Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50254445
Substrate
n/a
Meas. Tech.
ChEMBL_582534 (CHEMBL1060867)
Ki
0.039±n/a nM
Citation
 Bell, IMBednar, RACorcoran, HAFay, JFGallicchio, SNJohnston, VKHershey, JCMiller-Stein, CMMoore, ELMosser, SDRoller, SASalvatore, CATheberge, CRWong, BKBlair Zartman, CKane, SAWilliams, TMGraham, SLVacca, JP The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists. Bioorg Med Chem Lett 19:4740-2 (2009) [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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