| Reaction Details |
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 | Report a problem with these data |
| Target | Calcitonin gene-related peptide type 1 receptor |
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| Ligand | BDBM50224437 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_450785 (CHEMBL899870) |
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| Ki | 470±n/a nM |
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| Citation |  Paone, DV; Shaw, AW; Nguyen, DN; Burgey, CS; Deng, JZ; Kane, SA; Koblan, KS; Salvatore, CA; Mosser, SD; Johnston, VK; Wong, BK; Miller-Stein, CM; Hershey, JC; Graham, SL; Vacca, JP; Williams, TM Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974). J Med Chem50:5564-7 (2007) [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 |
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| 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 |
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| Type: | Enzyme Catalytic Domain |
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| Mol. Mass.: | 52980.45 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q16602 |
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| Residue: | 461 |
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| Sequence: | MEKKCTLYFLVLLPFFMILVTAELEESPEDSIQLGVTRNKIMTAQYECYQKIMQDPIQQA
EGVYCNRTWDGWLCWNDVAAGTESMQLCPDYFQDFDPSEKVTKICDQDGNWFRHPASNRT
WTNYTQCNVNTHEKVKTALNLFYLTIIGHGLSIASLLISLGIFFYFKSLSCQRITLHKNL
FFSFVCNSVVTIIHLTAVANNQALVATNPVSCKVSQFIHLYLMGCNYFWMLCEGIYLHTL
IVVAVFAEKQHLMWYYFLGWGFPLIPACIHAIARSLYYNDNCWISSDTHLLYIIHGPICA
ALLVNLFFLLNIVRVLITKLKVTHQAESNLYMKAVRATLILVPLLGIEFVLIPWRPEGKI
AEEVYDYIMHILMHFQGLLVSTIFCFFNGEVQAILRRNWNQYKIQFGNSFSNSEALRSAS
YTVSTISDGPGYSHDCPSEHLNGKSIHDIENVLLKPENLYN
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| BDBM50224437 |
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| n/a |
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| Name | BDBM50224437 |
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| Synonyms: | 4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)-N-[(3R)-2-oxo-6-(3-thienyl)azepan-3-yl]piperidine-1-carboxamide | CHEMBL240686 |
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| Type | Small organic molecule |
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| Emp. Form. | C22H26N6O3S |
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| Mol. Mass. | 454.545 |
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| SMILES | O=C(N[C@@H]1CCC(CNC1=O)c1ccsc1)N1CCC(CC1)n1c2cccnc2[nH]c1=O |
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| Structure | 
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