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TargetCalcitonin gene-related peptide type 1 receptor
LigandBDBM50385309
Substrate/Competitorn/a
Meas. Tech.ChEMBL_822705 (CHEMBL2040022)
IC50 0.340000±n/a nM
Citation Bell, IMStump, CAGallicchio, SNStaas, DDZartman, CBMoore, ELSain, NUrban, MBruno, JGCalamari, AKemmerer, ALMosser, SDFandozzi, CWhite, RBZrada, MMSelnick, HGGraham, SLVacca, JPKane, SASalvatore, CA MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. Bioorg Med Chem Lett22:3941-5 (2012) [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:
BDBM50385309
n/a
NameBDBM50385309
Synonyms:CHEMBL2035983
TypeSmall organic molecule
Emp. Form.C31H30F2N6O3
Mol. Mass.572.6051
SMILESC[C@]1(CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2C[C@]3(Cc2c1)C(=O)Nc1ncccc31)c1cc(F)cc(F)c1 |r|
Structure
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