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TargetCalcitonin gene-related peptide type 1 receptor
LigandBDBM50268484
Substrate/Competitorn/a
Meas. Tech.ChEMBL_510084 (CHEMBL998738)
EC50 0.034500±n/a nM
Citation Degnan, APChaturvedula, PVConway, CMCook, DADavis, CDDenton, RHan, XMacci, RMathias, NRMoench, PPin, SSRen, SXSchartman, RSignor, LJThalody, GWidmann, KAXu, CMacor, JEDubowchik, GM Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and effic J Med Chem51:4858-61 (2008) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Calcitonin gene-related peptide type 1 receptor
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:
MEKKCTLYFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQA
EGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRT
WTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNL
FFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTL
IVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICA
ALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKI
AEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSAS
YTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN
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BDBM50268484
n/a
NameBDBM50268484
Synonyms:(R)-4-(8-Fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide | (R)-N-(1-(1,4'-bipiperidin-1'-yl)-3-(7-methyl-1H-indazol-5-yl)-1-oxopropan-2-yl)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxamide | BMS-694153 | CHEMBL450668
TypeSmall organic molecule
Emp. Form.C35H45FN8O3
Mol. Mass.644.782
SMILESCc1cc(C[C@@H](NC(=O)N2CCC(CC2)N2Cc3cccc(F)c3NC2=O)C(=O)N2CCC(CC2)N2CCCCC2)cc2cn[nH]c12 |r|
Structure
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