Reaction Details |
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Target | Somatostatin receptor type 1/2/3/4/5 |
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Ligand | BDBM50020211 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_200345 (CHEMBL807247) |
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IC50 | 1801±n/a nM |
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Citation | Kazmierski, W; Wire, WS; Lui, GK; Knapp, RJ; Shook, JE; Burks, TF; Yamamura, HI; Hruby, VJ Design and synthesis of somatostatin analogues with topographical properties that lead to highly potent and specific mu opioid receptor antagonists with greatly reduced binding at somatostatin receptors. J Med Chem31:2170-7 (1988) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Somatostatin receptor type 1/2/3/4/5 |
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Name: | Somatostatin receptor type 1/2/3/4/5 |
Synonyms: | Somatostatin receptor |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of ChEMBL is 200351 |
Components: | This complex has 5 components. |
Component 1 |
Name: | Somatostatin receptor type 1 |
Synonyms: | SOMATOSTATIN SST1 | SRIF-2 | SS1R | SSR1_RAT | Somatostatin receptor | Somatostatin receptor type 1 | Sstr1 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 42752.93 |
Organism: | RAT |
Description: | SOMATOSTATIN SST1 SSTR1 RAT::P28646 |
Residue: | 391 |
Sequence: | MFPNGTAPSPTSSPSSSPGGCGEGVCSRGPGSGAADGMEEPGRNSSQNGTLSEGQGSAIL
ISFIYSVVCLVGLCGNSMVIYVILRYAKMKTATNIYILNLAIADELLMLSVPFLVTSTLL
RHWPFGALLCRLVLSVDAVNMFTSIYCLTVLSVDRYVAVVHPIKAARYRRPTVAKVVNLG
VWVLSLLVILPIVVFSRTAANSDGTVACNMLMPEPAQRWLVGFVLYTFLMGFLLPVGAIC
LCYVLIIAKMRMVALKAGWQQRKRSERKITLMVMMVVMVFVICWMPFYVVQLVNVFAEQD
DATVSQLSVILGYANSCANPILYGFLSDNFKRSFQRILCLSWMDNAAEEPVDYYATALKS
RAYSVEDFQPENLESGGVFRNGTCASRISTL
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Component 2 |
Name: | Somatostatin receptor type 3 |
Synonyms: | SOMATOSTATIN SST3 | SSR3_RAT | Somatostatin receptor | Somatostatin receptor 3 | Somatostatin receptor type 3 | Sstr3 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 47161.54 |
Organism: | RAT |
Description: | SOMATOSTATIN SST3 SSTR3 RAT::P30936 |
Residue: | 428 |
Sequence: | MAAVTYPSSVPTTLDPGNASSAWPLDTSLGNASAGTSLAGLAVSGILISLVYLVVCVVGL
LGNSLVIYVVLRHTSSPSVTSVYILNLALADELFMLGLPFLAAQNALSYWPFGSLMCRLV
MAVDGINQFTSIFCLTVMSVDRYLAVVHPTRSARWRTAPVARMVSAAVWVASAVVVLPVV
VFSGVPRGMSTCHMQWPEPAAAWRTAFIIYTAALGFFGPLLVICLCYLLIVVKVRSTTRR
VRAPSCQWVQAPACQRRRRSERRVTRMVVAVVALFVLCWMPFYLLNIVNVVCPLPEEPAF
FGLYFLVVALPYANSCANPILYGFLSYRFKQGFRRILLRPSRRVRSQEPGSGPPEKTEEE
EDEEEEERREEEERRMQRGQEMNGRLSQIAQPGPSGQQQRPCTGTAKEQQLLPQEATAGD
KASTLSHL
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Component 3 |
Name: | Somatostatin receptor type 4 |
Synonyms: | SOMATOSTATIN SST4 | SSR4_RAT | Somatostatin receptor | Somatostatin receptor type 4 | Sstr4 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 42096.84 |
Organism: | RAT |
Description: | SOMATOSTATIN SST4 SSTR4 RAT::P30937 |
Residue: | 384 |
Sequence: | MNTPATLPLGGEDTTWTPGINASWAPDEEEDAVRSDGTGTAGMVTIQCIYALVCLVGLVG
NALVIFVILRYAKMKTATNIYLLNLAVADELFMLSVPFVASAAALRHWPFGAVLCRAVLS
VDGLNMFTSVFCLTVLSVDRYVAVVHPLRAATYRRPSVAKLINLGVWLASLLVTLPIAVF
ADTRPARGGEAVACNLHWPHPAWSAVFVIYTFLLGFLLPVLAIGLCYLLIVGKMRAVALR
AGWQQRRRSEKKITRLVLMVVTVFVLCWMPFYVVQLLNLFVTSLDATVNHVSLILSYANS
CANPILYGFLSDNFRRSFQRVLCLRCCLLETTGGAEEEPLDYYATALKSRGGPGCICPPL
PCQQEPMQAEPACKRVPFTKTTTF
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Component 4 |
Name: | Somatostatin receptor type 2 |
Synonyms: | SOMATOSTATIN SST2 | SRIF-1 | SS2R | SSR2_RAT | Somatostatin receptor | Somatostatin receptor 2 | Somatostatin receptor type 2 | Sstr2 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 41212.21 |
Organism: | RAT |
Description: | SOMATOSTATIN SST2 SSTR2 RAT::P30680 |
Residue: | 369 |
Sequence: | MELTSEQFNGSQVWIPSPFDLNGSLGPSNGSNQTEPYYDMTSNAVLTFIYFVVCVVGLCG
NTLVIYVILRYAKMKTITNIYILNLAIADELFMLGLPFLAMQVALVHWPFGKAICRVVMT
VDGINQFTSIFCLTVMSIDRYLAVVHPIKSAKWRRPRTAKMINVAVWGVSLLVILPIMIY
AGLRSNQWGRSSCTINWPGESGAWYTGFIIYAFILGFLVPLTIICLCYLFIIIKVKSSGI
RVGSSKRKKSEKKVTRMVSIVVAVFIFCWLPFYIFNVSSVSVAISPTPALKGMFDFVVIL
TYANSCANPILYAFLSDNFKKSFQNVLCLVKVSGAEDGERSDSKQDKSRLNETTETQRTL
LNGDLQTSI
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Component 5 |
Name: | Somatostatin receptor type 5 |
Synonyms: | SOMATOSTATIN SST5 | SSR5_RAT | Somatostatin receptor | Somatostatin receptor type 5 | Sstr5 |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 39986.50 |
Organism: | RAT |
Description: | SOMATOSTATIN SST5 SSTR5 RAT::P30938 |
Residue: | 363 |
Sequence: | MEPLSLASTPSWNASAASSGNHNWSLVGSASPMGARAVLVPVLYLLVCTVGLSGNTLVIY
VVLRHAKMKTVTNVYILNLAVADVLFMLGLPFLATQNAVVSYWPFGSFLCRLVMTLDGIN
QFTSIFCLMVMSVDRYLAVVHPLRSARWRRPRVAKMASAAVWVFSLLMSLPLLVFADVQE
GWGTCNLSWPEPVGLWGAAFITYTSVLGFFGPLLVICLCYLLIVVKVKAAGMRVGSSRRR
RSEPKVTRMVVVVVLVFVGCWLPFFIVNIVNLAFTLPEEPTSAGLYFFVVVLSYANSCAN
PLLYGFLSDNFRQSFRKVLCLRRGYGMEDADAIEPRPDKSGRPQATLPTRSCEANGLMQT
SRI
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BDBM50020211 |
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n/a |
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Name | BDBM50020211 |
Synonyms: | CHEMBL216353 | D-Phec(-Cys-Tyr-D-Trp-Lys-Thr-Pen-)Asn-NH2 |
Type | Small organic molecule |
Emp. Form. | C51H68N12O11S2 |
Mol. Mass. | 1089.289 |
SMILES | C[C@@H](O)[C@@H]1NC(=O)[C@H](CCCCN)NC(=O)[C@H](Cc2c[nH]c3ccccc23)NC(=O)[C@H](Cc2ccc(O)cc2)NC(=O)[C@H](CSSC(C)(C)[C@H](NC1=O)C(=O)N[C@@H](CC(N)=O)C(N)=O)NC(=O)[C@H](N)Cc1ccccc1 |
Structure |
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