Ki Summary new BindingDB logo
myBDB logout
Reaction Details
Report a problem with these data
TargetCalcitonin gene-related peptide type 1 receptor
LigandBDBM50184069
Substrate/Competitorn/a
Meas. Tech.ChEMBL_969057
Ki 0.010000±n/a nM
Citation Chaturvedula PVMercer SEPin SSThalody GXu CConway CMKeavy DSignor LCantor GHMathias NMoench PDenton RMacci RSchartman RWhiterock VDavis CMacor JEDubowchik GM Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery. Bioorg Med Chem Lett 23:3157-61 (2013) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Calcitonin gene-related peptide type 1 receptor
Name:Adrenomedullin receptor AM1; CALCRL/RAMP2
Synonyms:Calcitonin gene-related peptide (CGRP) receptor | Calcitonin gene-related peptide 1 (CGRP) | Calcitonin receptor-like receptor
Type:Enzyme
Mol. Mass.:52931.38
Organism:Homo sapiens (Human)
Description:Q16602
Residue:461
Sequence:
MEKKCTLNFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQA
EGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRT
WTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNL
FFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTL
IVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICA
ALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKI
AEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSAS
YTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50184069
n/a
NameBDBM50184069
Synonyms:CHEMBL207197 | N-((R)-1-((S)-6-amino-1-oxo-1-(4-(pyridin-4-yl)piperazin-1-yl)hexan-2-ylamino)-3-(3,5-dibromo-4-hydroxyphenyl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxamide | N-{(1S)-5-amino-1-[(4-pyridin-4-ylpiperazin-1-yl)carbonyl]pentyl}-3,5-dibromo-Nalpha-{[4-(2-oxo-1,4-dihydroquinazolin-3(2H)-yl)piperidin-1-yl]carbonyl}-D-tyrosinamide | OLCEGEPANT
TypeSmall organic molecule
Emp. Form.C38H47Br2N9O5
Mol. Mass.869.645
SMILESNCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)N1CCC(CC1)N1Cc2ccccc2NC1=O)C(=O)N1CCN(CC1)c1ccncc1
Structure
Search PDB for entries with ligand similarity:Similarity to this molecule at least: