Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50385309
Substrate
n/a
Meas. Tech.
ChEMBL_822700 (CHEMBL2040017)
Ki
0.052000±n/a nM
Citation
 Bell, IMStump, CAGallicchio, SNStaas, DDZartman, CBMoore, ELSain, NUrban, MBruno, JGCalamari, AKemmerer, ALMosser, SDFandozzi, CWhite, RBZrada, MMSelnick, HGGraham, SLVacca, JPKane, SASalvatore, CA MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. Bioorg Med Chem Lett 22:3941-5 (2012) [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:
BDBM50385309
Synonyms:
CHEMBL2035983
Type:
Small organic molecule
Emp. Form.:
C31H30F2N6O3
Mol. Mass.:
572.6051
SMILES:
C[C@]1(CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2C[C@]3(Cc2c1)C(=O)Nc1ncccc31)c1cc(F)cc(F)c1 |r|
Structure:
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