Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50192544
Substrate
n/a
Meas. Tech.
ChEMBL_402775 (CHEMBL908626)
Ki
1000±n/a nM
Citation
 Burgey, CSStump, CANguyen, DNDeng, JZQuigley, AGNorton, BRBell, IMMosser, SDSalvatore, CARutledge, RZKane, SAKoblan, KSVacca, JPGraham, SLWilliams, TM Benzodiazepine calcitonin gene-related peptide (CGRP) receptor antagonists: optimization of the 4-substituted piperidine. Bioorg Med Chem Lett 16:5052-6 (2006) [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:
BDBM50192544
Synonyms:
4-(2-oxo-4-oxy-2,3-dihydro-imidazo[4,5-b]pyridin-1-yl)-piperidine-1-carboxylic acid [(R)-2-oxo-5-phenyl-1-(2,2,2-trifluoro-ethyl)-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]-amide | CHEMBL214950
Type:
Small organic molecule
Emp. Form.:
C29H26F3N7O4
Mol. Mass.:
593.5564
SMILES:
Oc1nc2[n+]([O-])cccc2n1C1CCN(CC1)C(=O)N[C@@H]1N=C(c2ccccc2)c2ccccc2N(CC(F)(F)F)C1=O |t:24|
Structure:
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