Reaction Details |
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Target | Calcitonin gene-related peptide type 1 receptor/Receptor activity-modifying protein 1 |
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Ligand | BDBM50184074 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_353838 (CHEMBL866916) |
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Ki | 83±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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BDBM50184074 |
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n/a |
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Name | BDBM50184074 |
Synonyms: | (R)-N-(3-(3,5-dibromo-4-hydroxyphenyl)-1-oxo-1-(4-phenylpiperazin-1-yl)propan-2-yl)-4-(2-oxo-2,3-dihydrobenzo[d]imidazol-1-yl)piperidine-1-carboxamide | CHEMBL381585 |
Type | Small organic molecule |
Emp. Form. | C32H34Br2N6O4 |
Mol. Mass. | 726.458 |
SMILES | Oc1c(Br)cc(C[C@@H](NC(=O)N2CCC(CC2)n2c3ccccc3[nH]c2=O)C(=O)N2CCN(CC2)c2ccccc2)cc1Br |
Structure |
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