Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50315403
Substrate
n/a
Meas. Tech.
ChEMBL_626019 (CHEMBL1106147)
IC50
95±n/a nM
Citation
 Stump, CABell, IMBednar, RAFay, JFGallicchio, SNHershey, JCJelley, RKreatsoulas, CMoore, ELMosser, SDQuigley, AGRoller, SASalvatore, CASharik, SSTheberge, CRZartman, CBKane, SAGraham, SLSelnick, HGVacca, JPWilliams, TM Identification of potent, highly constrained CGRP receptor antagonists. Bioorg Med Chem Lett 20:2572-6 (2010) [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:
BDBM50315403
Synonyms:
(R)-6-methyl-1-((2'-oxo-1',2',6,8-tetrahydrospiro[cyclopenta[g]quinoline-7,3'-pyrrolo[2,3-b]pyridine]-2-yl)methyl)-1H-imidazo[1,5,4-de]quinoxaline-2,5(4H,6H)-dione | CHEMBL1090515
Type:
Small organic molecule
Emp. Form.:
C29H22N6O3
Mol. Mass.:
502.5234
SMILES:
CN1C(=O)Cn2c3c1cccc3n(Cc1ccc3cc4C[C@]5(Cc4cc3n1)C(=O)Nc1ncccc51)c2=O |r|
Structure:
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