Reaction Details |
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Target | Substance-P receptor |
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Ligand | BDBM21015 |
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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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BDBM21015 |
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n/a |
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Name | BDBM21015 |
Synonyms: | (2S)-2-{2-[(2R)-2-[(2S)-2-amino-3-(4-hydroxyphenyl)propanamido]propanamido]-N-methylacetamido}-N-(2-hydroxyethyl)-3-phenylpropanamide | 2-Ala-4-MePhe-5-Gly-Enkephalin | CHEMBL38874 | D-Ala2-MePhe4-Met(0)5-enkephalin-ol | DAMGO | RX 783006 | US11492374, ID 2 | [3H]DAMGO | [tyrosyl-3,5-3H(N)]-D-Ala2-Mephe4-glyol5-enkephalin |
Type | Analgesics |
Emp. Form. | C26H35N5O6 |
Mol. Mass. | 513.586 |
SMILES | C[C@@H](NC(=O)[C@@H](N)Cc1ccc(O)cc1)C(=O)NCC(=O)N(C)[C@@H](Cc1ccccc1)C(=O)NCCO |
Structure |
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