Reaction Details |
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Target | Parathyroid hormone/parathyroid hormone-related peptide receptor |
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Ligand | BDBM50269979 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_505703 (CHEMBL944465) |
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IC50 | 990±n/a nM |
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Citation | Carter, PH; Liu, RQ; Foster, WR; Tamasi, JA; Tebben, AJ; Favata, M; Staal, A; Cvijic, ME; French, MH; Dell, V; Apanovitch, D; Lei, M; Zhao, Q; Cunningham, M; Decicco, CP; Trzaskos, JM; Feyen, JH Discovery of a small molecule antagonist of the parathyroid hormone receptor by using an N-terminal parathyroid hormone peptide probe. Proc Natl Acad Sci U S A104:6846-51 (2007) [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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BDBM50269979 |
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n/a |
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Name | BDBM50269979 |
Synonyms: | CHEMBL515170 | r-5-(2-E-cyclopropylvinyl)-t-3-ethyl-6,7-difluoro-5-(trifluoromethyl)benzo[e][1,4]-oxazepin-2(1H,3H,5H)-one |
Type | Small organic molecule |
Emp. Form. | C17H16F5NO2 |
Mol. Mass. | 361.3065 |
SMILES | CC[C@@H]1O[C@@](\C=C\C2CC2)(c2c(F)c(F)ccc2NC1=O)C(F)(F)F |r| |
Structure |
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