| Reaction Details |
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 | Report a problem with these data |
| Target | Cholecystokinin receptor type A |
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| Ligand | BDBM21139 |
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| Substrate/Competitor | [125I]CCK-8 |
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| Meas. Tech. | Radioligand Labeled Binding Assay and Phosphatidylinositol Hydrolysis Assay for the CCK Receptor |
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| Ki | 9.6±n/a nM |
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| EC50 | 2500±n/a nM |
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| Citation |  Agnes, RS; Lee, YS; Davis, P; Ma, SW; Badghisi, H; Porreca, F; Lai, J; Hruby, VJ Structure-activity relationships of bifunctional peptides based on overlapping pharmacophores at opioid and cholecystokinin receptors. J Med Chem49:2868-75 (2006) [PubMed] Article |
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| More Info.: | Get all data from this article, Solution Info, Assay Method |
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| Cholecystokinin receptor type A |
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| Name: | Cholecystokinin receptor type A |
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| Synonyms: | CCK-A receptor | CCK-AR | CCK1-R | CCKAR | CCKAR_HUMAN | CCKRA | Cholecystokinin receptor | Cholecystokinin receptor type A | Cholecystokinin-1 Receptor |
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| Type: | G Protein-Coupled Receptor (GPCR) |
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| Mol. Mass.: | 47859.34 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Stable expression of human CCK-1 receptors in HEK 293 cells. |
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| Residue: | 428 |
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| Sequence: | MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNT
LVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYF
MGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYS
NLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGI
KFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNS
SAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSY
TSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSH
MSASVPPQ
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| BDBM21139 |
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| [125I]CCK-8 |
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| Name | BDBM21139 |
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| Synonyms: | (3S)-3-[(2S)-2-[(2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)propanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid | CCK-Opioid Peptide, 9 | Tyr-D-Nle-Gly-Trp-Nle-Asp-Phe-NH2 |
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| Type | Peptide |
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| Emp. Form. | C47H61N9O10 |
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| Mol. Mass. | 912.0415 |
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| SMILES | CCCC[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N[C@@H](Cc1c[nH]c2ccccc12)C(=O)N[C@@H](CCCC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O |
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| Structure | 
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