Target Poor or Non Binder(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T53024 | Target Info | |||
| Target Name | Somatostatin receptor type 2 (SSTR2) | ||||
| Synonyms |
Sst(2); Somatostatin receptor 2; SS2R; SS2-R; SS-2-R; SRIF-1
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| Target Type | Successful Target | ||||
| Gene Name | SSTR2 | ||||
| Biochemical Class | GPCR rhodopsin | ||||
| UniProt ID | |||||
| Poor Binders of This Target (in total, 7 binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
Methyl 3-[3-[3-[3-[3-[acetyl(benzyl)amino]propanoyl-[2-(1H-indol-3-yl)ethyl]amino]propanoyl-(4-aminobutyl)amino]propanoyl-[(2R)-2-hydroxypropyl]amino]propanoyl-benzylamino]propanoate
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3218124
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| Activity |
Ki = 55000 nM
|
[1] | |||
| Compound Name |
3-[2-(2-Pyridinyl)ethyl]-1-[3-[(5-bromo-2-pyridinyl)(3,4-dichlorobenzyl)amino]propyl]thiourea
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL142295; SCHEMBL7425408; BDBM50068057; 1-{3-[(5-Bromo-pyridin-2-yl)-(3,4-dichloro-benzyl)-amino]-propyl}-3-(2-pyridin-2-yl-ethyl)-thiourea
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| Activity |
Ki = 74000 nM
|
[2] | |||
| Compound Name |
(1R,3R)-3-(4-(5-Fluoropyridin-2-yl)-1H-imidazol-2-yl)-1-(1-ethyl-pyrazol-4-yl)-1-(3-methyl-1,3,4-oxadiazol-3H-2-one-5-yl)-2,3,4,9-tetrahydro-1H-ss-carboline
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Investigative | Compound Info | ||
| Synonyms |
CHEMBL3582336; MK-1421; BDBM50091414
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| Activity |
IC50 ~ 100000 nM
|
[3] | |||
| Compound Name |
Methyl 3-[3-[3-[[2-[3-[acetyl(benzyl)amino]propanoyl-[2-(1H-indol-3-yl)ethyl]amino]acetyl]-(4-aminobutyl)amino]propanoyl-[(2R)-2-hydroxypropyl]amino]propanoyl-benzylamino]propanoate
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3217760
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|
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| Activity |
Ki = 110000 nM
|
[1] | |||
| Compound Name |
3-[3-(2-Pyridinylamino)propyl]-1-[3-[(2-pyridinyl)(4-bromobenzyl)amino]propyl]thiourea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL422475; BDBM50068056; 1-{3-[(4-Bromo-benzyl)-pyridin-2-yl-amino]-propyl}-3-[3-(pyridin-2-ylamino)-propyl]-thiourea
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| Activity |
Ki = 114000 nM
|
[2] | |||
| Compound Name |
1-(4-Aminobutyl)-8-benzyl-12-[(2R)-2-hydroxypropyl]-4-[2-(1H-indol-3-yl)ethyl]-1,4,8,12-tetrazacyclopentadecane-2,5,9,13-tetrone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3218120
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|
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| Activity |
Ki = 176000 nM
|
[1] | |||
| Compound Name |
1-(4-Aminobutyl)-9-benzyl-13-[(2R)-2-hydroxypropyl]-5-[2-(1H-indol-3-yl)ethyl]-1,5,9,13-tetrazacyclohexadecane-2,6,10,14-tetrone
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL3218121
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|
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| Activity |
Ki = 198000 nM
|
[1] | |||
| Click to Show/Hide the Information of All Poor Binders | |||||
| Non Binders of This Target (in total, 5 non binders) | Download | Top | |||
|---|---|---|---|---|---|
| Compound Name |
3-(4-Piperidinophenyl)-1-[3-[(5-bromo-2-pyridinyl)(3,4-dichlorobenzyl)amino]propyl]thiourea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL143539; BDBM50068038
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| Activity |
Ki > 300000 nM
|
[2] | |||
| Compound Name |
3-[3-(2-Pyridinylamino)propyl]-1-[3-[(5-bromo-2-pyridinyl)(3,4-dichlorobenzyl)amino]propyl]thiourea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL143245; SCHEMBL7426084; BDBM50068058
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| Activity |
Ki > 300000 nM
|
[2] | |||
| Compound Name |
3-(3-Phenylpropyl)-1-[4-[(2-pyridinyl)(4-bromobenzyl)amino]butyl]thiourea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL142811; BDBM50068048; 1-{4-[(4-Bromo-benzyl)-pyridin-2-yl-amino]-butyl}-3-(3-phenyl-propyl)-thiourea
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| Activity |
Ki > 300000 nM
|
[2] | |||
| Compound Name |
3-(4-Piperidinophenyl)-1-[2-[(5-bromo-2-pyridinyl)(3,4-dichlorobenzyl)amino]ethyl]thiourea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL142293; SCHEMBL8175064; BDBM50068041; L017960
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|
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| Activity |
Ki > 300000 nM
|
[2] | |||
| Compound Name |
3-(1H-Benzimidazole-2-ylmethyl)-1-[2-[(5-bromo-2-pyridinyl)(3,4-dichlorobenzyl)amino]ethyl]thiourea
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|
Investigative | Compound Info | ||
| Synonyms |
CHEMBL342781; BDBM50068051
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| Activity |
Ki > 300000 nM
|
[2] | |||
| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Synthesis and binding affinities for sst receptors of cyclic peptoid SRIF-mimetics. Medchemcomm. 2012;3:1531-5. | ||||
| REF 2 | Nonpeptide somatostatin agonists with sst4 selectivity: synthesis and structure-activity relationships of thioureas. J Med Chem. 1998 Nov 19;41(24):4693-705. | ||||
| REF 3 | Discovery of MK-1421, a Potent, Selective sstr3 Antagonist, as a Development Candidate for Type 2 Diabetes. ACS Med Chem Lett. 2015 Mar 18;6(5):513-7. | ||||
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