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TargetCalcitonin gene-related peptide type 1 receptor
LigandBDBM50342612
Substrate/Competitorn/a
Meas. Tech.ChEMBL_745045
Ki 0.14±n/a nM
Citation Paone, DVNguyen, DNShaw, AWBurgey, CSPotteiger, CMDeng, JZMosser, SDSalvatore, CAYu, SRoller, SKane, SASelnick, HGVacca, JPWilliams, TM Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918. Bioorg Med Chem Lett21:2683-6 (2011) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Calcitonin gene-related peptide type 1 receptor
Name:Adrenomedullin receptor AM1; CALCRL/RAMP2
Synonyms:Calcitonin gene-related peptide (CGRP) receptor | Calcitonin gene-related peptide 1 (CGRP) | Calcitonin receptor-like receptor
Type:Enzyme
Mol. Mass.:52931.38
Organism:Homo sapiens (Human)
Description:Q16602
Residue:461
Sequence:
MEKKCTLNFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQA
EGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRT
WTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNL
FFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTL
IVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICA
ALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKI
AEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSAS
YTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN
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  Blast E-value cutoff:
BDBM50342612
NameBDBM50342612
Synonyms:CHEMBL1770557 | N-((6S,9R)-6-(2,3-difluorophenyl)-3-(2,2,2-trifluoroethyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl)-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide
TypeSmall organic molecule
Emp. Form.C28H28F5N7O2
Mol. Mass.589.5596
SMILESFc1cccc([C@@H]2CC[C@@H](NC(=O)N3CCC(CC3)n3c4cccnc4[nH]c3=O)c3ncc(CC(F)(F)F)n3C2)c1F |r|
Structure
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