Reaction Details |
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Target | Parathyroid hormone/parathyroid hormone-related peptide receptor |
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Ligand | BDBM50600473 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2234293 (CHEMBL5148065) |
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IC50 | 280±n/a nM |
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Citation | Arai, Y; Kiyotsuka, Y; Nagamochi, M; Oyama, K; Izumi, M Lead optimization of pyrido[2,3-d][1]benzazepin-6-one derivatives leading to the discovery of a potent, selective, and orally available human parathyroid hormone receptor 1 (hPTHR1) antagonist (DS69910557). Bioorg Med Chem64:0 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Parathyroid hormone/parathyroid hormone-related peptide receptor |
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Name: | Parathyroid hormone/parathyroid hormone-related peptide receptor |
Synonyms: | PTH/PTHr receptor | PTH/PTHrP type I receptor | PTH1 receptor | PTH1R | PTH1R_HUMAN | PTHR | PTHR1 | Parathyroid hormone 1 receptor | Parathyroid hormone receptor |
Type: | Enzyme Catalytic Domain |
Mol. Mass.: | 66370.95 |
Organism: | Homo sapiens (Human) |
Description: | PARATHYROID HT1 0 HUMAN::Q03431 |
Residue: | 593 |
Sequence: | MGTARIAPGLALLLCCPVLSSAYALVDADDVMTKEEQIFLLHRAQAQCEKRLKEVLQRPA
SIMESDKGWTSASTSGKPRKDKASGKLYPESEEDKEAPTGSRYRGRPCLPEWDHILCWPL
GAPGEVVAVPCPDYIYDFNHKGHAYRRCDRNGSWELVPGHNRTWANYSECVKFLTNETRE
REVFDRLGMIYTVGYSVSLASLTVAVLILAYFRRLHCTRNYIHMHLFLSFMLRAVSIFVK
DAVLYSGATLDEAERLTEEELRAIAQAPPPPATAAAGYAGCRVAVTFFLYFLATNYYWIL
VEGLYLHSLIFMAFFSEKKYLWGFTVFGWGLPAVFVAVWVSVRATLANTGCWDLSSGNKK
WIIQVPILASIVLNFILFINIVRVLATKLRETNAGRCDTRQQYRKLLKSTLVLMPLFGVH
YIVFMATPYTEVSGTLWQVQMHYEMLFNSFQGFFVAIIYCFCNGEVQAEIKKSWSRWTLA
LDFKRKARSGSSSYSYGPMVSHTSVTNVGPRVGLGLPLSPRLLPTATTNGHPQLPGHAKP
GTPALETLETTPPAMAAPKDDGFLNGSCSGLDEEASGPERPPALLQEEWETVM
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BDBM50600473 |
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n/a |
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Name | BDBM50600473 |
Synonyms: | CHEMBL5183438 |
Type | Small organic molecule |
Emp. Form. | C30H32Cl2N4O2 |
Mol. Mass. | 551.507 |
SMILES | CC1(C)c2ncc(Cl)cc2-c2ccc(Cl)cc2N(c2ccc(cc2)N2CC(CNC3CCOCC3)C2)C1=O |
Structure |
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