Reaction Details |
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Target | Calcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1 |
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Ligand | BDBM50184068 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_353840 (CHEMBL864503) |
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IC50 | 990±n/a nM |
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Citation | Williams, TM; Stump, CA; Nguyen, DN; Quigley, AG; Bell, IM; Gallicchio, SN; Zartman, CB; Wan, BL; Penna, KD; Kunapuli, P; Kane, SA; Koblan, KS; Mosser, SD; Rutledge, RZ; Salvatore, C; Fay, JF; Vacca, JP; Graham, SL Non-peptide calcitonin gene-related peptide receptor antagonists from a benzodiazepinone lead. Bioorg Med Chem Lett16:2595-8 (2006) [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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BDBM50184068 |
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n/a |
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Name | BDBM50184068 |
Synonyms: | (R)-N-(1-ethyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)-4-(2-oxo-1,2-dihydroquinazolin-3(4H)-yl)piperidine-1-carboxamide | CHEMBL211052 |
Type | Small organic molecule |
Emp. Form. | C31H32N6O3 |
Mol. Mass. | 536.6242 |
SMILES | CCN1c2ccccc2C(=N[C@@H](NC(=O)N2CCC(CC2)N2Cc3ccccc3NC2=O)C1=O)c1ccccc1 |c:10| |
Structure |
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