Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50246312
Substrate
n/a
Meas. Tech.
ChEMBL_558102 (CHEMBL956592)
Ki
1.7±n/a nM
Citation
 Theberge, CRBednar, RABell, IMCorcoran, HAFay, JFHershey, JCJohnston, VKKane, SAMosser, SSalvatore, CAWilliams, TMZartman, CBZhang, XFGraham, SLVacca, 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:
BDBM50246312
Synonyms:
(R)-2-(5,7-dimethyl-3-(2-(3-methyl-2,5-dioxo-1',3'-dihydrospiro[imidazolidine-4,2'-indene]-5'-ylamino)-2-oxoethyl)-2-oxo-2,3-dihydro-1H-benzo[d]imidazol-1-yl)-N,N-dimethylacetamide | CHEMBL519421
Type:
Small organic molecule
Emp. Form.:
C27H30N6O5
Mol. Mass.:
518.5643
SMILES:
CN(C)C(=O)Cn1c2c(C)cc(C)cc2n(CC(=O)Nc2ccc3C[C@]4(Cc3c2)N(C)C(=O)NC4=O)c1=O |r|
Structure:
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