Reaction Details |
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Target | Substance-P receptor |
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Ligand | BDBM50002454 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEBML_208650 |
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IC50 | 500±n/a nM |
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Citation | Lawrence, KB; Venepalli, BR; Appell, KC; Goswami, R; Logan, ME; Tomczuk, BE; Yanni, JM Synthesis and substance P antagonist activity of naphthimidazolium derivatives. J Med Chem35:1273-9 (1992) [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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BDBM50002454 |
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n/a |
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Name | BDBM50002454 |
Synonyms: | CHEMBL386306 | D-Lys(Nicotinoyl)-Pro(3-Pyridyl)-Ala-Pro(3,4-dichloro)-D-Phe-Asn-D-Trp-Phe-D-Trp-Leu-Nle (Spantide) |
Type | Small organic molecule |
Emp. Form. | C86H103Cl2N17O14 |
Mol. Mass. | 1669.75 |
SMILES | CCCC[C@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](Cc1ccccc1)NC(=O)[C@@H]1C(Cl)C(Cl)CN1C(=O)[C@H](C)NC(=O)[C@@H]1C(CCN1C(=O)[C@H](CCCCN)NC(=O)c1cccnc1)c1cccnc1)C(O)=O |
Structure |
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