Reaction Details |
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Target | Cholecystokinin receptor type A |
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Ligand | BDBM21142 |
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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 | 910±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 |
Synonyms: | CCK-A receptor | CCK-AR | CCK1-R | CCKAR | CCKAR_HUMAN | CCKRA | Cholecystokinin receptor | Cholecystokinin receptor type A | Cholecystokinin-1 Receptor |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 47859.34 |
Organism: | Homo sapiens (Human) |
Description: | Stable expression of human CCK-1 receptors in HEK 293 cells. |
Residue: | 428 |
Sequence: | MDVVDSLLVNGSNITPPCELGLENETLFCLDQPRPSKEWQPAVQILLYSLIFLLSVLGNT
LVITVLIRNKRMRTVTNIFLLSLAVSDLMLCLFCMPFNLIPNLLKDFIFGSAVCKTTTYF
MGTSVSVSTFNLVAISLERYGAICKPLQSRVWQTKSHALKVIAATWCLSFTIMTPYPIYS
NLVPFTKNNNQTANMCRFLLPNDVMQQSWHTFLLLILFLIPGIVMMVAYGLISLELYQGI
KFEASQKKSAKERKPSTTSSGKYEDSDGCYLQKTRPPRKLELRQLSTGSSSRANRIRSNS
SAANLMAKKRVIRMLIVIVVLFFLCWMPIFSANAWRAYDTASAERRLSGTPISFILLLSY
TSSCVNPIIYCFMNKRFRLGFMATFPCCPNPGPPGARGEVGEEEEGGTTGASLSRFSYSH
MSASVPPQ
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BDBM21142 |
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[125I]CCK-8 |
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Name | BDBM21142 |
Synonyms: | (3S)-3-[(2S)-2-[(2R)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]hexanamido]acetamido}-3-(1H-indol-3-yl)-N-methylpropanamido]hexanamido]-3-{[(1S)-1-carbamoyl-2-phenylethyl]carbamoyl}propanoic acid | CCK-Opioid Peptide, 12 | Tyr-D-Nle-Gly-D-Trp-NMeNle-Asp-Phe-NH2 |
Type | Peptide |
Emp. Form. | C48H63N9O10 |
Mol. Mass. | 926.0681 |
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)[C@@H](CCCC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](Cc1ccccc1)C(N)=O |
Structure |
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