Reaction Details |
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Target | Calcitonin gene-related peptide type 1 receptor |
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Ligand | BDBM50342620 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_745043 (CHEMBL1772119) |
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IC50 | 7.4±n/a nM |
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Citation | Paone, DV; Nguyen, DN; Shaw, AW; Burgey, CS; Potteiger, CM; Deng, JZ; Mosser, SD; Salvatore, CA; Yu, S; Roller, S; Kane, SA; Selnick, HG; Vacca, JP; Williams, TM Orally bioavailable imidazoazepanes as calcitonin gene-related peptide (CGRP) receptor antagonists: discovery of MK-2918. Bioorg Med Chem Lett21:2683-6 (2011) [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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BDBM50342620 |
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n/a |
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Name | BDBM50342620 |
Synonyms: | (6S,9R)-6-(2,3-difluorophenyl)-N,N-dimethyl-9-(4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamido)-6,7,8,9-tetrahydro-5H-imidazo[1,2-a]azepine-3-carboxamide | CHEMBL1770565 |
Type | Small organic molecule |
Emp. Form. | C29H32F2N8O3 |
Mol. Mass. | 578.613 |
SMILES | CN(C)C(=O)c1cnc2[C@@H](CC[C@H](Cn12)c1cccc(F)c1F)NC(=O)N1CCC(CC1)n1c2cccnc2[nH]c1=O |r| |
Structure |
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