Protein Information

General Information of the Protein

Protein ID	PT00853
Protein Name	Renin
Secondarily Protein Name	Angiotensinogenase
Gene Name	REN
Sequence	MDGWRRMPRWGLLLLLWGSCTFGLPTDTTTFKRIFLKRMPSIRESLKERGVDMARLGPEWSQPMKRLTLGNTTSSVILTNYMDTQYYGEIGIGTPPQTFKVVFDTGSSNVWVPSSKCSRLYTACVYHKLFDASDSSSYKHNGTELTLRYSTGTVSGFLSQDIITVGGITVTQMFGEVTEMPALPFMLAEFDGVVGMGFIEQAIGRVTPIFDNIISQGVLKEDVFSFYYNRDSENSQSLGGQIVLGGSDPQHYEGNFHYINLIKTGVWQIQMKGVSVGSSTLLCEDGCLALVDTGASYISGSTSSIEKLMEALGAKKRLFDYVVKCNEGPTLPDISFHLGGKEYTLTSADYVFQESYSSKKLCTLAIHAMDIPPPTGPTWALGATFIRKFYTEFDRRNNRIGFALAR Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Enzyme > Protease > Aspartic protease > Aspartic protease AA clan > Aspartic protease A1A subfamily
Function	Renin is a highly specific endopeptidase, whose only known function is to generate angiotensin I from angiotensinogen in the plasma, initiating a cascade of reactions that produce an elevation of blood pressure and increased sodium retention by the kidney. Show/Hide
Uniprot ID	Primary ID: P00797 Secondarily ID: Q6FI38 Q6T5C2 Show/Hide
Ensembl ID	ENSG00000143839
HGNC ID	HGNC:9958
Subcellular Location	Secreted 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: CL000011 , CHO

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0036770 Compound Info	(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2,2-dimethylethyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-8-methyl-2-(propan-2-yl)nonanamide Show/Hide	C30H53N3O6	1
1	IC50 = 0.7 nM Bioactivity Info	TI LI LO TS
CP0717245 Compound Info	N-((3S,4S)-4-Benzylpyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropoxy)benzamide Hydrochloride Salt Show/Hide	C27H39ClN2O4	1
1	IC50 = 170 nM Bioactivity Info	TI LI LO TS
CP0917566 Compound Info	rac-N-((3S,4S)-4-Benzylpyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropoxy)benzamide Hydrochloride Salt Show/Hide	C27H39ClN2O4	1
1	IC50 = 450 nM Bioactivity Info	TI LI LO TS
CP0913946 Compound Info	rac-N-((3S,4S)-4-Benzylpyrrolidin-3-ylmethyl)-N-(4-chlorophenyl)-4-methoxy-3-(3-methoxypropoxy)benzamide Hydrochloride Salt Show/Hide	C30H36Cl2N2O4	1
1	IC50 = 1700 nM Bioactivity Info	TI LI LO TS
CP0864193 Compound Info	rac-N-((3S,4S)-4-Benzylpyrrolidin-3-ylmethyl)-N-phenyl-4-methoxy-3-(3-methoxypropoxy)-benzamide Hydrochloride Salt Show/Hide	C30H37ClN2O4	1
1	IC50 = 1900 nM Bioactivity Info	TI LI LO TS
CP0913945 Compound Info	N-((3R,4R)-4-Benzylpyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropoxy)benzamide Hydrochloride Salt Show/Hide	C27H39ClN2O4	1
1	IC50 = 2700 nM Bioactivity Info	TI LI LO TS
CP0875096 Compound Info	rac-Benzyl-((3S,4S)-4-benzylpyrrolidin-3-ylmethyl)-(4-chlorophenyl)-amine Hydrochloride Salt Show/Hide	C25H28Cl2N2	1
1	IC50 = 4100 nM Bioactivity Info	TI LI LO TS
CP0913944 Compound Info	((3S,4S)-4-Benzylpyrrolidin-3-ylmethyl)-(4-chlorophenyl)-phenylamine Hydrochloride Salt Show/Hide	C24H26Cl2N2	1
1	IC50 = 7600 nM Bioactivity Info	TI LI LO TS
CP0903864 Compound Info	rac-((3S,4S)-4-Benzylpyrrolidin-3-ylmethyl)-isopropyl-[4-methoxy-3-(3-methoxypropoxy)benzyl]-amine Hydrochloride Salt Show/Hide	C27H41ClN2O3	1
1	IC50 = 7700 nM Bioactivity Info	TI LI LO TS
CP0913947 Compound Info	rac-N-((3S,4S)-4-Benzylpyrrolidin-3-yl-methyl)-(4-chlorophenyl)-[4-methoxy-3-(3-methoxypropoxy)-benzyl]-amine Hydrochloride Salt Show/Hide	C30H38Cl2N2O3	1
1	IC50 = 9800 nM Bioactivity Info	TI LI LO TS
CP0913948 Compound Info	rac-(4-Benzylpyrrolidin-3-ylmethyl)-(4-chlorophenyl)-phenylamine Hydrochloride Salt Show/Hide	C24H26Cl2N2	1
1	IC50 = 14000 nM Bioactivity Info	TI LI LO TS
CP0875097 Compound Info	((3R,4R)-4-Benzylpyrrolidin-3-ylmethyl)-(4-chlorophenyl)-phenylamine Hydrochloride Salt Show/Hide	C24H26Cl2N2	1
1	IC50 = 18000 nM Bioactivity Info	TI LI LO TS
CP0011744 Compound Info	N-[(2S,3S)-3-amino-2-hydroxy-3-phenylpropyl]-3,4-dichloro-N-(2-methylpropyl)benzenesulfonamide Show/Hide	C19H24Cl2N2O3S	1
1	IC50 > 100000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000131 , HEK293-F

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0074456 Compound Info	2-tert-butyl-4-(3-methoxypropylamino)-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl]pyrimidine-5-carboxamide Show/Hide	C27H46N6O4	3
1	IC50 = 0.38 nM
2	IC50 = 0.79 nM
3	IC50 = 1.5 nM
CP0036770 Compound Info	(2S,4S,5S,7S)-5-amino-N-(2-carbamoyl-2,2-dimethylethyl)-4-hydroxy-7-{[4-methoxy-3-(3-methoxypropoxy)phenyl]methyl}-8-methyl-2-(propan-2-yl)nonanamide Show/Hide	C30H53N3O6	10
1	IC50 = 0.4 nM
2	IC50 = 0.5 nM
3	IC50 = 0.53 nM
4	IC50 = 0.6 nM
5	IC50 = 0.65 nM
6	IC50 = 0.7 nM
7	IC50 = 0.84 nM
8	IC50 = 2.21 nM
9	IC50 = 2.3 nM
10	IC50 = 3 nM
CP0579965 Compound Info	US10155731, Example 270 Show/Hide	C22H32N6O4	1
1	IC50 = 0.4 nM
CP0579590 Compound Info	methyl N-[3-[3-[[cyclopropyl-[(2R)-morpholine-2-carbonyl]amino]methyl]indol-1-yl]propyl]carbamate Show/Hide	C22H30N4O4	1
1	IC50 = 0.9 nM
CP0689386 Compound Info	methyl 4-((R)-1-((1S,3R,4S)-3-amino-4-hydroxycyclopentanecarbonyl)piperidin-3-yl)-4-(6-chloro-3'-ethylbiphenyl-2-yl)-4-hydroxybutylcarbamate Show/Hide	C31H42ClN3O5	1
1	IC50 = 1.8 nM
CP0228492 Compound Info	methyl N-[4-[(3R)-1-[(1R,3S)-3-aminocyclopentanecarbonyl]piperidin-3-yl]-4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxybutyl]carbamate Show/Hide	C31H42FN3O4	1
1	IC50 = 3.3 nM
CP0580056 Compound Info	US10155731, Example 268 Show/Hide	C21H30N6O4	1
1	IC50 = 3.6 nM
CP0577007 Compound Info	US10155731, Example 271 Show/Hide	C22H32N6O4	1
1	IC50 = 3.7 nM
CP0228493 Compound Info	methyl N-[4-[3-chloro-2-(3-ethylphenyl)phenyl]-4-hydroxy-4-[(3R)-1-[(1R,3S)-3-(methylamino)cyclopentanecarbonyl]piperidin-3-yl]butyl]carbamate Show/Hide	C32H44ClN3O4	1
1	IC50 = 4.3 nM
CP0117902 Compound Info	methyl N-[4-[(3R)-1-[(1R,3S)-3-aminocyclopentanecarbonyl]piperidin-3-yl]-4-[3-chloro-2-(3-ethylphenyl)phenyl]-4-hydroxybutyl]carbamate Show/Hide	C31H42ClN3O4	1
1	IC50 = 8.4 nM
CP0569514 Compound Info	US8975252, 39 Show/Hide	C21H29N3O3	1
1	IC50 = 13 nM
CP0865214 Compound Info	methyl 4-((R)-1-(4-aminobutanoyl)piperidin-3-yl)-4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxybutylcarbamate Show/Hide	C29H40FN3O4	1
1	IC50 = 13 nM
CP0689241 Compound Info	methyl 4-(6-chloro-3'-ethylbiphenyl-2-yl)-4-hydroxy-4-((R)-1-(4-(methylamino)butanoyl)piperidin-3-yl)butylcarbamate Show/Hide	C30H42ClN3O4	1
1	IC50 = 16 nM
CP0673266 Compound Info	methyl 4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxy-4-((R)-1-(4-(methylamino)butanoyl)piperidin-3-yl)butylcarbamate Show/Hide	C30H42FN3O4	1
1	IC50 = 20 nM
CP0369555 Compound Info	methyl N-[4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxy-4-[(3R)-1-(2-piperidin-4-ylacetyl)piperidin-3-yl]butyl]carbamate Show/Hide	C32H44FN3O4	1
1	IC50 = 23 nM
CP0254722 Compound Info	2-tert-butyl-4-hexyl-N-(2-methylpropyl)-N-[(3S,5R)-5-(morpholine-4-carbonyl)piperidin-3-yl]pyrimidine-5-carboxamide Show/Hide	C29H49N5O3	3
1	IC50 = 24 nM
2	IC50 = 29 nM
3	IC50 > 10 nM
CP0766749 Compound Info	methyl 4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxy-4-((3R)-1-(2-(morpholin-2-yl)acetyl)piperidin-3-yl)butylcarbamate Show/Hide	C31H42FN3O5	1
1	IC50 = 24 nM
CP0684961 Compound Info	methyl 4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxy-4-((3R)-1-(3-hydroxy-4-(methylamino)butanoyl)piperidin-3-yl)butylcarbamate Show/Hide	C30H42FN3O5	1
1	IC50 = 29 nM
CP0757362 Compound Info	methyl 4-((3R)-1-(4-amino-3-hydroxybutanoyl)piperidin-3-yl)-4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxybutylcarbamate Show/Hide	C29H40FN3O5	1
1	IC50 = 36 nM
CP0471782 Compound Info	methyl N-[4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxy-4-[(3R)-1-(2-piperidin-3-ylacetyl)piperidin-3-yl]butyl]carbamate Show/Hide	C32H44FN3O4	1
1	IC50 = 40 nM
CP0110370 Compound Info	methyl N-[4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxy-4-[(3R)-1-[3-methoxy-4-(methylamino)butanoyl]piperidin-3-yl]butyl]carbamate Show/Hide	C31H44FN3O5	1
1	IC50 = 50 nM
CP0965060 Compound Info	methyl 4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxy-4-((R)-1-(4-(2-hydroxyethylamino)butanoyl)piperidin-3-yl)butylcarbamate Show/Hide	C31H44FN3O5	1
1	IC50 = 63 nM
CP0762386 Compound Info	methyl 4-((R)-1-(6-aminohexanoyl)piperidin-3-yl)-4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxybutylcarbamate Show/Hide	C31H44FN3O4	1
1	IC50 = 100 nM
CP0766748 Compound Info	methyl 4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxy-4-((R)-1-(piperidine-4-carbonyl)piperidin-3-yl)butylcarbamate Show/Hide	C31H42FN3O4	1
1	IC50 = 102 nM
CP0255937 Compound Info	methyl N-[4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxy-4-[(3R)-1-[2-(methylamino)ethylcarbamoyl]piperidin-3-yl]butyl]carbamate Show/Hide	C29H41FN4O4	1
1	IC50 = 120 nM
CP0369554 Compound Info	methyl N-[4-[(3R)-1-(5-aminopentanoyl)piperidin-3-yl]-4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxybutyl]carbamate Show/Hide	C30H42FN3O4	1
1	IC50 = 120 nM
CP0705220 Compound Info	methyl 4-((R)-1-(2-aminoethylcarbamoyl)piperidin-3-yl)-4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxybutylcarbamate Show/Hide	C28H39FN4O4	1
1	IC50 = 150 nM
CP0412181 Compound Info	methyl N-[4-[(3R)-1-[(4R)-4-amino-5-hydroxypentanoyl]piperidin-3-yl]-4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxybutyl]carbamate Show/Hide	C30H42FN3O5	1
1	IC50 = 180 nM
CP0717245 Compound Info	N-((3S,4S)-4-Benzylpyrrolidin-3-ylmethyl)-N-isopropyl-4-methoxy-3-(3-methoxypropoxy)benzamide Hydrochloride Salt Show/Hide	C27H39ClN2O4	1
1	IC50 = 300 nM
CP0541269 Compound Info	benzyl (2S)-2-amino-5-[(3R)-3-[1-[2-(3-ethylphenyl)-3-fluorophenyl]-1-hydroxy-4-(methoxycarbonylamino)butyl]piperidin-1-yl]-5-oxopentanoate Show/Hide	C37H46FN3O6	1
1	IC50 = 450 nM
CP0902964 Compound Info	methyl 4-((R)-1-((S)-4-amino-5-hydroxypentanoyl)piperidin-3-yl)-4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxybutylcarbamate Show/Hide	C30H42FN3O5	1
1	IC50 = 460 nM
CP0568689 Compound Info	methyl N-[4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxy-4-[(3R)-1-(pyrrolidine-3-carbonyl)piperidin-3-yl]butyl]carbamate Show/Hide	C30H40FN3O4	1
1	IC50 = 540 nM
CP0725657 Compound Info	(2S)-methyl 2-amino-5-((3R)-3-(1-(3'-ethyl-6-fluorobiphenyl-2-yl)-1-hydroxy-4-(methoxycarbonylamino)butyl)piperidin-1-yl)-5-oxopentanoate Show/Hide	C31H42FN3O6	1
1	IC50 = 540 nM
CP0117900 Compound Info	methyl N-[4-[(3R)-1-[(2S)-4-amino-2-hydroxybutanoyl]piperidin-3-yl]-4-[2-(3-ethylphenyl)-3-fluorophenyl]-4-hydroxybutyl]carbamate Show/Hide	C29H40FN3O5	1
1	IC50 = 840 nM
CP0905323 Compound Info	methyl 4-((R)-1-(2-aminoacetyl)piperidin-3-yl)-4-(3'-ethyl-6-fluorobiphenyl-2-yl)-4-hydroxybutylcarbamate Show/Hide	C27H36FN3O4	1
1	IC50 = 3800 nM
CP0069235 Compound Info	5-(4-{[(3,5-difluorophenyl)methyl]amino}phenyl)-6-ethylpyrimidine-2,4-diamine Show/Hide	C19H19F2N5	2
1	IC50 = 4000 nM
2	IC50 = 6600 nM

Clinical Information about the Protein

Target 1 ( Angiotensinogenase renin (REN) )

Target Type	Successful Target
Disease	5 Target-related Diseases				5
1	Hypertension [ICD-11: BA00-BA04]
2	Ulcerative colitis [ICD-11: DD71]
3	Type-2 diabetes [ICD-11: 5A11]
4	Cardiovascular disease [ICD-11: BA00-BE2Z]
5	Glaucoma/ocular hypertension [ICD-11: 9C61]
Approved Drug(s)	2 Approved Drugs				2
1	Aliskiren	Drug Info	Approved	Hypertension
2	Remikiren	Drug Info	Approved	Hypertension
Clinical Trial Drug(s)	5 Clinical Trial Drugs				5
1	CP-80794	Drug Info	Phase 2	Hypertension
2	SPH3127	Drug Info	Phase 2	Ulcerative colitis
3	TAK-272	Drug Info	Phase 2	Type-2 diabetes
4	ACT-178882	Drug Info	Phase 1	Cardiovascular disease
5	VTP-27999	Drug Info	Phase 1	Hypertension
Discontinued Drug(s)	2 Discontinued Drugs				2
1	Enalkiren	Drug Info	Discontinued in Phase 2	Glaucoma/ocular hypertension
2	ZANKIREN	Drug Info	Discontinued in Phase 2	Hypertension

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han