Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T35842 | Target Info | |||
| Target Name | Melanocortin receptor 1 (MC1R) | ||||
| Synonyms |
Melanotropin receptor; Melanocyte-stimulating hormone receptor; Melanocortin-1 receptor; MSHR; MSH-R; MC1-R
Click to Show/Hide
|
||||
| Target Type | Successful Target | ||||
| Gene Name | MC1R | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 5 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
(2R)-2-Amino-N-[(2S)-5-(diaminomethylideneamino)-1-piperidin-1-ylpentan-2-yl]-3-(4-fluorophenyl)propanamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL429742; BDBM50372556
Click to Show/Hide
|
||||
| Activity |
EC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
(2R)-2-Amino-N-[(2S)-5-(diaminomethylideneamino)-1-oxo-1-piperidin-1-ylpentan-2-yl]-3-(4-fluorophenyl)propanamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL256630; BDBM50372553
Click to Show/Hide
|
||||
| Activity |
EC50 ~ 50000 nM
|
[1] | |||
| Compound Name |
(R)-2-[(1H-Indol-3-ylmethyl)-amino]-3-naphthalen-2-yl-propionamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL9219; MK-15; BDBM50111188; Nalpha-(1H-Indole-3-ylmethyl)-3-(2-naphthyl)-D-alaninamide
Click to Show/Hide
|
||||
| Activity |
Ki = 74000 nM
|
[2] | |||
| Compound Name |
N-[(2R)-3-(4-Chlorophenyl)-1-(4-cyclohexyl-4-oxidopiperazin-4-ium-1-yl)-1-oxopropan-2-yl]-1,2,3,4-tetrahydroisoquinoline-3-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL363757; BDBM50151508
Click to Show/Hide
|
||||
| Activity |
Ki = 152000 nM
|
[3] | |||
| Compound Name |
(1R,4S,6R)-N-[(2R)-1-[4-(Tert-butylcarbamoyl)-4-cyclohexylpiperidin-1-yl]-3-(4-fluorophenyl)-1-oxopropan-2-yl]-7-methyl-7-azabicyclo[2.2.2]octane-6-carboxamide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
RY764; RY-764; CHEMBL364346; GTPL1337; SCHEMBL14040521; BDBM50169442; RY 764; Q27088656
Click to Show/Hide
|
||||
| Activity |
EC50 = 160000 nM
|
[4] | |||
| Non Binders of This Target (in total, 9 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
4-(2-Naphthylmethyl)-1-piperazinecarboxamidine
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL8561; BDBM50111168; 4-Naphthalen-2-ylmethyl-piperazine-1-carboxamidine
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[5] | |||
| Compound Name |
3-(Piperazin-1-ylmethyl)-1H-indole
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
3-Piperazin-1-ylmethyl-1H-indole; CHEMBL276397; 1H-Indole,3-(1-piperazinylmethyl)-; ACMC-1C6NR; SCHEMBL948663; CTK4A8882; ALBB-009662; 1-(1H-Indole-3-ylmethyl)piperazine; BDBM50111159; STK505991; ZINC22924625; AKOS005172105; QC-9778; AC-26732; AB0097921; FT-0723189; 746P666; 1H-indole, 3-(1-piperazinylmethyl)-, hydrochloride
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[5] | |||
| Compound Name |
(S)-5-Guanidino-2-[(1,2,3,4-tetrahydro-naphthalen-2-ylmethyl)-amino]-pentanoic acid amide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL8676; MK-28; BDBM50111185
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[2] | |||
| Compound Name |
4-(1H-Indole-3-ylmethyl)-1-piperazinecarboxamidine
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL8598; BDBM50111171; 4-(1H-Indol-3-ylmethyl)-piperazine-1-carboxamidine
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[5] | |||
| Compound Name |
(R)-5-Guanidino-2-[(naphthalen-2-ylmethyl)-amino]-pentanoic acid amide
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL266055; MK-20; BDBM50111196; Nalpha-(2-Naphthylmethyl)-D-argininamide
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[2] | |||
| Compound Name |
N-(1-Naphthylmethyl)-N-(2-naphthylmethyl)amine
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL8129; Oprea1_758708; MLS000859006; HMS2798P17; ZINC4343360; BDBM50111163; MCULE-1376042569; SMR000459185; N-(2-Naphthylmethyl)-1-naphthalenemethanamine; Naphthalen-2-ylmethyl-naphthalen-1-ylmethyl-amine
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[5] | |||
| Compound Name |
Nalpha-(1H-Indole-3-ylmethyl)-L-Arg-L-Trp-NH2
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL267007; MK-29B; BDBM50111190
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[2] | |||
| Compound Name |
N-(3-Aminopropyl)-2-naphthalenemethanamine
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL8201; BDBM50111154; N*1*-Naphthalen-2-ylmethyl-propane-1,3-diamine
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[5] | |||
| Compound Name |
1-(Naphthalen-2-ylmethyl)piperazine
Click to Show/Hide
|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL8756; 1-Naphthalen-2-ylmethyl-piperazine; Oprea1_775617; SCHEMBL593143; 1-(2-naphthylmethyl)-piperazine; 1-(beta-napthylmethyl)piperazine; CTK2E5435; DTXSID20358696; BDBM50111166; STL321465; ZINC20790799; AKOS009158679; 1-(2-NAPHTHYLMETHYL)PIPERAZINE; 1-[(naphthalen-2-yl)methyl]piperazine; MCULE-4088318939; NE51610; Piperazine, 1-(2-naphthalenylmethyl)-; DB-110844; BB 0249443; EN300-81737; Z1250089962
Click to Show/Hide
|
||||
| Activity |
Ki > 1000000 nM
|
[5] | |||
| Click to Show/Hide the Information of All Non Binders | |||||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and biological activity of novel peptide mimetics as melanocortin receptor agonists. Bioorg Med Chem Lett. 2008 Feb 1;18(3):1223-8. | ||||
| REF 2 | N-alkylaminoacids and their derivatives interact with melanocortin receptors. Bioorg Med Chem Lett. 2002 Apr 8;12(7):1039-42. | ||||
| REF 3 | New substituted piperazines as ligands for melanocortin receptors. Correlation to the X-ray structure of "THIQ". J Med Chem. 2004 Aug 26;47(18):4613-26. | ||||
| REF 4 | Discovery and activity of (1R,4S,6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1,1-dimethylethyl)amino]carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl)methyl]-2-oxo... Bioorg Med Chem Lett. 2005 Aug 1;15(15):3501-5. | ||||
| REF 5 | Reductive amination products containing naphthalene and indole moieties bind to melanocortin receptors. Bioorg Med Chem Lett. 2002 Apr 8;12(7):1035-8. | ||||
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.