D-(-)-Menthol; (-)-Menthol; CS-0016777; FT-0600039; FT-0604399; FT-0604426; FT-0604430; FT-0620596; FT-0625488; FT-0695077; FT-0695078; FT-0695079; H2461; M0321; (+/-)-Menthol, racemic, >=98.0% (GC); 2-Isopropy-5-methylcyclohexanol-1,2,6,6-d4; D04849; D04918; (1S,2R,5R)-2-isopropyl-5-methyl-cyclohexanol; A808833; J-500418; Q27109870; Z1258992394
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| Activity |
IC50 = 92000 nM
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[3] | |||
| Compound Name |
N-[(1R)-2-Amino-2-oxo-1-phenylethyl]-N-[[4-[(4-fluorophenyl)methoxy]-3-methoxyphenyl]methyl]thiophene-2-carboxamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3936873; BDBM50207567
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Compound Name |
N-[(2R)-1-Amino-1-oxopropan-2-yl]-N-[(3-methoxyphenyl)methyl]benzamide
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3952818; BDBM50207648
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| Activity |
IC50 ~ 100000 nM
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[2] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Discovery and development of a novel class of phenoxyacetyl amides as highly potent TRPM8 agonists for use as cooling agents. Bioorg Med Chem Lett. 2017 Aug 15;27(16):3931-3938. | ||||
| REF 2 | Synthesis and optimization of novel alpha-phenylglycinamides as selective TRPM8 antagonists. Bioorg Med Chem. 2017 Jan 15;25(2):727-742. | ||||
| REF 3 | TRPM8 voltage sensor mutants reveal a mechanism for integrating thermal and chemical stimuli. Nat Chem Biol. 2007 Mar;3(3):174-82. | ||||
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