Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50268473
Substrate
n/a
Meas. Tech.
ChEMBL_523854 (CHEMBL1004155)
IC50
0.022±n/a nM
Citation
 Degnan, APConway, CMDalterio, RAMacci, RMercer, SESchartman, RXu, CDubowchik, GMMacor, JE Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. Bioorg Med Chem Lett 19:3555-8 (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:
BDBM50268473
Synonyms:
(R)-1-(1,4'-bipiperidin-1'-yl)-3-(7-methyl-1H-indazol-5-yl)-1-oxopropan-2-yl 4-(7-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxylate | CHEMBL451164
Type:
Small organic molecule
Emp. Form.:
C35H44FN7O4
Mol. Mass.:
645.7668
SMILES:
Cc1cc(C[C@@H](OC(=O)N2CCC(CC2)N2Cc3ccc(F)cc3NC2=O)C(=O)N2CCC(CC2)N2CCCCC2)cc2cn[nH]c12 |r|
Structure:
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