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TargetParathyroid hormone/parathyroid hormone-related peptide receptor
LigandBDBM50600473
Substrate/Competitorn/a
Meas. Tech.ChEMBL_2234293 (CHEMBL5148065)
IC50 280±n/a nM
Citation Arai, YKiyotsuka, YNagamochi, MOyama, KIzumi, 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
More Info.:Get all data from this article,  Assay Method
 
Parathyroid hormone/parathyroid hormone-related peptide receptor
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
Blast this sequence in BindingDB or PDB
  Blast E-value cutoff:
BDBM50600473
n/a
NameBDBM50600473
Synonyms:CHEMBL5183438
TypeSmall organic molecule
Emp. Form.C30H32Cl2N4O2
Mol. Mass.551.507
SMILESCC1(C)c2ncc(Cl)cc2-c2ccc(Cl)cc2N(c2ccc(cc2)N2CC(CNC3CCOCC3)C2)C1=O
Structure
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