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Target
Calcitonin gene-related peptide type 1 receptor
Ligand
BDBM362181
Substrate
n/a
Meas. Tech.
Receptor Functional Assay
Ki
4.30±n/a nM
Citation
 Bell, IM; Fraley, ME; Gallicchio, SN; Ginnetti, A; Mitchell, HJ; Paone, DV; Staas, DD; Wang, C; Zartman, CB Piperidinone carboxamide azaindane CGRP receptor antagonists US Patent  US9833448 Publication Date 12/5/2017 
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:
BDBM362181
Synonyms:
US10272077, Example 32 from U.S. Pat. No. 7,390,798 | US9833448, Example 8 from US 2010/0179166
Type:
Small organic molecule
Emp. Form.:
C32H30F2N6O3
Mol. Mass.:
584.6158
SMILES:
CC(C)(O)c1cnc2[C@@H](CC[C@H](Cn12)c1cccc(F)c1F)NC(=O)c1cc2CC3(Cc2cn1)C(=O)Nc1ncccc31 |r|
Structure:
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