Reaction Details |
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Target | Calcitonin gene-related peptide type 1 receptor |
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Ligand | BDBM50273291 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_509823 (CHEMBL1000504) |
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Ki | 0.260000±n/a nM |
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Citation | Degnan, AP; Chaturvedula, PV; Conway, CM; Cook, DA; Davis, CD; Denton, R; Han, X; Macci, R; Mathias, NR; Moench, P; Pin, SS; Ren, SX; Schartman, R; Signor, LJ; Thalody, G; Widmann, KA; Xu, C; Macor, JE; Dubowchik, GM Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and effic J Med Chem51:4858-61 (2008) [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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BDBM50273291 |
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n/a |
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Name | BDBM50273291 |
Synonyms: | (R)-N-(1-(1,4'-bipiperidin-1'-yl)-3-(1H-indazol-5-yl)-1-oxopropan-2-yl)-4-(2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxamide | CHEMBL454751 |
Type | Small organic molecule |
Emp. Form. | C34H44N8O3 |
Mol. Mass. | 612.765 |
SMILES | O=C(N[C@H](Cc1ccc2[nH]ncc2c1)C(=O)N1CCC(CC1)N1CCCCC1)N1CCC(CC1)N1Cc2ccccc2NC1=O |r| |
Structure |
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