Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50441042
Substrate
n/a
Meas. Tech.
ChEMBL_985765 (CHEMBL2433982)
IC50
1.7±n/a nM
Citation
 Tora, GDegnan, APConway, CMKostich, WADavis, CDPin, SSSchartman, RXu, CWidmann, KAMacor, JEDubowchik, GM Preparation of imidazoles as potent calcitonin gene-related peptide (CGRP) antagonists. Bioorg Med Chem Lett 23:5684-8 (2013) [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:
BDBM50441042
Synonyms:
CHEMBL2430164 | US9695176, 2
Type:
Small organic molecule
Emp. Form.:
C33H37N7O3
Mol. Mass.:
579.692
SMILES:
CCN1CCn2c(C1)cnc2C(Cc1cc(C)c2[nH]ncc2c1)OC(=O)N1CCC(CC1)c1cc2ccccc2[nH]c1=O
Structure:
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