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Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50246273
Substrate
n/a
Meas. Tech.
ChEMBL_558103 (CHEMBL959032)
IC50
13±n/a nM
Citation
 Theberge, CR; Bednar, RA; Bell, IM; Corcoran, HA; Fay, JF; Hershey, JC; Johnston, VK; Kane, SA; Mosser, S; Salvatore, CA; Williams, TM; Zartman, CB; Zhang, XF; Graham, SL; Vacca, JP Potent benzimidazolone-based CGRP receptor antagonists. Bioorg Med Chem Lett 18:6122-5 (2008) [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:
BDBM50246273
Synonyms:
(R)-2-(3-(2-amino-2-oxoethyl)-4,6-dimethyl-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)-N-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-yl)acetamide | CHEMBL487068
Type:
Small organic molecule
Emp. Form.:
C25H26N6O5
Mol. Mass.:
490.5111
SMILES:
CN1C(=O)NC(=O)[C@]11Cc2ccc(NC(=O)Cn3c4cc(C)cc(C)c4n(CC(N)=O)c3=O)cc2C1 |r|
Structure:
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