Reaction Details Report a problem with these data
Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50254937
Substrate
n/a
Meas. Tech.
ChEMBL_560218 (CHEMBL1015393)
Ki
130±n/a nM
Citation
Stump, CA; Bell, IM; Bednar, RA; Bruno, JG; Fay, JF; Gallicchio, SN; Johnston, VK; Moore, EL; Mosser, SD; Quigley, AG; Salvatore, CA; Theberge, CR; Blair Zartman, C; Zhang, XF; Kane, SA; Graham, SL; Vacca, JP; Williams, TM The discovery of highly potent CGRP receptor antagonists. Bioorg Med Chem Lett 19:214-7 (2008) [PubMed] Article
More Info.:
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:
BDBM50254937
Synonyms:
(R)-N-(5-oxo-2-(pyridin-3-yl)-1,1',3',5-tetrahydrospiro[imidazole-4,2'-indene]-5'-yl)-2-(2-oxo-3-(pyridin-2-yl)-2,3-dihydro-1H-benzo[d]imidazol-1-yl)acetamide | CHEMBL472829
Type:
Small organic molecule
Emp. Form.:
C30H23N7O3
Mol. Mass.:
529.5487
SMILES:
O=C(Cn1c2ccccc2n(-c2ccccn2)c1=O)Nc1ccc2C[C@]3(Cc2c1)N=C(NC3=O)c1cccnc1 |r,c:34|