Reaction Details |
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Target | Calcitonin gene-related peptide type 1 receptor |
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Ligand | BDBM50173483 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_321593 (CHEMBL884701) |
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pH | 7.4±n/a |
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IC50 | >300000±n/a nM |
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Comments | extracted |
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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 |
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More Info.: | Get all data from this article, Assay Method |
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Calcitonin gene-related peptide type 1 receptor |
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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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BDBM50173483 |
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n/a |
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Name | BDBM50173483 |
Synonyms: | (S)-6-Amino-2-[(R)-3-(3,5-dibromo-4-hydroxy-phenyl)-2-(4-phenyl-butyrylamino)-propionylamino]-hexanoic acid phenethyl-amide | CHEMBL196582 |
Type | Small organic molecule |
Emp. Form. | C33H40Br2N4O4 |
Mol. Mass. | 716.503 |
SMILES | NCCCC[C@H](NC(=O)[C@@H](Cc1cc(Br)c(O)c(Br)c1)NC(=O)CCCc1ccccc1)C(=O)NCCc1ccccc1 |
Structure |
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