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Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50382779
Substrate
n/a
Meas. Tech.
ChEMBL_815265 (CHEMBL2025456)
IC50
0.1±n/a nM
Citation
 Luo, G; Chen, L; Civiello, R; Pin, SS; Xu, C; Kostich, W; Kelley, M; Conway, CM; Macor, JE; Dubowchik, GM Calcitonin gene-related peptide (CGRP) receptor antagonists: pyridine as a replacement for a core amide group. Bioorg Med Chem Lett 22:2917-21 (2012) [PubMed]  Article 
Target
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:
MEKKCTLYFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQAEGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRTWTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNLFFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTLIVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICAALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKIAEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSASYTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN
  
Inhibitor
Name:
BDBM50382779
Synonyms:
CHEMBL2022601
Type:
Small organic molecule
Emp. Form.:
C35H41N7O3
Mol. Mass.:
607.7451
SMILES:
Cc1cc(CC(OC(=O)N2CCC(CC2)N2Cc3ccccc3NC2=O)c2cc(CN3CCCCC3)ccn2)cc2cn[nH]c12
Structure:
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