Target
Calcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1
Ligand
BDBM50217483
Substrate
n/a
Meas. Tech.
ChEMBL_448633 (CHEMBL897783)
Ki
35±n/a nM
Citation
 Shaw, AWPaone, DVNguyen, DNStump, CABurgey, CSMosser, SDSalvatore, CARutledge, RZKane, SAKoblan, KSGraham, SLVacca, JPWilliams, TM Caprolactams as potent CGRP receptor antagonists for the treatment of migraine. Bioorg Med Chem Lett 17:4795-8 (2007) [PubMed]  Article 
Target
Name:
Calcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1
Synonyms:
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of EBI is 327200
Components:
This complex has 2 components.
Component 1
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
  
Component 2
Name:
Receptor activity-modifying protein 1
Synonyms:
Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 | RAMP1 | RAMP1_HUMAN
Type:
PROTEIN
Mol. Mass.:
16992.80
Organism:
Homo sapiens (Human)
Description:
EBI_100673
Residue:
148
Sequence:
MARALCRLPRRGLWLLLAHHLFMTTACQEANYGALLRELCLTQFQVDMEAVGETLWCDWGRTIRSYRELADCTWHMAEKLGCFWPNAEVDRFFLAVHGRYFRSCPISGRAVRDPPGSILYPFIVVPITVTLLVTALVVWQSKRTEGIV
  
Inhibitor
Name:
BDBM50217483
Synonyms:
(cis racemic)-N-(1-(cyclopropylmethyl)-2-oxo-5-phenylazepan-3-yl)-4-(2-oxo-4-phenyl-2,3-dihydroimidazol-1-yl)piperidine-1-carboxamide | (trans racemic)-N-(1-(cyclopropylmethyl)-2-oxo-5-phenylazepan-3-yl)-4-(2-oxo-4-phenyl-2,3-dihydroimidazol-1-yl)piperidine-1-carboxamide | CHEMBL235457
Type:
Small organic molecule
Emp. Form.:
C31H37N5O3
Mol. Mass.:
527.6572
SMILES:
O=C(NC1CC(CCN(CC2CC2)C1=O)c1ccccc1)N1CCC(CC1)n1cc([nH]c1=O)-c1ccccc1
Structure:
Search PDB for entries with ligand similarity: