Reaction Details |
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Target | Substance-P receptor |
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Ligand | BDBM50081930 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_143041 (CHEMBL750290) |
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IC50 | >1000±n/a nM |
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Citation | Borg, S; Vollinga, RC; Labarre, M; Payza, K; Terenius, L; Luthman, K Design, synthesis, and evaluation of Phe-Gly mimetics: heterocyclic building blocks for pseudopeptides. J Med Chem42:4331-42 (1999) [PubMed] |
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More Info.: | Get all data from this article, Assay Method |
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Substance-P receptor |
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Name: | Substance-P receptor |
Synonyms: | NK-1 receptor | NK-1R | NK1 Receptor | NK1R_RAT | Neurokinin 1 receptor | Neurokinin NK1 | SPR | Substance-P receptor | Tac1r | Tachykinin receptor 1 | Tacr1 |
Type: | G Protein-Coupled Receptor (GPCR) |
Mol. Mass.: | 46371.54 |
Organism: | Rattus norvegicus (rat) |
Description: | Competition binding assays were carried out using membrane preparations from transfected CHO cells that constitutively expressed the rat NK1 receptor. |
Residue: | 407 |
Sequence: | MDNVLPMDSDLFPNISTNTSESNQFVQPTWQIVLWAAAYTVIVVTSVVGNVVVIWIILAH
KRMRTVTNYFLVNLAFAEACMAAFNTVVNFTYAVHNVWYYGLFYCKFHNFFPIAALFASI
YSMTAVAFDRYMAIIHPLQPRLSATATKVVIFVIWVLALLLAFPQGYYSTTETMPSRVVC
MIEWPEHPNRTYEKAYHICVTVLIYFLPLLVIGYAYTVVGITLWASEIPGDSSDRYHEQV
SAKRKVVKMMIVVVCTFAICWLPFHVFFLLPYINPDLYLKKFIQQVYLASMWLAMSSTMY
NPIIYCCLNDRFRLGFKHAFRCCPFISAGDYEGLEMKSTRYLQTQSSVYKVSRLETTIST
VVGAHEEEPEEGPKATPSSLDLTSNGSSRSNSKTMTESSSFYSNMLA
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BDBM50081930 |
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n/a |
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Name | BDBM50081930 |
Synonyms: | CHEMBL268138 | H-Arg-Pro-Lys-pro-Gln-Gln-Phe-{5-[(S)-1-amino-2-phenylethyl]-1,3,4-oxadiazol-2-ylcarbonyl}-Leu-Met-NH2 |
Type | Small organic molecule |
Emp. Form. | C62H94N18O12S |
Mol. Mass. | 1315.588 |
SMILES | CSCC[C@H](N)C(=O)N[C@@H](CC(C)C)C(=O)c1nnc(o1)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCCN)NC(=O)[C@@H]1CCCN1C(=O)[C@@H](N)CCCNC(N)=N |
Structure |
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