General Information of the Protein
Protein ID
PT02986
Protein Name
Parathyroid hormone/parathyroid hormone-related peptide receptor
Secondarily
Protein Name
PTH/PTHrP type I receptor
Parathyroid hormone 1 receptor
Gene Name
PTH1R
Secondarily
Gene Name
PTHR
PTHR1
Sequence
MGTARIAPGLALLLCCPVLSSAYALVDADDVMTKEEQIFLLHRAQAQCEKRLKEVLQRPASIMESDKGWTSASTSGKPRKDKASGKLYPESEEDKEAPTGSRYRGRPCLPEWDHILCWPLGAPGEVVAVPCPDYIYDFNHKGHAYRRCDRNGSWELVPGHNRTWANYSECVKFLTNETREREVFDRLGMIYTVGYSVSLASLTVAVLILAYFRRLHCTRNYIHMHLFLSFMLRAVSIFVKDAVLYSGATLDEAERLTEEELRAIAQAPPPPATAAAGYAGCRVAVTFFLYFLATNYYWILVEGLYLHSLIFMAFFSEKKYLWGFTVFGWGLPAVFVAVWVSVRATLANTGCWDLSSGNKKWIIQVPILASIVLNFILFINIVRVLATKLRETNAGRCDTRQQYRKLLKSTLVLMPLFGVHYIVFMATPYTEVSGTLWQVQMHYEMLFNSFQGFFVAIIYCFCNGEVQAEIKKSWSRWTLALDFKRKARSGSSSYSYGPMVSHTSVTNVGPRVGLGLPLSPRLLPTATTNGHPQLPGHAKPGTPALETLETTPPAMAAPKDDGFLNGSCSGLDEEASGPERPPALLQEEWETVM
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Organism
Homo sapiens, Human
Protein Classification
Membrane receptor
>
Family B G protein-coupled receptor
>
Peptide receptor (family B GPCR)
>
Parathyroid hormone receptor
>
Parathyroid hormone receptor
Function
Receptor for parathyroid hormone and for parathyroid hormone-related peptide. The activity of this receptor is mediated by G proteins which activate adenylyl cyclase and also a phosphatidylinositol-calcium second messenger system.
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Uniprot ID
Primary ID:
Q03431

Secondarily ID:
Q2M1U3
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Ensembl ID
ENSG00000160801
HGNC ID
HGNC:9608
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000026 , CHO-K1
 Cell Line Info 
Compound ID Compound Name Compound Formula
CP0580116
 Compound Info 
4-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]azetidin-3-yl]methylamino]cyclohexane-1-carboxylic acid
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C32H34Cl2N4O3
  1
1
IC50 = 40 nM
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CP0571322
 Compound Info 
4-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]azetidin-3-yl]methylamino]cyclohexane-1-carboxylic acid
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C32H34Cl2N4O3
  1
1
IC50 = 50 nM
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CP0571323
 Compound Info 
4-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-fluoroazetidin-3-yl]methylamino]cyclohexane-1-carboxylic acid
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C32H33Cl2FN4O3
  1
1
IC50 = 80 nM
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CP0417251
 Compound Info 
5-cyclohexyl-3,3-dimethyl-1-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]-2-oxo-1,4-benzodiazepine-8-carbonitrile
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C31H39N5O2
  1
1
IC50 = 90 nM
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CP0535315
 Compound Info 
2-chloro-5,5-dimethyl-7-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]-6-oxopyrido[2,3-d][1]benzazepine-9-carbonitrile
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C29H30ClN5O2
  1
1
IC50 = 90 nM
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CP0577545
 Compound Info 
4-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-fluoroazetidin-3-yl]methylamino]-1-methylcyclohexane-1-carboxylic acid
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C33H35Cl2FN4O3
  1
1
IC50 = 90 nM
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CP0579196
 Compound Info 
4-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-fluoroazetidin-3-yl]methylamino]bicyclo[2.2.2]octane-1-carboxylic acid
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C34H35Cl2FN4O3
  1
1
IC50 = 90 nM
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CP0564438
 Compound Info 
2,9-dichloro-7-[4-[3-methoxy-3-[(oxan-4-ylamino)methyl]azetidin-1-yl]phenyl]-5,5-dimethylpyrido[2,3-d][1]benzazepin-6-one
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C31H34Cl2N4O3
  1
1
IC50 = 100 nM
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CP0579195
 Compound Info 
methyl 1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-[(oxan-4-ylamino)methyl]azetidine-3-carboxylate
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C32H34Cl2N4O4
  1
1
IC50 = 110 nM
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CP0578513
 Compound Info 
4-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-methoxyazetidin-3-yl]methylamino]cyclohexane-1-carboxylic acid
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C33H36Cl2N4O4
  1
1
IC50 = 150 nM
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CP0329804
 Compound Info 
2,9-dichloro-5,5-dimethyl-7-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]pyrido[2,3-d][1]benzazepin-6-one
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C28H30Cl2N4O2
  1
1
IC50 = 170 nM
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CP0571062
 Compound Info 
4-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-fluoroazetidin-3-yl]methylamino]-1-methylcyclohexane-1-carboxylic acid
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C33H35Cl2FN4O3
  1
1
IC50 = 170 nM
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CP0414019
 Compound Info 
5-cyclohexyl-3,3-dimethyl-1-[4-[2-[(1-methylsulfonylpiperidin-4-yl)amino]ethylamino]phenyl]-2-oxo-1,4-benzodiazepine-8-carbonitrile
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C32H42N6O3S
  1
1
IC50 = 180 nM
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CP0578267
 Compound Info 
4-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-methoxyazetidin-3-yl]methylamino]cyclohexane-1-carboxylic acid
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C33H36Cl2N4O4
  1
1
IC50 = 180 nM
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CP0562182
 Compound Info 
2-chloro-9-fluoro-5,5-dimethyl-7-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]pyrido[2,3-d][1]benzazepin-6-one
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C28H30ClFN4O2
  1
1
IC50 = 250 nM
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CP0535314
 Compound Info 
2-chloro-9-methoxy-5,5-dimethyl-7-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]pyrido[2,3-d][1]benzazepin-6-one
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C29H33ClN4O3
  1
1
IC50 = 270 nM
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CP0569986
 Compound Info 
2,9-dichloro-5,5-dimethyl-7-[4-[3-[(oxan-4-ylamino)methyl]azetidin-1-yl]phenyl]pyrido[2,3-d][1]benzazepin-6-one
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C30H32Cl2N4O2
  1
1
IC50 = 280 nM
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CP0403578
 Compound Info 
2-chloro-5,5,9-trimethyl-7-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]pyrido[2,3-d][1]benzazepin-6-one
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C29H33ClN4O2
  1
1
IC50 = 380 nM
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CP0554299
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-5-cyclohexyl-3,3-dimethyl-2-oxo-1,4-benzodiazepine-8-carbonitrile
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C26H31N5O
  1
1
IC50 = 730 nM
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CP0550382
 Compound Info 
2,9-dichloro-7-[4-[3-methoxy-3-[[methyl(oxan-4-yl)amino]methyl]azetidin-1-yl]phenyl]-5,5-dimethylpyrido[2,3-d][1]benzazepin-6-one
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C32H36Cl2N4O3
  1
1
IC50 = 780 nM
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CP0414354
 Compound Info 
9-chloro-2-fluoro-5,5-dimethyl-7-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]pyrido[2,3-d][1]benzazepin-6-one
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C28H30ClFN4O2
  1
1
IC50 = 800 nM
 Bioactivity Info 
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CP0578512
 Compound Info 
2,9-dichloro-7-[4-[3-hydroxy-3-[(oxan-4-ylamino)methyl]azetidin-1-yl]phenyl]-5,5-dimethylpyrido[2,3-d][1]benzazepin-6-one
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C30H32Cl2N4O3
  1
1
IC50 = 840 nM
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CP0579984
 Compound Info 
3-[[1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-fluoroazetidin-3-yl]methylamino]cyclobutane-1-carboxylic acid
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C30H29Cl2FN4O3
  1
1
IC50 = 840 nM
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CP0414352
 Compound Info 
8-chloro-5-cyclohexyl-3,3-dimethyl-1-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]-1-benzazepin-2-one
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C31H40ClN3O2
  1
1
IC50 = 970 nM
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CP0437417
 Compound Info 
9-chloro-2,5,5-trimethyl-7-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]pyrido[2,3-d][1]benzazepin-6-one
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C29H33ClN4O2
  1
1
IC50 = 1600 nM
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CP0576004
 Compound Info 
3,10-dichloro-7,7-dimethyl-5-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]benzo[d][1]benzazepin-6-one
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C29H31Cl2N3O2
  1
1
IC50 = 1800 nM
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CP0563740
 Compound Info 
5-cyclohexyl-1-[4-[2-(cyclohexylamino)ethylamino]phenyl]-3,3-dimethyl-2-oxo-1,4-benzodiazepine-8-carbonitrile
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C32H41N5O
  1
1
IC50 = 2300 nM
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CP0414353
 Compound Info 
3-chloro-7,7-dimethyl-5-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]benzo[d][1]benzazepin-6-one
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C29H32ClN3O2
  1
1
IC50 = 3200 nM
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CP0549505
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-5-cyclohexyl-3,3-dimethyl-1,4-benzodiazepin-2-one
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C25H31ClN4O
  1
1
IC50 = 3500 nM
 Bioactivity Info 
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CP0549503
 Compound Info 
1-[4-(2-aminoethoxy)phenyl]-5-cyclohexyl-3,3-dimethyl-2-oxo-1,4-benzodiazepine-8-carbonitrile
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C26H30N4O2
  1
1
IC50 = 4000 nM
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CP0549504
 Compound Info 
1-[4-(3-aminopropylamino)phenyl]-5-cyclohexyl-3,3-dimethyl-2-oxo-1,4-benzodiazepine-8-carbonitrile
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C27H33N5O
  1
1
IC50 = 4100 nM
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CP0472276
 Compound Info 
8-chloro-5-cyclohexyl-1-[5-[2-(oxan-4-ylamino)ethylamino]pyridin-2-yl]-3-propan-2-yl-1,3,4-benzotriazepin-2-one
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C29H39ClN6O2
  1
1
IC50 = 4370 nM
 Bioactivity Info 
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CP0554300
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-5-cyclohexyl-3,3,8-trimethyl-1,4-benzodiazepin-2-one
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C26H34N4O
  1
1
IC50 = 6100 nM
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CP0576163
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-5-cyclohexyl-3-methyl-3-propan-2-yl-1,4-benzodiazepin-2-one
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C27H35ClN4O
  1
1
IC50 = 6800 nM
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CP0414020
 Compound Info 
1-[4-(3-aminopropyl)phenyl]-5-cyclohexyl-3,3-dimethyl-2-oxo-1,4-benzodiazepine-8-carbonitrile
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C27H32N4O
  1
1
IC50 = 7600 nM
 Bioactivity Info 
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CP0472277
 Compound Info 
5-cyclohexyl-3,3-dimethyl-1-[4-[2-(oxan-4-ylamino)ethylamino]phenyl]-2-oxo-1-benzazepine-8-carbonitrile
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C32H40N4O2
  1
1
IC50 = 8800 nM
 Bioactivity Info 
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CP0417240
 Compound Info 
8-chloro-5-cyclohexyl-1-[4-(4,5-dihydro-1H-imidazol-2-ylmethyl)phenyl]-3-propan-2-yl-1,3,4-benzotriazepin-2-one
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C27H32ClN5O
  1
1
IC50 = 9400 nM
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CP0539595
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-5-cyclohexyl-8-methoxy-3,3-dimethyl-1,4-benzodiazepin-2-one
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C26H34N4O2
  1
1
IC50 = 14000 nM
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CP0549506
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-5-cyclohexyl-3-propan-2-yl-3H-1,4-benzodiazepin-2-one
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C26H33ClN4O
  1
1
IC50 = 14000 nM
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CP0553024
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-3,3-dimethyl-5-(1-methylcyclohexyl)-1,4-benzodiazepin-2-one
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C26H33ClN4O
  1
1
IC50 = 16000 nM
 Bioactivity Info 
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CP0536632
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-3,3-dimethyl-5-(2-methylpropyl)-1,4-benzodiazepin-2-one
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C23H29ClN4O
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1
IC50 = 23000 nM
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CP0564384
 Compound Info 
1-[4-(2,9-dichloro-5,5-dimethyl-6-oxopyrido[2,3-d][1]benzazepin-7-yl)phenyl]-3-[(oxan-4-ylamino)methyl]azetidine-3-carboxylic acid
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C31H32Cl2N4O4
  1
1
IC50 = 23000 nM
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CP0554301
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-5-cyclohexyl-3H-1,4-benzodiazepin-2-one
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C23H27ClN4O
  1
1
IC50 = 38000 nM
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CP0530307
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-5-cyclohexyl-3-(dimethylamino)-3H-1,4-benzodiazepin-2-one
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C25H32ClN5O
  1
1
IC50 = 44000 nM
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CP0559470
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-3,3-dimethyl-5-phenyl-1,4-benzodiazepin-2-one
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C25H25ClN4O
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1
IC50 = 45000 nM
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CP0571794
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-4-cyclohexyl-3H-1,4-benzodiazepine-2,5-dione
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C23H27ClN4O2
  1
1
IC50 > 100000 nM
 Bioactivity Info 
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CP0571795
 Compound Info 
1-[4-(2-aminoethylamino)phenyl]-8-chloro-4-cyclohexyl-3,5-dihydro-1,4-benzodiazepin-2-one
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C23H29ClN4O
  1
1
IC50 > 100000 nM
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CP0400098
 Compound Info 
5-cyclohexyl-1-[4-[2-(1H-imidazol-2-yl)ethylamino]phenyl]-3,8-dimethyl-1,3,4-benzotriazepin-2-one
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C27H32N6O
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1
Kd = 2884.03 nM
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Cell Line ID: CL000006 , HEK293
 Cell Line Info 
Cell Line ID: CL000787 , HKRK-B28
 Cell Line Info 
Cell Line ID: CL000009 , LLC-PK1
 Cell Line Info 
Cell Line ID: CL000099 , SaOS-2
 Cell Line Info 
Clinical Information about the Protein
Target 1 ( Parathyroid hormone 1 receptor (PTH1R) )
Target Type Successful Target
Disease 1 Target-related Disease  1
1 Hypoparathyroidism [ICD-11: 5A50]
Clinical Trial Drug(s) 1 Clinical Trial Drug  1
1 PCO371
 Drug Info 
Phase 1
Hypoparathyroidism
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06582 Parathyroid hormone/parathyroid hormone-related peptide receptor Rattus norvegicus, Rat
 Protein Info 
PT07326 Parathyroid hormone/parathyroid hormone-related peptide receptor Mus musculus, Mouse
 Protein Info