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Target
Parathyroid hormone/parathyroid hormone-related peptide receptor
Ligand
BDBM50269979
Substrate
n/a
Meas. Tech.
ChEMBL_505729 (CHEMBL945435)
IC50
5780±n/a nM
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 A 104:6846-51 (2007) [PubMed]  Article 
Target
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:
MGTARIAPGLALLLCCPVLSSAYALVDADDVMTKEEQIFLLHRAQAQCEKRLKEVLQRPASIMESDKGWTSASTSGKPRKDKASGKLYPESEEDKEAPTGSRYRGRPCLPEWDHILCWPLGAPGEVVAVPCPDYIYDFNHKGHAYRRCDRNGSWELVPGHNRTWANYSECVKFLTNETREREVFDRLGMIYTVGYSVSLASLTVAVLILAYFRRLHCTRNYIHMHLFLSFMLRAVSIFVKDAVLYSGATLDEAERLTEEELRAIAQAPPPPATAAAGYAGCRVAVTFFLYFLATNYYWILVEGLYLHSLIFMAFFSEKKYLWGFTVFGWGLPAVFVAVWVSVRATLANTGCWDLSSGNKKWIIQVPILASIVLNFILFINIVRVLATKLRETNAGRCDTRQQYRKLLKSTLVLMPLFGVHYIVFMATPYTEVSGTLWQVQMHYEMLFNSFQGFFVAIIYCFCNGEVQAEIKKSWSRWTLALDFKRKARSGSSSYSYGPMVSHTSVTNVGPRVGLGLPLSPRLLPTATTNGHPQLPGHAKPGTPALETLETTPPAMAAPKDDGFLNGSCSGLDEEASGPERPPALLQEEWETVM
  
Inhibitor
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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