Reaction Details |
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Target | Calcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1 |
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Ligand | BDBM50385309 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_822688 (CHEMBL2040005) |
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Ki | 0.047±n/a nM |
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Citation | Bell, IM; Stump, CA; Gallicchio, SN; Staas, DD; Zartman, CB; Moore, EL; Sain, N; Urban, M; Bruno, JG; Calamari, A; Kemmerer, AL; Mosser, SD; Fandozzi, C; White, RB; Zrada, MM; Selnick, HG; Graham, SL; Vacca, JP; Kane, SA; Salvatore, CA MK-8825: a potent and selective CGRP receptor antagonist with good oral activity in rats. Bioorg Med Chem Lett22:3941-5 (2012) [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/Receptor activity-modifying protein 1 |
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Name: | Calcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1 |
Synonyms: | Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 327200 |
Components: | This complex has 2 components. |
Component 1 |
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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Component 2 |
Name: | Receptor activity-modifying protein 1 |
Synonyms: | Calcitonin-gene-related peptide receptor, CALCRL/RAMP1 | RAMP1 | RAMP1_HUMAN |
Type: | PROTEIN |
Mol. Mass.: | 16992.80 |
Organism: | Homo sapiens (Human) |
Description: | EBI_100673 |
Residue: | 148 |
Sequence: | MARALCRLPRRGLWLLLAHHLFMTTACQEANYGALLRELCLTQFQVDMEAVGETLWCDWG
RTIRSYRELADCTWHMAEKLGCFWPNAEVDRFFLAVHGRYFRSCPISGRAVRDPPGSILY
PFIVVPITVTLLVTALVVWQSKRTEGIV
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BDBM50385309 |
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n/a |
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Name | BDBM50385309 |
Synonyms: | CHEMBL2035983 |
Type | Small organic molecule |
Emp. Form. | C31H30F2N6O3 |
Mol. Mass. | 572.6051 |
SMILES | C[C@]1(CNC2(CCCC2)C(=O)N1CC(=O)Nc1cnc2C[C@]3(Cc2c1)C(=O)Nc1ncccc31)c1cc(F)cc(F)c1 |r| |
Structure |
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