Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50254445
Substrate
n/a
Meas. Tech.
ChEMBL_560218 (CHEMBL1015393)
Ki
0.04±n/a nM
Citation
 Stump, CABell, IMBednar, RABruno, JGFay, JFGallicchio, SNJohnston, VKMoore, ELMosser, SDQuigley, AGSalvatore, CATheberge, CRBlair Zartman, CZhang, XFKane, SAGraham, SLVacca, JPWilliams, TM The discovery of highly potent CGRP receptor antagonists. Bioorg Med Chem Lett 19:214-7 (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:
BDBM50254445
Synonyms:
(S)-2-(2,5-dioxo-2,4,5,6-tetrahydro-1H-imidazo[1,5,4-de]quinoxalin-1-yl)-N-(2'-oxo-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridine]-5-yl)acetamide | CHEMBL512773
Type:
Small organic molecule
Emp. Form.:
C26H20N6O4
Mol. Mass.:
480.4748
SMILES:
O=C(Cn1c2cccc3NC(=O)Cn(c23)c1=O)Nc1ccc2C[C@@]3(Cc2c1)C(=O)Nc1ncccc31 |r|
Structure:
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