| 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 | BDBM50224431 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_969057 (CHEMBL2400791) |
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| Ki | 0.770000±n/a nM |
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| Citation |  Chaturvedula, PV; Mercer, SE; Pin, SS; Thalody, G; Xu, C; Conway, CM; Keavy, D; Signor, L; Cantor, GH; Mathias, N; Moench, P; Denton, R; Macci, R; Schartman, R; Whiterock, V; Davis, C; Macor, JE; Dubowchik, GM Discovery of (R)-N-(3-(7-methyl-1H-indazol-5-yl)-1-(4-(1-methylpiperidin-4-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinolin-3-yl)piperidine-1-carboxamide (BMS-742413): a potent human CGRP antagonist with superior safety profile for the treatment of migraine through intranasal delivery. Bioorg Med Chem Lett23:3157-61 (2013) [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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| BDBM50224431 |
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| n/a |
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| Name | BDBM50224431 |
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| Synonyms: | CHEMBL236593 | MK-0974 | 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 | Telcagepant |
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| Type | Small organic molecule |
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| Emp. Form. | C26H27F5N6O3 |
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| Mol. Mass. | 566.523 |
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| SMILES | Fc1cccc([C@@H]2CC[C@@H](NC(=O)N3CCC(CC3)n3c4cccnc4[nH]c3=O)C(=O)N(CC(F)(F)F)C2)c1F |
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| Structure | 
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