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Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM495117
Substrate
n/a
Meas. Tech.
Determination of Binding Affinity for CGRP Receptor by Radioligand Binding Assay in SK-N-MC Cell Membranes
Ki
0.080±n/a nM
Citation
 Kondo, A; Morita, N; Ishikawa, T; Yoshida, M; Moriyama, A; Wanajo, I Pyrrolidine derivative US Patent  US10995084 Publication Date 5/4/2021 
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:
BDBM495117
Synonyms:
US10995084, Ex. No. 4B-23
Type:
Small organic molecule
Emp. Form.:
C29H27ClF3N5O4
Mol. Mass.:
602.004
SMILES:
C[C@@H](NC(=O)c1cc(F)c(Oc2cc(C)n[nH]c2=O)c(F)c1)C(=O)N1[C@@H](CC[C@@H]1C(C)(C)C#N)c1cc(Cl)ccc1F |r|
Structure:
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