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Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50224431
Substrate
n/a
Meas. Tech.
ChEMBL_582536 (CHEMBL1060869)
IC50
11±n/a nM
Citation
 Bell, IM; Bednar, RA; Corcoran, HA; Fay, JF; Gallicchio, SN; Johnston, VK; Hershey, JC; Miller-Stein, CM; Moore, EL; Mosser, SD; Roller, SA; Salvatore, CA; Theberge, CR; Wong, BK; Blair Zartman, C; Kane, SA; Williams, TM; Graham, SL; Vacca, JP The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists. Bioorg Med Chem Lett 19:4740-2 (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:
BDBM50224431
Synonyms:
CHEMBL236593 | MK-0974 | N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide | Telcagepant
Type:
Small organic molecule
Emp. Form.:
C26H27F5N6O3
Mol. Mass.:
566.523
SMILES:
Fc1cccc([C@@H]2CC[C@@H](NC(=O)N3CCC(CC3)n3c4cccnc4[nH]c3=O)C(=O)N(CC(F)(F)F)C2)c1F
Structure:
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