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Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM50440788
Substrate
n/a
Meas. Tech.
ChEMBL_986467 (CHEMBL2434392)
Ki
0.017000±n/a nM
Citation
 Bell, IM; Gallicchio, SN; Stump, CA; Bruno, JG; Fan, H; Gantert, LT; Hostetler, ED; Kemmerer, AL; McWherter, M; Moore, EL; Mosser, SD; Purcell, ML; Riffel, K; Salvatore, CA; Sanabria-Bohórquez, S; Staas, DD; White, RB; Williams, M; Zartman, CB; Cook, JJ; Hargreaves, RJ; Kane, SA; Graham, SL; Selnick, HG [(11)C]MK-4232: The First Positron Emission Tomography Tracer for the Calcitonin Gene-Related Peptide Receptor. ACS Med Chem Lett 4:863-8 (2013) [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:
BDBM50440788
Synonyms:
CHEMBL2431249
Type:
Small organic molecule
Emp. Form.:
C32H32F2N6O3
Mol. Mass.:
586.6317
SMILES:
CN1C[C@](C)(N(CC(=O)Nc2cnc3C[C@]4(Cc3c2)C(=O)Nc2ncccc42)C(=O)C11CCCC1)c1cc(F)cc(F)c1 |r|
Structure:
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