Protein Information

General Information of the Protein

Protein ID	PT01648
Protein Name	Vasopressin V2 receptor
Secondarily Protein Name	AVPR V2 Antidiuretic hormone receptor Renal-type arginine vasopressin receptor
Gene Name	AVPR2
Secondarily Gene Name	ADHR DIR DIR3 V2R
Sequence	MLMASTTSAVPGHPSLPSLPSNSSQERPLDTRDPLLARAELALLSIVFVAVALSNGLVLAALARRGRRGHWAPIHVFIGHLCLADLAVALFQVLPQLAWKATDRFRGPDALCRAVKYLQMVGMYASSYMILAMTLDRHRAICRPMLAYRHGSGAHWNRPVLVAWAFSLLLSLPQLFIFAQRNVEGGSGVTDCWACFAEPWGRRTYVTWIALMVFVAPTLGIAACQVLIFREIHASLVPGPSERPGGRRRGRRTGSPGEGAHVSAAVAKTVRMTLVIVVVYVLCWAPFFLVQLWAAWDPEAPLEGAPFVLLMLLASLNSCTNPWIYASFSSSVSSELRSLLCCARGRTPPSLGPQDESCTTASSSLAKDTSS Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Membrane receptor > Family A G protein-coupled receptor > Peptide receptor (family A GPCR) > Short peptide receptor (family A GPCR) > Vasopressin and oxytocin receptor
Function	Receptor for arginine vasopressin. The activity of this receptor is mediated by G proteins which activate adenylate cyclase. Involved in renal water reabsorption. Show/Hide
Uniprot ID	Primary ID: P30518 Secondarily ID: C5HF20 O43192 Q3MJD3 Q9UCV9 Show/Hide
HGNC ID	HGNC:897
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: CL000094 , 1321N1

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0471688 Compound Info	CHEMBL4799793 Show/Hide	C22H23ClN4O	1
1	Ki = 560 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000011 , CHO

Cell Line Info

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000065 , HEK293-EBNA

Cell Line Info

Cell Line ID: CL000524 , HEK293-FT

Cell Line Info

Cell Line ID: CL000017 , HeLa

Cell Line Info

Cell Line ID: CL000779 , LV2

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0078819 Compound Info	(2S)-N-{2-Methyl-4-[(1-methyl-4,10-dihydropyrazolo[3,4-b]-[1,5]benzodiazepin-5(1H)-yl)carbonyl]benzyl}-2-[(4-methyl-1,4-diazepan-1-yl)carbonothioyl]pyrrolidine-1-carboxamide Show/Hide	C32H40N8O2S	1
1	EC50 = 850 nM
CP0040044 Compound Info	3-chloro-4-(10,11-dihydro-5H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-10-ylcarbonyl)-1-(5-fluoro-2-methylphenylcarboxamido)benzene Show/Hide	C27H21ClFN3O2	4
1	IC50 = 1 nM
2	IC50 = 1.2 nM
3	IC50 = 5 nM
4	Ki = 2.3 nM
CP0106503 Compound Info	3-chloro-4-[16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]-1-(2-phenylphenylcarboxamido)benzene Show/Hide	C34H30ClN3O2	1
1	IC50 = 4 nM
CP0196743 Compound Info	1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-(4-methylphenyl)benzamide Show/Hide	C35H32ClN3O2	1
1	IC50 = 5 nM
CP0206403 Compound Info	1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-trifluoromethylbenzamide Show/Hide	C29H25ClF3N3O2	1
1	IC50 = 7 nM
CP0042892 Compound Info	3'N-(2-hexahydro-1-pyridinylethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C37H41FN4O3	2
1	IC50 = 8 nM
2	IC50 = 39 nM
CP0154510 Compound Info	(4S)-N-[2-(dimethylamino)ethyl]-1-[4-[(2-phenylbenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxamide Show/Hide	C39H40N4O3	1
1	IC50 = 8 nM
CP0219489 Compound Info	1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-chlorobenzamide Show/Hide	C28H25Cl2N3O2	1
1	IC50 = 10 nM
CP0289902 Compound Info	methyl 2-[[1-[4-[(5-fluoro-2-methylbenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carbonyl]amino]acetate Show/Hide	C33H32FN3O5	1
1	IC50 = 10 nM
CP0124484 Compound Info	3'N-(2-dimethylaminoethyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C39H40N4O3	1
1	IC50 = 11 nM
CP0281438 Compound Info	3'N-(2-hydroxyethyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C37H35N3O4	1
1	IC50 = 11 nM
CP0062116 Compound Info	1N-{4-[6-chloro-16-ethyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-chlorobenzamide Show/Hide	C29H27Cl2N3O2	1
1	IC50 = 13 nM
CP0227811 Compound Info	3-chloro-4-[16-methyl-(12R)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]-1-(2-phenylphenylcarboxamido)benzene Show/Hide	C34H30ClN3O2	1
1	IC50 = 15 nM
CP0154509 Compound Info	3'N-(3-dimethylaminopropyl)-1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C40H42N4O3	1
1	IC50 = 16 nM
CP0154159 Compound Info	2-[1-[4-(2-phenylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3-ylcarboxamido]acetic acid Show/Hide	C37H33N3O5	1
1	IC50 = 18 nM
CP0056752 Compound Info	3'N-(2-dimethylaminoethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C34H37FN4O3	1
1	IC50 = 20 nM
CP0280289 Compound Info	3'N-(3-dimethylaminopropyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C35H39FN4O3	1
1	IC50 = 23 nM
CP0104567 Compound Info	1N-{4-[6-chloro-16-methyl-(12S)-2,10-diazatetracyclo[11.2.1.02,12.04,9]hexadeca-4(9),5,7-trien-10-ylcarbonyl]phenyl}-2-fluorobenzamide Show/Hide	C28H25ClFN3O2	1
1	IC50 = 26 nM
CP0365138 Compound Info	2-Methyl-N-[4-(2,3,4,5-tetrahydro-benzo[b][1,4]diazepine-1-carbonyl)-phenyl]-benzamide Show/Hide	C24H23N3O2	1
1	IC50 = 28 nM
CP0304035 Compound Info	3'N-(2-tetrahydro-1H-1-pyrrolylethyl)-1-[4-(5-fluoro-2-methylphenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C36H39FN4O3	1
1	IC50 = 39 nM
CP0041307 Compound Info	(4R)-N-[2-(dimethylamino)ethyl]-1-[4-[(2-fluorobenzoyl)amino]benzoyl]spiro[3,5-dihydro-2H-1-benzazepine-4,3'-cyclopentene]-1'-carboxamide Show/Hide	C33H35FN4O3	1
1	IC50 = 341 nM
CP0105811 Compound Info	3'N-(2-tetrahydro-1H-1-pyrrolylethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C35H37FN4O3	1
1	IC50 > 1000 nM
CP0194057 Compound Info	3'N-(2-dimethylaminoethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C33H35FN4O3	1
1	IC50 > 1000 nM
CP0197121 Compound Info	3'N-(2-hydroxyethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C31H30FN3O4	1
1	IC50 > 1000 nM
CP0304375 Compound Info	3'N-(2-hexahydro-1-pyridinylethyl)-1-[4-(2-fluorophenylcarboxamido)benzoyl]spiro[2,3,4,5-tetrahydro-1H-benzo[b]azepine-4,1'-(2'-cyclopentene)]-3'-carboxamide Show/Hide	C36H39FN4O3	1
1	IC50 > 1000 nM
CP0271007 Compound Info	2-Methyl-N-[4-(2,3,4,5-tetrahydro-benzo[b]azepine-1-carbonyl)-phenyl]-benzamide Show/Hide	C25H24N2O2	1
1	Ki = 7.2 nM
CP0260717 Compound Info	2-phenyl-N-[4-(2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)phenyl]benzamide Show/Hide	C30H26N2O2	1
1	Ki = 7.5 nM
CP0178094 Compound Info	N-[4-[5-(dimethylamino)-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]phenyl]-2-methylbenzamide Show/Hide	C27H29N3O2	1
1	Ki = 9.7 nM
CP0083253 Compound Info	(5H,11H-benzo[e]pyrrolo[1,2-a][1,4]diazepin-10-yl)-[2-chloro-4-(3-methyl-pyrazol-1-yl)-phenyl]-methanone Show/Hide	C23H19ClN4O	1
1	Ki = 39.9 nM
CP0195952 Compound Info	(2S,4R)-1-((R)-5-chloro-1-(2,4-dimethoxyphenylsulfonyl)-3-(2-methoxyphenyl)-2-oxoindolin-3-yl)-4-hydroxy-N,N-dimethylpyrrolidine-2-carboxamide Show/Hide	C30H32ClN3O8S	1
1	Ki = 325 nM
CP0117986 Compound Info	(2S)-1-[(4R,7S,10S,13S,16S,19R)-19-amino-7-(2-amino-2-oxoethyl)-10-(3-amino-3-oxopropyl)-13-[(2S)-butan-2-yl]-16-[(4-hydroxyphenyl)methyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]-N-[(2S)-1-[(2-amino-2-oxoethyl)amino]-4-methyl-1-oxopentan-2-yl]pyrrolidine-2-carboxamide Show/Hide	C43H66N12O12S2	2
1	Ki = 1544 nM
2	Ki = 3500 nM
CP0070065 Compound Info	4-ethoxy-N-(2-oxo-2-(2-(2-oxoindolin-3-ylidene)hydrazinyl)ethyl)-N-p-tolylbenzenesulfonamide Show/Hide	C25H24N4O5S	1
1	Ki = 2500 nM
CP0041007 Compound Info	1-(1-(4-(1-acetylpiperidin-4-yloxy)-2-methoxybenzoyl)piperidin-4-yl)-1H-benzo[d][1,3]oxazin-2(4H)-one Show/Hide	C28H33N3O6	1
1	Ki = 37000 nM
CP0219136 Compound Info	4-[(3,5-dihydroxyphenyl)methyl]-N-[[2-methyl-4-(1-methyl-4,10-dihydropyrazolo[4,3-c][1,5]benzodiazepine-5-carbonyl)phenyl]methyl]piperazine-1-carboxamide Show/Hide	C32H35N7O4	1
1	Ki >= 58.4 nM
CP0053149 Compound Info	N-[3-[4-[4-(2-oxo-3,4-dihydroquinolin-1-yl)piperidine-1-carbonyl]phenoxy]propyl]acetamide Show/Hide	C26H31N3O4	1
1	Ki > 81000 nM

Clinical Information about the Protein

Target 1 ( Vasopressin V2 receptor (V2R) )

Target Type	Successful Target
Disease	9 Target-related Diseases				9
1	Euvolemic hyponatremia [ICD-11: 5C72]
2	Diabetic complication [ICD-11: 5A2Y]
3	Hyponatraemia [ICD-11: 5C72]
4	Autism spectrum disorder [ICD-11: 6A02]
5	Diabetes insipidus [ICD-11: 5A61.5]
6	Anxiety disorder [ICD-11: 6B00-6B0Z]
7	Nocturia [ICD-11: MF55]
8	Urinary incontinence [ICD-11: MF50.2]
9	Dysmenorrhea [ICD-11: GA34.3]
Approved Drug(s)	6 Approved Drugs				6
1	Conivaptan	Drug Info	Approved	Euvolemic hyponatremia
2	Desmopressin	Drug Info	Approved	Diabetic complication
3	Mozavaptan	Drug Info	Approved	Hyponatraemia
4	Oxytocin	Drug Info	Approved	Autism spectrum disorder
5	Tolvaptan	Drug Info	Approved	Hyponatraemia
6	Vasopressin	Drug Info	Approved	Diabetes insipidus
Clinical Trial Drug(s)	3 Clinical Trial Drugs				3
1	Lixivaptan	Drug Info	Phase 3	Hyponatraemia
2	SSR149415	Drug Info	Phase 2	Anxiety disorder
3	VA-106483	Drug Info	Phase 2	Nocturia
Discontinued Drug(s)	3 Discontinued Drugs				3
1	OPC-51803	Drug Info	Discontinued in Phase 1	Urinary incontinence
2	VNA-932	Drug Info	Discontinued in Phase 1	Urinary incontinence
3	JTV-605	Drug Info	Terminated	Dysmenorrhea

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han