Reaction Details |
![](/images/Email.png) | Report a problem with these data |
Target | Calcitonin gene-related peptide type 1 receptor |
---|
Ligand | BDBM50173474 |
---|
Substrate/Competitor | n/a |
---|
Meas. Tech. | ChEMBL_321593 (CHEMBL884701) |
---|
pH | 7.4±n/a |
---|
IC50 | >300000±n/a nM |
---|
Comments | extracted |
---|
Citation | Rudolf, K; Eberlein, W; Engel, W; Pieper, H; Entzeroth, M; Hallermayer, G; Doods, H Development of human calcitonin gene-related peptide (CGRP) receptor antagonists. 1. Potent and selective small molecule CGRP antagonists. 1-[N2-[3,5-dibromo-N-[[4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl]carbonyl]-D-tyrosyl]-l-lysyl]-4-(4-pyridinyl)piperazine: the first CGRP antagonist J Med Chem48:5921-31 (2005) [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
|
|
|
BDBM50173474 |
---|
n/a |
---|
Name | BDBM50173474 |
Synonyms: | CHEMBL197079 | N-{(S)-2-(4-Amino-3,5-dibromo-phenyl)-1-[(R)-5-amino-1-(piperazine-1-carbonyl)-pentylcarbamoyl]-ethyl}-4-phenyl-butyramide |
Type | Small organic molecule |
Emp. Form. | C29H40Br2N6O3 |
Mol. Mass. | 680.474 |
SMILES | NCCCC[C@@H](NC(=O)[C@H](Cc1cc(Br)c(N)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)N1CCNCC1 |
Structure |
|