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TargetCalcitonin gene-related peptide type 1 receptor
LigandBDBM50342628
Substrate/Competitorn/a
Meas. Tech.ChEMBL_745043 (CHEMBL1772119)
IC50 4.3±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:Calcitonin gene-related peptide type 1 receptor
Synonyms:Adrenomedullin receptor AM1; CALCRL/RAMP2 | CALCRL | CALRL_HUMAN | CGRP type 1 receptor | CGRP type 1 receptor mRNA | CGRPR | Calcitonin gene-related peptide (CGRP) receptor | Calcitonin gene-related peptide 1 (CGRP) | Calcitonin receptor-like receptor | Calcitonin receptor-like receptor (CLR) | Human CL receptor
Type:Enzyme Catalytic Domain
Mol. Mass.:52980.45
Organism:Homo sapiens (Human)
Description:Q16602
Residue:461
Sequence:
MEKKCTLYFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQA
EGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRT
WTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNL
FFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTL
IVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICA
ALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKI
AEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSAS
YTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50342628
n/a
NameBDBM50342628
Synonyms:CHEMBL1770718 | N-((6S,9R)-6-(2,3-difluorophenyl)-3-(methoxymethyl)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepin-9-yl)-2'-oxo-1',2'-dihydrospiro[piperidine-4,3'-pyrrolo[2,3-b]pyridine]-1-carboxamide
TypeSmall organic molecule
Emp. Form.C28H30F2N6O3
Mol. Mass.536.573
SMILESCOCc1cnc2[C@@H](CC[C@H](Cn12)c1cccc(F)c1F)NC(=O)N1CCC2(CC1)C(=O)Nc1ncccc21 |r|
Structure
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