Protein Information

General Information of the Protein

Protein ID	PT01154
Protein Name	Mineralocorticoid receptor
Secondarily Protein Name	Nuclear receptor subfamily 3 group C member 2
Gene Name	NR3C2
Secondarily Gene Name	MCR MLR
Sequence	METKGYHSLPEGLDMERRWGQVSQAVERSSLGPTERTDENNYMEIVNVSCVSGAIPNNSTQGSSKEKQELLPCLQQDNNRPGILTSDIKTELESKELSATVAESMGLYMDSVRDADYSYEQQNQQGSMSPAKIYQNVEQLVKFYKGNGHRPSTLSCVNTPLRSFMSDSGSSVNGGVMRAVVKSPIMCHEKSPSVCSPLNMTSSVCSPAGINSVSSTTASFGSFPVHSPITQGTPLTCSPNVENRGSRSHSPAHASNVGSPLSSPLSSMKSSISSPPSHCSVKSPVSSPNNVTLRSSVSSPANINNSRCSVSSPSNTNNRSTLSSPAASTVGSICSPVNNAFSYTASGTSAGSSTLRDVVPSPDTQEKGAQEVPFPKTEEVESAISNGVTGQLNIVQYIKPEPDGAFSSSCLGGNSKINSDSSFSVPIKQESTKHSCSGTSFKGNPTVNPFPFMDGSYFSFMDDKDYYSLSGILGPPVPGFDGNCEGSGFPVGIKQEPDDGSYYPEASIPSSAIVGVNSGGQSFHYRIGAQGTISLSRSARDQSFQHLSSFPPVNTLVESWKSHGDLSSRRSDGYPVLEYIPENVSSSTLRSVSTGSSRPSKICLVCGDEASGCHYGVVTCGSCKVFFKRAVEGQHNYLCAGRNDCIIDKIRRKNCPACRLQKCLQAGMNLGARKSKKLGKLKGIHEEQPQQQQPPPPPPPPQSPEEGTTYIAPAKEPSVNTALVPQLSTISRALTPSPVMVLENIEPEIVYAGYDSSKPDTAENLLSTLNRLAGKQMIQVVKWAKVLPGFKNLPLEDQITLIQYSWMCLSSFALSWRSYKHTNSQFLYFAPDLVFNEEKMHQSAMYELCQGMHQISLQFVRLQLTFEEYTIMKVLLLLSTIPKDGLKSQAAFEEMRTNYIKELRKMVTKCPNNSGQSWQRFYQLTKLLDSMHDLVSDLLEFCFYTFRESHALKVEFPAMLVEIISDQLPKVESGNAKPLYFHRK Show/Hide
Organism	Homo sapiens, Human
Protein Classification	Transcription factor > Nuclear receptor > Nuclear hormone receptor subfamily 3 > Nuclear hormone receptor subfamily 3 group C > Nuclear hormone receptor subfamily 3 group C member 2
Function	Receptor for both mineralocorticoids (MC) such as aldosterone and glucocorticoids (GC) such as corticosterone or cortisol. Binds to mineralocorticoid response elements (MRE) and transactivates target genes. The effect of MC is to increase ion and water transport and thus raise extracellular fluid volume and blood pressure and lower potassium levels. Show/Hide
Uniprot ID	Primary ID: P08235 Secondarily ID: B0ZBF5 B0ZBF7 Q2NKL1 Q96KQ8 Q96KQ9 Show/Hide
Ensembl ID	ENSG00000151623
HGNC ID	HGNC:7979
Subcellular Location	Cytoplasm Nucleus Endoplasmic reticulum 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: CL000068 , A-549

Cell Line Info

Compound ID	Compound Name	Compound Formula
CP0073120 Compound Info	(3S)-3-(3-bromo-4-hydroxyphenyl)-2,2-dimethyl-3-phenyl-N-(1,3-thiazol-2-yl)propanamide Show/Hide	C20H19BrN2O2S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0074372 Compound Info	2-[(9S)-3-hydroxy-9H-xanthen-9-yl]-2-methyl-N-(1,3,4-thiadiazol-2-yl)propanamide Show/Hide	C19H17N3O3S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0087252 Compound Info	2-[(9S)-3-hydroxy-9H-xanthen-9-yl]-2-methyl-N-(1,3-thiazol-2-yl)propanamide Show/Hide	C20H18N2O3S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0087253 Compound Info	(3S)-3-(4-hydroxyphenyl)-2,2-dimethyl-3-phenyl-N-(1,3-thiazol-2-yl)propanamide Show/Hide	C20H20N2O2S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0256572 Compound Info	(3S)-3-(3-fluoro-4-hydroxyphenyl)-2,2-dimethyl-3-phenyl-N-(1,3-thiazol-2-yl)propanamide Show/Hide	C20H19FN2O2S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0256573 Compound Info	(3S)-3-(3-fluoro-4-hydroxyphenyl)-2,2-dimethyl-3-phenyl-N-(1,3,4-thiadiazol-2-yl)propanamide Show/Hide	C19H18FN3O2S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0078261 Compound Info	2-fluoro-N,N-dimethyl-4-[(5R)-5-[2-methyl-1-oxo-1-(1,3,4-thiadiazol-2-ylamino)propan-2-yl]-5H-chromeno[2,3-b]pyridin-2-yl]benzamide Show/Hide	C27H24FN5O3S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0083140 Compound Info	N,N-dimethyl-4-[(5S)-5-[2-methyl-1-oxo-1-(1,3,4-thiadiazol-2-ylamino)propan-2-yl]-5H-chromeno[2,3-b]pyridin-2-yl]benzamide Show/Hide	C27H25N5O3S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0716109 Compound Info	[(5S)-2-[4-[(Ethylmethylamino)carbonyl]-3-fluorophenyl]-alpha,alpha-dimethyl-N-1,3,4-thiadiazol-2-yl-5H-[1]benzopyrano-[2,3-b]pyridin-5-acetamide Show/Hide	C28H26FN5O3S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0052880 Compound Info	2-[(5S)-9-fluoro-2-[4-(morpholine-4-carbonyl)phenyl]-5H-chromeno[2,3-b]pyridin-5-yl]-2-methyl-N-(1,3,4-thiadiazol-2-yl)propanamide Show/Hide	C29H26FN5O4S	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0053814 Compound Info	N-carbamoyl-2-[(5S)-9-fluoro-2-[4-(morpholine-4-carbonyl)phenyl]-5H-chromeno[2,3-b]pyridin-5-yl]-2-methylpropanamide Show/Hide	C28H27FN4O5	1
1	EC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0143500 Compound Info	1-tert-butyl-3-[(3S)-3-[1-(4-fluorophenyl)indazol-5-yl]-2,2-dimethyl-3-phenylpropyl]urea Show/Hide	C29H33FN4O	1
1	IC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0258531 Compound Info	2,2,2-trifluoro-N-[(3S)-3-[1-(4-fluorophenyl)indazol-5-yl]-2,2-dimethyl-3-phenylpropyl]ethanesulfonamide Show/Hide	C26H25F4N3O2S	1
1	IC50 > 5000 nM Bioactivity Info	TI LI LO TS
CP0313985 Compound Info	3,3,3-trifluoro-N-[(3S)-3-[1-(4-fluorophenyl)indazol-5-yl]-2,2-dimethyl-3-phenylpropyl]propanamide Show/Hide	C27H25F4N3O	1
1	IC50 > 5000 nM Bioactivity Info	TI LI LO TS

Cell Line ID: CL000023 , BTI-Tn-5B1-4

Cell Line Info

Cell Line ID: CL000026 , CHO-K1

Cell Line Info

Cell Line ID: CL000109 , COS-1

Cell Line Info

Cell Line ID: CL000053 , COS-7

Cell Line Info

Cell Line ID: CL000044 , CV-1

Cell Line Info

Cell Line ID: CL000213 , EA.hy 926

Cell Line Info

Cell Line ID: CL000742 , FreeStyle 293-F

Cell Line Info

Cell Line ID: CL000025 , HEK-293T

Cell Line Info

Cell Line ID: CL000006 , HEK293

Cell Line Info

Cell Line ID: CL000148 , Huh-7

Cell Line Info

Cell Line ID: CL000048 , PC-3

Cell Line Info

Cell Line ID: CL000013 , Sf9

Cell Line Info

Cell Line ID: CL000043 , U2OS

Cell Line Info

Cell Line ID: CL000952 , UAS-MR-bla HEK293

Cell Line Info

Biochemical Assays

Compound ID	Compound Name	Compound Formula
CP0068586 Compound Info	(1S,2R,10S,11S,14S,15R,17S)-17-hydroxy-14-(2-hydroxyacetyl)-2-methyl-5-oxotetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-ene-15-carbaldehyde Show/Hide	C21H28O5	2
1	EC50 = 1.3 nM
2	Kd = 0.5 nM
CP0035175 Compound Info	2',15'-dimethyl-5,5'-dioxo-(9'R)-spiro[tetrahydrofuran-2,14'-tetracyclo[8.7.0.02,7.011,15]heptadec-6'-ene]-9-yl ethanethioate Show/Hide	C24H32O4S	3
1	IC50 = 11 nM
2	Ki = 2.323 nM
3	Ki = 5.012 nM
CP0047174 Compound Info	(1S,2R,10S,11S,14R,15S,17S)-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one Show/Hide	C21H28O5	4
1	IC50 = 11 nM
2	IC50 = 18 nM
3	IC50 = 44 nM
4	Ki = 37 nM
CP0198788 Compound Info	6-[(2R,5R)-5-(2-fluorophenyl)-2-methylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C18H18FN3O3	1
1	IC50 = 13 nM
CP0523229 Compound Info	6-[(2R,5R)-2-methyl-5-phenylmorpholin-4-yl]-4H-1,4-benzoxazin-3-one Show/Hide	C19H20N2O3	1
1	IC50 = 13 nM
CP0038813 Compound Info	(1S,2R,10S,11S,14S,15S)-14-acetyl-2,15-dimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadec-6-en-5-one Show/Hide	C21H30O2	3
1	IC50 = 14 nM
2	IC50 > 14 nM
3	Kd = 0.39 nM
CP0422036 Compound Info	4-[(5R)-1-(3-Chloro-4-cyanophenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl]-2-methoxybenzoic Acid Show/Hide	C23H22ClN3O3	1
1	IC50 = 15.2 nM
CP0723935 Compound Info	(S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide Show/Hide	C21H22N4O3	1
1	IC50 = 18 nM
CP0072961 Compound Info	6-[(2R,5R)-5-(3-fluorophenyl)-2-methylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C18H18FN3O3	1
1	IC50 = 19 nM
CP0072958 Compound Info	6-[(2R,5R)-2-methyl-5-phenylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C18H19N3O3	3
1	IC50 = 25 nM
2	Ki = 6.3 nM
3	Ki = 25.12 nM
CP0056351 Compound Info	4-[(5R)-1-(3-Chloro-4-cyanophenyl)-5-cyclopentyl-4,5-dihydro-1H-pyrazol-3-yl]-2-ethoxybenzoic Acid Show/Hide	C24H24ClN3O3	1
1	IC50 = 25.6 nM
CP0008077 Compound Info	(1R,2S,10S,11S,13R,14R,15S,17S)-1-fluoro-14,17-dihydroxy-14-(2-hydroxyacetyl)-2,13,15-trimethyltetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-3,6-dien-5-one Show/Hide	C22H29FO5	3
1	IC50 = 33 nM
2	IC50 = 40 nM
3	Ki = 7.2 nM
CP0035110 Compound Info	4-(2,3-dihydrobenzofuran-7-yl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-1H-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide Show/Hide	C24H23F3N2O5	1
1	IC50 = 38 nM
CP0567193 Compound Info	6-[(2R,5R)-5-(4-fluorophenyl)-2-methylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C18H18FN3O3	1
1	IC50 = 39 nM
CP0250625 Compound Info	4-(5-Fluoro-2-hydroxy-phenyl)-2-hydroxy-4-methyl-2-trifluoromethyl-pentanoic acid (4-methyl-1-oxo-1H-benzo[d][1,2]oxazin-6-yl)-amide Show/Hide	C22H20F4N2O5	1
1	IC50 = 41 nM
CP0389439 Compound Info	2-[(2R,5R)-4-(3-oxo-4H-pyrido[3,2-b][1,4]oxazin-6-yl)-5-phenylmorpholin-2-yl]acetonitrile Show/Hide	C19H18N4O3	1
1	IC50 = 56 nM
CP0523231 Compound Info	6-[(5R)-2,2-dimethyl-5-phenylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C19H21N3O3	1
1	IC50 = 86 nM
CP0437171 Compound Info	7-[(2R,5R)-2-methyl-5-phenylmorpholin-4-yl]-1H-pyrido[3,4-b][1,4]oxazin-2-one Show/Hide	C18H19N3O3	1
1	IC50 = 109 nM
CP0523230 Compound Info	2-[(2R,5R)-2-methyl-5-phenylmorpholin-4-yl]-8H-pyrimido[5,4-b][1,4]oxazin-7-one Show/Hide	C17H18N4O3	1
1	IC50 = 113 nM
CP0100868 Compound Info	methyl (1R,2S,9R,10R,11S,14R,15S,17R)-2,15-dimethyl-5,5'-dioxospiro[18-oxapentacyclo[8.8.0.01,17.02,7.011,15]octadec-6-ene-14,2'-oxolane]-9-carboxylate Show/Hide	C24H30O6	4
1	IC50 = 122 nM
2	IC50 = 240 nM
3	IC50 = 244 nM
4	Ki = 125.89 nM
CP0141819 Compound Info	4-(5-fluoro-2-methoxyphenyl)-2-hydroxy-4-methyl-N-(4-methyl-1-oxo-1H-benzo[d][1,2]oxazin-6-yl)-2-(trifluoromethyl)pentanamide Show/Hide	C23H22F4N2O5	1
1	IC50 = 130 nM
CP0157310 Compound Info	N-[[4-(2,4-dimethylimidazol-1-yl)phenyl]methyl]-2,5-difluorobenzenesulfonamide Show/Hide	C18H17F2N3O2S	2
1	IC50 = 191 nM
2	Ki = 113 nM
CP0556140 Compound Info	6-[(2S,5R)-2-(methoxymethyl)-5-phenylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C19H21N3O4	1
1	IC50 = 276 nM
CP0086230 Compound Info	6-[(3R)-3-phenylmorpholin-4-yl]-4H-1,4-benzoxazin-3-one Show/Hide	C18H18N2O3	1
1	IC50 = 401 nM
CP0035186 Compound Info	(10S,11S,14S,15S,17R)-17-[4-(dimethylamino)phenyl]-14-hydroxy-15-methyl-14-(prop-1-yn-1-yl)tetracyclo[8.7.0.0^{2,7}.0^{11,15}]heptadeca-1,6-dien-5-one Show/Hide	C29H35NO2	5
1	IC50 = 590 nM
2	IC50 = 6000 nM
3	IC50 > 1000 nM
4	Ki = 640 nM
5	Ki > 10000 nM
CP0447334 Compound Info	6-[(2S,5R)-2-methyl-5-phenylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C18H19N3O3	1
1	IC50 = 727 nM
CP0548735 Compound Info	6-[(3R)-3-phenylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C17H17N3O3	1
1	IC50 = 1181 nM
CP0041416 Compound Info	(6alpha)-17-(Acetyloxy)-6-methylpreg-4-ene-3,20-dione Show/Hide	C24H34O4	1
1	IC50 = 1197 nM
CP0558838 Compound Info	7-[(2R,5R)-2-methyl-5-phenylmorpholin-4-yl]-1H-pyrido[2,3-b][1,4]oxazin-2-one Show/Hide	C18H19N3O3	1
1	IC50 = 2225 nM
CP0437172 Compound Info	6-[(2S,5R)-2-(hydroxymethyl)-5-phenylmorpholin-4-yl]-4H-pyrido[3,2-b][1,4]oxazin-3-one Show/Hide	C18H19N3O4	1
1	IC50 > 10000 nM
CP0152273 Compound Info	17-(2-diazoacetyl)-10,13-dimethyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one Show/Hide	C21H28N2O2	1
1	Kd = 0.74 nM
CP0122523 Compound Info	(8R,9S,14S)-17-acetyl-13-(2-diazoacetyl)-10-methyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one Show/Hide	C22H28N2O3	1
1	Kd = 20 nM
CP0230767 Compound Info	(8R,9S,14S)-13-(2-diazoacetyl)-17-[(1R)-1-hydroxyethyl]-10-methyl-1,2,6,7,8,9,11,12,14,15,16,17-dodecahydrocyclopenta[a]phenanthren-3-one Show/Hide	C22H30N2O3	1
1	Kd = 20 nM
CP0157703 Compound Info	[(3R)-7-fluoro-6-(2-methylpropyl)-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]methanesulfonamide Show/Hide	C22H24FN3O6S	1
1	Ki < 0.3162 nM
CP0233172 Compound Info	6-[(3R)-7-fluoro-3-(methylsulfonylmethyl)-2,3-dihydro-1,4-benzoxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C19H17FN2O6S	1
1	Ki = 0.3162 nM
CP0035170 Compound Info	(S)-N-(3-(1-cyclopropyl-1-(2,4-difluorophenyl)ethyl)-1H-indol-7-yl)methanesulfonamide Show/Hide	C20H20F2N2O2S	1
1	Ki = 0.494 nM
CP0361153 Compound Info	2-[(3S)-7-chloro-6-(2-methylpropyl)-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetamide Show/Hide	C23H24ClN3O5	1
1	Ki = 0.5012 nM
CP0157700 Compound Info	2-[(3S)-7-fluoro-6-(2-methylpropyl)-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide Show/Hide	C24H26FN3O5	1
1	Ki = 0.631 nM
CP0233173 Compound Info	[(3R)-7-fluoro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]methanesulfonamide Show/Hide	C18H16FN3O6S	1
1	Ki = 0.7943 nM
CP0157706 Compound Info	6-[(3S)-7-fluoro-3-(2-methylpropyl)-2,3-dihydro-1,4-benzoxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C21H21FN2O4	1
1	Ki = 1.995 nM
CP0849447 Compound Info	(R)-5-benzyl-5-(5-chloro-1H-benzo[d]imidazol-2-yl)-3-((R)-1-(4-fluorophenyl)ethyl)oxazolidine-2,4-dione Show/Hide	C25H19ClFN3O3	1
1	Ki = 2 nM
CP0035174 Compound Info	(R)-N-(3-(1-cyclopropyl-1-(2,4-difluorophenyl)ethyl)-1H-indol-7-yl)methanesulfonamide Show/Hide	C20H20F2N2O2S	1
1	Ki = 2.25 nM
CP0468900 Compound Info	US10017502, Example 8a Show/Hide	C20H18BrN3O5	1
1	Ki = 2.512 nM
CP0233170 Compound Info	US10017502, Example 6b Show/Hide	C20H18ClN3O5	1
1	Ki = 3.162 nM
CP0362783 Compound Info	2-[(3S)-6-cyclopropyl-7-fluoro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetamide Show/Hide	C22H20FN3O5	1
1	Ki = 3.162 nM
CP0157697 Compound Info	US10017502, Example 5a Show/Hide	C19H16ClN3O5	1
1	Ki = 3.981 nM
CP0546490 Compound Info	N-methyl-2-[(3S)-7-methyl-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetamide Show/Hide	C21H21N3O5	1
1	Ki = 3.981 nM
CP0157701 Compound Info	2-[(3S)-4-[2-(carbamoylamino)pyridine-4-carbonyl]-7-fluoro-6-(2-methylpropyl)-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide Show/Hide	C22H26FN5O4	1
1	Ki = 7.943 nM
CP0233171 Compound Info	2-[(2S)-6-chloro-1-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-3,4-dihydro-2H-quinoxalin-2-yl]acetamide Show/Hide	C19H17ClN4O4	1
1	Ki = 7.943 nM
CP0157702 Compound Info	2-[(3S)-7-fluoro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-6-propan-2-yloxy-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide Show/Hide	C23H24FN3O6	1
1	Ki = 10 nM
CP0259336 Compound Info	6-[(3S)-6-(cyclohexylmethyl)-7-fluoro-3-(2-hydroxyethyl)-2,3-dihydro-1,4-benzoxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C26H29FN2O5	1
1	Ki = 10 nM
CP0224693 Compound Info	5-[(E)-(3-fluoro-6H-benzo[c][1]benzoxepin-11-ylidene)methyl]-1,3-dihydrobenzimidazol-2-one Show/Hide	C22H15FN2O2	1
1	Ki = 12.59 nM
CP0565064 Compound Info	N-methyl-2-[(3S)-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-7-(trifluoromethyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetamide Show/Hide	C21H18F3N3O5	1
1	Ki = 12.59 nM
CP0368939 Compound Info	6-[(3R)-3,7-dimethyl-3-(methylsulfonylmethyl)-2H-1,4-benzoxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C21H22N2O6S	1
1	Ki = 15.85 nM
CP0244393 Compound Info	[(3R)-4-(3,4-dihydro-2H-1,4-benzoxazine-6-carbonyl)-7-fluoro-2,3-dihydro-1,4-benzoxazin-3-yl]methanesulfonamide Show/Hide	C18H18FN3O5S	1
1	Ki = 39.81 nM
CP0536855 Compound Info	US10017502, Example 4b Show/Hide	C20H18FN3O5	1
1	Ki = 39.81 nM
CP0157695 Compound Info	N-methyl-2-[(3S)-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetamide Show/Hide	C20H19N3O5	1
1	Ki = 50.12 nM
CP0361154 Compound Info	[(3R)-7-fluoro-4-(1H-indole-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]methanesulfonamide Show/Hide	C18H16FN3O4S	1
1	Ki = 50.12 nM
CP0224692 Compound Info	2-{(3S or 3R)-7-Fluoro-4-[(3-oxo-3,4-dihydro-2H-1,4-benzoxazin-6-yl)carbonyl]-3,4-dihydro-2H-1,4-benzoxazin-3-yl}acetamide Show/Hide	C19H16FN3O5	1
1	Ki = 63.1 nM
CP0361156 Compound Info	methyl 2-[(3S)-7-fluoro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetate Show/Hide	C20H17FN2O6	1
1	Ki = 63.1 nM
CP0244392 Compound Info	2-[(3S)-6-chloro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide Show/Hide	C20H18ClN3O5	1
1	Ki = 100 nM
CP0434545 Compound Info	2-[(3S)-5,7-difluoro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetamide Show/Hide	C19H15F2N3O5	1
1	Ki = 100 nM
CP0537867 Compound Info	6-[(2S)-6-fluoro-2-methyl-3,4-dihydro-2H-quinoline-1-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C19H17FN2O3	1
1	Ki = 125.89 nM
CP0244390 Compound Info	2-[(3S)-7-chloro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetic acid Show/Hide	C19H15ClN2O6	1
1	Ki = 158.49 nM
CP0368938 Compound Info	6-[(3S)-7-fluoro-3-methyl-2,3-dihydro-1,4-benzoxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C18H15FN2O4	1
1	Ki = 158.49 nM
CP0361155 Compound Info	6-[(3S)-7-fluoro-3-(2-hydroxyethyl)-2,3-dihydro-1,4-benzoxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C19H17FN2O5	1
1	Ki = 199.53 nM
CP0576898 Compound Info	2-[(2R)-6-fluoro-1-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-3,4-dihydro-2H-quinolin-2-yl]-N-methylacetamide Show/Hide	C21H20FN3O4	1
1	Ki = 316.23 nM
CP0565067 Compound Info	2-[(3S)-7-chloro-5-methyl-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide Show/Hide	C21H20ClN3O5	1
1	Ki = 398.11 nM
CP0536843 Compound Info	2-[(3S)-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetonitrile Show/Hide	C19H15N3O4	1
1	Ki = 501.19 nM
CP0157704 Compound Info	6-(3,4-dihydro-2H-quinoline-1-carbonyl)-4H-1,4-benzoxazin-3-one Show/Hide	C18H16N2O3	1
1	Ki = 630.96 nM
CP0361157 Compound Info	6-(2-methyl-3,4-dihydro-2H-quinoline-1-carbonyl)-4H-1,4-benzoxazin-3-one Show/Hide	C19H18N2O3	1
1	Ki = 794.33 nM
CP0157705 Compound Info	6-(2,3-dihydro-1,4-benzoxazine-4-carbonyl)-4H-1,4-benzoxazin-3-one Show/Hide	C17H14N2O4	1
1	Ki = 1000 nM
CP0362781 Compound Info	7-[(3S)-7-fluoro-3-(2-methylpropyl)-2,3-dihydro-1,4-benzoxazine-4-carbonyl]-3,4-dihydro-1H-quinolin-2-one Show/Hide	C22H23FN2O3	1
1	Ki = 1000 nM
CP0565063 Compound Info	2-[(3S)-7-cyano-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide Show/Hide	C21H18N4O5	1
1	Ki = 1000 nM
CP0544491 Compound Info	6-[(3S)-3-methyl-2,3-dihydropyrido[3,2-b][1,4]oxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C17H15N3O4	1
1	Ki = 1258.93 nM
CP0368944 Compound Info	6-[(2-methyl-3,4-dihydro-2H-quinolin-1-yl)sulfonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C18H18N2O4S	1
1	Ki = 1995.26 nM
CP0362785 Compound Info	6-[(2R)-6-fluoro-2-methyl-3,4-dihydro-2H-quinoline-1-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C19H17FN2O3	1
1	Ki = 6309.57 nM
CP0577864 Compound Info	2-[(3S)-7-fluoro-4-(2-oxo-1,4-dihydro-3,1-benzoxazine-7-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]-N-methylacetamide Show/Hide	C20H18FN3O5	1
1	Ki > 6309.57 nM
CP0090808 Compound Info	3-(3-fluorophenyl)-1-(4-methylphenyl)-3-(4-nitroanilino)propan-1-one Show/Hide	C22H19FN2O3	1
1	Ki > 10000 nM
CP0157694 Compound Info	US10017502, Example 4a Show/Hide	C20H18FN3O5	1
1	Ki > 10000 nM
CP0224691 Compound Info	2-[(2S)-7-fluoro-1-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-3,5-dihydro-2H-4,1-benzoxazepin-2-yl]acetamide Show/Hide	C20H18FN3O5	1
1	Ki > 10000 nM
CP0233168 Compound Info	N-ethyl-2-[7-fluoro-4-(3-oxo-4H-1,4-benzoxazine-6-carbonyl)-2,3-dihydro-1,4-benzoxazin-3-yl]acetamide Show/Hide	C21H20FN3O5	1
1	Ki > 10000 nM
CP0244389 Compound Info	6-[(3S)-3-(2-aminoethyl)-7-fluoro-2,3-dihydro-1,4-benzoxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C19H18FN3O4	1
1	Ki > 10000 nM
CP0362784 Compound Info	6-[(3R)-7-fluoro-3-methyl-2,3-dihydro-1,4-benzoxazine-4-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C18H15FN2O4	1
1	Ki > 10000 nM
CP0565065 Compound Info	6-[(2R)-5-chloro-2-(2-hydroxyethyl)-2,3-dihydroindole-1-carbonyl]-4H-1,4-benzoxazin-3-one Show/Hide	C19H17ClN2O4	1
1	Ki > 10000 nM

Clinical Information about the Protein

Target 1 ( Mineralocorticoid receptor (MR) )

Target Type	Successful Target
Disease	8 Target-related Diseases				8
1	Hypertension [ICD-11: BA00-BA04]
2	Contraception [ICD-11: QA21]
3	Heart failure [ICD-11: BD10-BD13]
4	Cerebral salt-wasting syndrome [ICD-11: 5C72]
5	Congestive heart failure [ICD-11: BD10]
6	Chronic kidney disease [ICD-11: GB61]
7	Diabetic nephropathy [ICD-11: GB61.Z]
8	Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved Drug(s)	6 Approved Drugs				6
1	Aldosterone	Drug Info	Approved	Hypertension
2	Drospirenone	Drug Info	Approved	Contraception
3	Eplerenone	Drug Info	Approved	Heart failure
4	Fludrocortisone	Drug Info	Approved	Cerebral salt-wasting syndrome
5	Spironolactone	Drug Info	Approved	Congestive heart failure
6	Finerenone	Drug Info	Approved	Chronic kidney disease
Clinical Trial Drug(s)	3 Clinical Trial Drugs				3
1	AZD9977	Drug Info	Phase 2	Heart failure
2	BR-4628	Drug Info	Phase 2	Heart failure
3	LY-2623091	Drug Info	Phase 2	Chronic kidney disease
Discontinued Drug(s)	1 Discontinued Drug				1
1	PF-03882845	Drug Info	Terminated	Diabetic nephropathy
Investigative Drug(s)	1 Investigative Drug				1
1	WAY-255348	Drug Info	Investigative	Solid tumour/cancer

Target 2 ( Aldosterone receptor (NR3C2) )

Target Type	Literature-reported Target

Target 3 ( Corticosteroid receptor type I (NR3C2) )

Target Type	Literature-reported Target

Target 4 ( HUMAN mineralocorticoid receptor (MR) )

Target Type	Unknown Type Target
Disease	1 Target-related Disease				1
1	Coronavirus Disease 2019 (COVID-19) [ICD-11: 1D6Y]
Investigative Drug(s)	1 Investigative Drug				1
1	Eplerenone	Drug Info	Investigative	Coronavirus Disease 2019 (COVID-19)

Cite

About MolBiC

Correspondence

Prof. Feng ZHU

Prof. Leo, Lianyi Han