Target Poor or Non Binder(s) Information
Target General Information | Top | ||||
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Target ID | T67710 | Target Info | |||
Target Name | Parathyroid hormone 1 receptor (PTH1R) | ||||
Synonyms |
Parathyroid hormone-related peptide (PTHRP); PTH1R; PTH/PTHrP type I receptor; PTH/PTHr receptor
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Target Type | Successful Target | ||||
Gene Name | PTH1R | ||||
Biochemical Class | GPCR secretin | ||||
UniProt ID |
Poor Binders of This Target (in total, 4 binders) | Download | Top | |||
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Compound Name |
Chembl4203200
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Investigative | Compound Info | ||
Synonyms |
BDBM50457785
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Activity |
EC50 = 50000 nM
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[1] | |||
Compound Name |
Chembl4213349
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Investigative | Compound Info | ||
Synonyms |
BDBM50457779
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Activity |
EC50 = 67000 nM
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[1] | |||
Compound Name |
(3S,5S)-5-[(E)-2-Cyclopropylethenyl]-3-ethyl-6,7-difluoro-5-(trifluoromethyl)-1H-4,1-benzoxazepin-2-one
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Investigative | Compound Info | ||
Synonyms |
CHEMBL515170; BDBM50269979
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Activity |
IC50 = 68000 nM
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[2] | |||
Compound Name |
1-(3,5-Dimethyl-4-(2-((2-((1r,4r)-4-methylcyclohexyl)-4-oxo-1,3,8-triazaspiro[4.5]dec-1-en-8-yl)sulfonyl)ethyl)phenyl)-1-methylurea
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Investigative | Compound Info | ||
Synonyms |
CHEMBL4208963; CH5447240; SCHEMBL850127; TQR0476; BDBM50457781
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Activity |
IC50 = 93700 nM
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[1] |
Non Binders of This Target (in total, 3 non binders) | Download | Top | |||
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Compound Name |
Chembl4204089
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Investigative | Compound Info | ||
Synonyms |
BDBM50457784
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Activity |
EC50 > 1000000 nM
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[1] | |||
Compound Name |
Chembl4214849
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Investigative | Compound Info | ||
Synonyms |
SCHEMBL847240; BDBM50457783; 2-Cyclohexyl-8-(2-o-tolyl-ethanesulfonyl)-1,3,8-triaza-spiro[4.5]dec-1-en-4-one; 2-cyclohexyl-8-[2-(2-methylphenyl)ethylsulfonyl]-1,3,8-triazaspiro[4.5]dec-1-en-4-one
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Activity |
EC50 > 1000000 nM
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[1] | |||
Compound Name |
Chembl4206600
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Investigative | Compound Info | ||
Synonyms |
SCHEMBL850091; BDBM50457780; 8-(3-chlorophenyl)sulfonyl-2-(2,4-dichlorophenyl)-1,3,8-triazaspiro[4.5]dec-1-en-4-one
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Activity |
EC50 > 1000000 nM
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[1] |
References | Top | ||||
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REF 1 | Development of a Novel Human Parathyroid Hormone Receptor 1 (hPTHR1) Agonist (CH5447240), a Potent and Orally Available Small Molecule for Treatment of Hypoparathyroidism. J Med Chem. 2018 Jul 26;61(14):5949-5962. | ||||
REF 2 | 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. 2007 Apr 17;104(16):6846-51. |
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